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Catalog No. Product Name Information Product Use Citations Product Validations
E0020New Lupenone Lupenone (Lup-20(29)-en-3-one, lupeone) is an isolated compound exhibiting anti-oxidative, anti-inflammation, and anti-diabetic activities. Lupenone can protect SH-SY5y cells against METH-induced neuronal apoptosis through the PI3K/Akt pathway.
E0129New Oxysophocarpine Oxysophocarpine (OSC) is an alkaloid extracted from Sophora alopecuroides. Oxysophocarpine inhibits the growth and metastasis of oral squamous cell carcinoma (OSCC) by targeting the Nrf2/HO-1 axis. OSC protects cells against apoptosis and inflammatory responses and compromised miR-155 activity by attenuating MAPK and NF-κB pathways.
E0212New Cornuside

Cornuside is a bisiridoid glucoside compound isolated from the fruit of Cornus officinalis SIEB. et ZUCC. Cornuside suppresses lipopolysaccharide-induced inflammatory mediators by inhibiting NF-κB activation in RAW 264.7 macrophages. Cornuside attenuates apoptosis in rat cortical neurons.

S0231 NSC15364 NSC 15364 (compound 59) is an inhibitor that directly interacts with VDAC1 and prevents VDAC1 oligomerization, concomitant with an inhibition of apoptosis.
S0411 BAM 15 BAM 15 is a novel mitochondrial protonophore uncoupler capable of protecting mammals from acute renal ischemic-reperfusion injury and cold-induced microtubule damage. BAM 15 is also a potent AMPK activator. BAM 15 attenuates transportation-induced apoptosis in iPS-differentiated retinal tissue.
Neuroscience, 2012, 223:238-45
S0539 BTZO-1 BTZO-1 binds to macrophage migration inhibitory factor (MIF) with Kd of 68.6 nM. BTZO-1 activats antioxidant response element (ARE)-mediated gene expression and suppresses oxidative stress-induced cardiomyocyte apoptosis in vitro.
S0947 Cafestol Cafestol is a natural diterpenes extracted from coffee beans. Cafestol induces apoptosis and regulates a variety of inflammatory mediators to reduce inflammation. Cafestol inhibits PI3K/Akt pathway. Cafestol also can reduce the production of ROS in the leukemia cell line HL60.
S1077 SB202190 (FHPI) SB202190 (FHPI) is a potent p38 MAPK inhibitor targeting p38α/β with IC50 of 50 nM/100 nM in cell-free assays, sometimes used instead of SB 203580 to investigate potential roles for SAPK2a/p38 in vivo. SB202190 inhibits endothelial cell apoptosis via induction of autophagy and heme oxygenase-1. SB202190 significantly suppresses Erastin‐dependent ferroptosis.
Nature, 2021, 600(7888):314-318
Immunity, 2021, S1074-7613(21)00210-7
Nat Commun, 2021, 12(1):6941
S1132 3-Aminobenzamide 3-Aminobenzamide (3-ABA , 3-Amino Benzamide, 3-AB) is a potent inhibitor of Poly(ADP-ribose)polymerase (PARP) and inhibits cell apoptosis after SCI (Spinal Cord Injury) in caspase-independent way.
Cell Death Discov, 2021, 7(1):181
Acta Pharm Sin B, 2019, 9(4):782-793
J Cell Biochem, 2017, 118(11):3943-3952
S1386 Nafamostat mesilate (FUT-175) Nafamostat mesilate (FUT-175) is a synthetic serine protease inhibitor, used as an anticoagulant during hemodialysis. Nafamostat mesylate blocks activation of SARS-CoV-2 and is investigated as a new treatment option for COVID-19. Nafamostat Mesilate attenuates inflammation and apoptosis.
bioRxiv, 2021, 2021.03.31.437960
EMBO J, 2020, e2020106057
bioRxiv, 2020, 2020.10.02.324228
S1733 Methylprednisolone (NSC-19987) Methylprednisolone (NSC-19987) is a synthetic glucocorticoid receptor agonist, used to achieve prompt suppression of inflammation. Methylprednisolone activates ACE2 and reduces IL-6 levels, thus improves severe or critical COVID-19. Methylprednisolone markedly reduces autophagy and apoptosis.
Drug Test Anal, 2020, 10.1002/dta.2917
Nat Med, 2017, 23(4):424-428
Trop J Pharm Res, 2014, 13 (1): 53-59
S2872 GW5074 GW5074 is a potent and selective c-Raf inhibitor with IC50 of 9 nM, no effect on the activities of JNK1/2/3, MEK1, MKK6/7, CDK1/2, c-Src, p38 MAP, VEGFR2 or c-Fms is noted. GW5074 inhibits LK-induced apoptosis.
Cell Res, 2021, 10.1038/s41422-021-00532-7
Antibiotics (Basel), 2021, 10(10)1223
J Neurosci, 2020, 40(34):6522-6535
S3236 Mesaconitine Mesaconitine, one of the aconite alkaloids in Aconiti tuber, increases the [Ca2+]i level in endothelial cells by influx of Ca2+ from extracellular spaces.
S3267 Kaempferol-3-O-rutinoside Kaempferol-3-O-rutinoside (Nicotiflorin, Nikotoflorin, Kaempferol 3-O-β-rutinoside), a flavonoid extracted from Carthamus tinctorius, alters the shape and structure of injured neurons, decreases the number of apoptotic cells, down-regulates expression of p-JAK2, p-STAT3, caspase-3, and Bax and decreases Bax immunoredactivity, and increases Bcl-2 protein expression and immunoreactivity.
S3269 Acetylcorynoline Acetylcorynoline, a major alkaloid component derived from Corydalis bungeana which is a traditional Chinese medical herb, shows anti-inflammatory properties. Acetylcorynoline may decrease egl-1 expression to suppress apoptosis pathways and increase rpn5 expression to enhance the activity of proteasomes.
S3275 Senkyunolide I Senkyunolide I (SEI, SENI) is an orally active compound isolated from Ligusticum chuanxiong with analgesic, anti-migraine, neuroprotective, anti-oxidation and anti-apoptosis activities. Senkyunolide I (SEI, SENI) up-regulates the phosphorylation of Erk1/2 and induces Nrf2 nuclear translocation with enhanced HO-1 and NQO1 expressions. Senkyunolide I (SEI, SENI) promotes the ratio of Bcl-2/Bax and inhibits the expressions of cleaved caspase 3 and caspase 9.
Cell Commun Signal, 2021, 19(1):115
S3294 Demethyl-Coclaurine Demethyl-Coclaurine (Higenamine, Norcoclaurine), the key component of the Chinese herb aconite root, is a beta-2 adrenergic receptor (β2-AR) agonist. Demethyl-Coclaurine stimulates AKT phosphorylation and requires PI3K activation for the anti-apoptotic effect in cardiomyocytes.
S3576New TVB-3166 TVB-3166 is an orally-available, reversible, potent and selective inhibitor of fatty acid synthase (FASN) with IC50 of 0.042 μM in an in vitro biochemical assay. TVB-3166 induces apoptosis, and inhibits in-vivo xenograft tumor growth.
S4484New Trametinib DMSO solvate Trametinib (GSK1120212, JTP-74057, Mekinist) DMSO solvate is a highly specific and potent MEK1/2 inhibitor with IC50 of 0.92 nM/1.8 nM in cell-free assay. Trametinib activates autophagy and induces apoptosis.
S4513New RGD peptide (GRGDNP) RGD peptide (GRGDNP) is an inhibitor of binding of integrins to the extracellular matrixs. RGD peptide (GRGDNP) induces apoptosis presumably through direct activation of caspase-3.
S5971New Pemetrexed Pemetrexed (LY231514, Alimta) is a novel antifolate and antimetabolite for thymidylate synthase (TS), dihydrofolate reductase (DHFR) and glycinamide ribonucleotide formyltransferase (GARFT) with Ki of 1.3 nM, 7.2 nM and 65 nM in cell-free assays, respectively. Pemetrexed induces autophagy and apoptosis.
J Exp Clin Cancer Res, 2021, 40(1):344
Br J Cancer, 2021, 10.1038/s41416-021-01441-7
Front Oncol, 2021, 11:711043
S6812New Z-Guggulsterone Z-Guggulsterone, a constituent of Ayurvedic medicinal plant Commiphora mukul, inhibits angiogenesis in vitro and in vivo. Z-Guggulsterone exhibits anti-inflammatory effects in microglia. Z-Guggulsterone induces apoptosis in gastric cancer cells through the intrinsic mitochondria-dependent pathway.
S7033 GSK2656157 GSK2656157 is an ATP-competitive and highly selective inhibitor of PERK with IC50 of 0.9 nM in a cell-free assay, 500-fold greater against a panel of 300 kinases. GSK2656157 decreases apoptosis and inhibits excessive autophagy.
Neurobiol Dis, 2021, 156:105407
Cell Death Dis, 2020, 11(2):125
Sci Rep, 2020, 10(1):9666
S8037 Necrostatin-1 Necrostatin-1 (Nec-1) is a specific RIP1 (RIPK1) inhibitor and inhibits TNF-α-induced necroptosis with EC50 of 490 nM in 293T cells. Necrostatin-1 also blocks IDO and suppresses autophagy and apoptosis.
Cells, 2022, 11(1)134
Int J Mol Sci, 2022, 23(1)506
Cell, 2021, S0092-8674(21)00885-0
S8632 Chk2 Inhibitor II (BML-277) Chk2 Inhibitor II (BML-277) is an ATP-competitive inhibitor of Chk2 with IC50 of 15 nM. It is 1000-fold more selective toward Chk2 serine/threonine kinase than for Chk1 and Cdk1/B kinases. Chk2 Inhibitor II (BML-277) dose dependently protects human CD4(+) and CD8(+) T-cells from apoptosis due to ionizing radiation.
Mol Cancer Res, 2021, 10.1158/1541-7786.MCR-20-0791
DNA Repair (Amst), 2021, 110:103264
mBio, 2020, 11(3):e01190-20
S8974 GSK2795039 GSK2795039 is an inhibitor of NADPH oxidase 2 (NOX2) with pIC50 of 6.57 for NOX2-mediated activation of HRP/Amplex Red. GSK2795039 inhibits reactive oxygen species (ROS) production, NADPH consumption and reduces apoptosis.
S9631New Puromycin aminonucleoside Puromycin aminonucleoside (NSC 3056, PAN, Stylomycin aminonucleoside, ARDMA, SAN), the aminonucleoside portion of the antibiotic puromycin, is a reversible inhibitor of dipeptidyl-peptidase II and cytosol alanyl aminopeptidase that induces apoptosis in mesangial cells (MCs) accompanied by declined cell viability and enhanced inflammatory response.
S9668 PKR-IN-C16 PKR-IN-C16 (imoxin, C16, Imidazolo-oxindole PKR inhibitor C16) is a specific inhibitor of RNA-dependent protein kinase (PKR, Protein Kinase R, EIF2AK2). PKR-IN-C16 prevents apoptosis and IL-1β production in an acute excitotoxic rat model with a neuroinflammatory component.
Cell Chem Biol, 2021, S2451-9456(21)00303-2
Pulm Circ, 2021, 11(4):20458940211046156
S9724New SZL P1-41 SZL P1-41 (compound #25) is a specific inhibitor of S-phase kinase-associated protein 2 (Skp2) that indeed binds to Skp2, prevents Skp2-Skp1 interaction and inhibits Skp2 SCF E3 ligase activity, which consequently suppresses survival of cancer cells and cancer stem cells. SZL P1-41 causes higher apoptosis rates in cancer cells.
S9805New WM-3835 WM-3835 is a novel and high-specific small molecule Lysine Acetyltransferase 7 (KAT7, MYST2, HBO1) inhibitor, able to potently suppressed OS cell proliferation and migration, and leads to apoptosis activation.
S0056 (E/Z)-BCI (E/Z)-BCI (BCI, NSC 150117) is an inhibitor of dual specific phosphatase 1/6 (DUSP1/DUSP6) and mitogen-activated protein kinase with EC50 of 13.3 μM and 8.0 μM for DUSP6 and DUSP1 in cells, respectively. (E)-BCI induces apoptosis via generation of reactive oxygen species (ROS) and activation of intrinsic mitochondrial pathway in H1299 lung cancer cells.
S0103 ML327 ML327 is an isoxazole compound that blocks MYC expression and tumor formation in neuroblastoma. ML327 also restores E-cadherin expression with In-Cell Western EC50 of 1.0 μM. ML327 induces apoptosis.
S0149 C-DIM5 C-DIM5 (DIM-C-pPhOCH3) is an agonist of Nur77 (Nerve growth factor-induced Bα (NGFI-Bα)/nuclear receptor 4A1 (NR4A1)) which is an orphan nuclear receptor. C-DIM5 (DIM-C-pPhOCH3) decreases survival and induces apoptosis in RKO colon cancer cells.
S0278 SU5614 SU5614 (Chloro-SU5416, Chloro-Semaxanib) is a small molecule receptor tyrosine kinases (RTK) inhibitor of VEGFR-2, c-kit, and both wild-type and mutant FLT3. SU5614 reduces cell proliferation and induces apoptosis.
Adv Sci (Weinh), 2021, e2101848
S0354 Alsterpaullone Alsterpaullone (Alp, 9-Nitropaullone, NSC 705701) is a potent inhibitor of CDK with IC50 of 35 nM, 15 nM, 200 nM and 40 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E and CDK5/p35, respectively. Alsterpaullone also acts as a potent inhibitor of glycogen synthase kinase-3 (GSK-3) with IC50 of both 4 nM for GSK-3α and GSK-3β. Alsterpaullone induces apoptosis by activation of caspase-9. Alsterpaullone has antitumor activity and possesses potential for the treatment of neurodegenerative and proliferative disorders.
S0407 XCT790 XCT-790 (Compound 12) is a potent and selective inverse agonist for estrogen-related receptor α (ERRα) with IC50 of 0.37 μM. XCT-790 (Compound 12) is inactive against ERRγ and the estrogen receptors ERα and ERβ. XCT-790 (Compound 12) significantly inhibits in vivo tumor growth and angiogenesis, and induces apoptosis.
S0444 Indibulin Indibulin (ZIO 301, D 24851, Zybulin) is an orally applied inhibitor of tubulin assembly with potent anticancer activity. Indibulin induces mitotic arrest and apoptosis.
Bioorg Med Chem, 2020, 28(20):115712
S0445 SC-43 SC-43, a sorafenib derivative, is an agonist of Src-homology protein tyrosine phosphatase-1 (SHP-1/PTPN6) and reduces liver fibrosis. SC-43 reduces p-STAT3 and induces apoptosis with anti-tumor activity.
S0709 Tubastatin A TFA Tubastatin A TFA (Tubastatin A trifluoroacetate salt) is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay. It is selective against all the other isozymes (1000-fold) except HDAC8 (57-fold). Tubastatin A promotes autophagy and increases apoptosis.
S0765 MAZ51 MAZ51 is a potent and selective inhibitor of vascular endothelial growth factor receptor (VEGFR)-3 (Flt-4) tyrosine kinase. MAZ51 induces cell rounding and G2/M cell cycle arrest in glioma cells through phosphorylation of Akt/GSK3β and activation of RhoA. MAZ51 inhibits the proliferation and induces the apoptosis of a variety of non-VEGFR-3-expressing tumor cell lines.
S0817 SKI-V SKI V is a noncompetitive and potent inhibitor of non-lipid sphingosine kinase with IC50 of 2 μM for GST-hSK. SKI-V also inhibits PI3K with IC50 of 6 μM for hPI3k. SKI-V decreases formation of the mitogenic second messenger sphingosine-1-phosphate (S1P) and induces apoptosis with antitumor activity.
S0884 RA-9 RA-9 is a cell-permeable, potent and selective inhibitor of proteasome-associated deubiquitinating enzymes (DUBs) with favorable toxicity profile and anticancer activity. RA-9 selectively induces apoptosis in ovarian cancer cell lines.
S0913 4',5,7-Trimethoxyflavone 4',5,7-Trimethoxyflavone (5,​7,​4'-​Trimethoxyflavone, TMF) is a flavonoid isolated from Kaempferia parviflora (KP) that induces apoptosis. 4',5,7-Trimethoxyflavone increases sub-G1 phase, DNA fragmentation, annexin-V/PI staining and Bax/Bcl-xL ratio, activates caspase-3 and degrades poly (ADP-ribose) polymerase (PARP) protein.
S0918 Ginkgolic acid C17:1 Ginkgolic acid C17:1 (GAC 17:1) inhibits constitutive activation of STAT3 through the abrogation of upstream JAK2 and Src. Ginkgolic acid C17:1 can induce the substantial expression of PTEN and SHP-1. Ginkgolic acid C17:1 induces apoptosis of tumor cells.
S0931 Jaceosidin Jaceosidin, a flavonoid isolated from Artemisia vestita, possesses anti-tumor and anti-proliferative activities in many cancer cells. Jaceosidin induces apoptosis, activates Bax and down-regulates Mcl-1 and c-FLIP expression. Jaceosidin inhibits COX-2 expression and NF-κB activation.
S0949 Cucurbitacin IIb Cucurbitacin IIb (CuIIb, Dihydrocucurbitacin F, 25-deacetyl hemslecin A) inhibits phosphorylation of STAT3, JNK and Erk1/2, enhances the phosphorylation of IκB and NF-κB, blocks nuclear translocation of NF-κB and decreases mRNA levels of IκBα and TNF-α. Cucurbitacin IIb exhibits anti-inflammatory activity and induces apoptosis. Cucurbitacin IIb is isolated from Hemsleya amabilis.
S1002 ABT-737 ABT-737 is a BH3 mimetic inhibitor of Bcl-xL, Bcl-2 and Bcl-w with EC50 of 78.7 nM, 30.3 nM and 197.8 nM in cell-free assays, respectively; no inhibition observed against Mcl-1, Bcl-B or Bfl-1. ABT-737 induces mitochondrial pathway apoptosis and mitophagy. Phase 2.
ACS Appl Mater Interfaces, 2022, 10.1021/acsami.1c22138
Science, 2021, 371(6535)eabc5386
Cell Death Dis, 2021, 12(8):736
S1003 Linifanib (ABT-869) Linifanib (ABT-869, AL39324, RG3635) is a novel, potent ATP-competitive VEGFR/PDGFR inhibitor for KDR, CSF-1R, Flt-1/3 and PDGFRβ with IC50 of 4 nM, 3 nM, 3 nM/4 nM and 66 nM respectively, mostly effective in mutant kinase-dependent cancer cells (i.e. FLT3). Linifanib (ABT-869) induces autophagy and apoptosis. Phase 3.
Cancer Lett, 2021, 507:80-88
Hum Cell, 2021, 34(6):1911-1918
Hum Cell, 2021, 10.1007/s13577-021-00639-4
S1004 Veliparib (ABT-888) Veliparib (ABT-888, NSC 737664) is a potent inhibitor of PARP1 and PARP2 with Ki of 5.2 nM and 2.9 nM in cell-free assays, respectively. It is inactive to SIRT2. Veliparib increases autophagy and apoptosis. Phase 3.
Cell, 2022, 185(1):169-183.e19
Transl Oncol, 2022, 15(1):101283
Sci Transl Med, 2021, 13(592)eabc7211
S1008 Selumetinib (AZD6244) Selumetinib (AZD6244, ARRY-142886) is a potent, highly selective MEK inhibitor with IC50 of 14 nM for MEK1 and Kd value of 530 nM for MEK2. It also inhibits ERK1/2 phosphorylation with IC50 of 10 nM, no inhibition to p38α, MKK6, EGFR, ErbB2, ERK2, B-Raf, etc. Selumetinib suppresses cell proliferation, migration and trigger apoptosis. Phase 3.
Proc Natl Acad Sci U S A, 2022, 119(3)e2114134119
Nat Cell Biol, 2021, 23(4):377-390
J Extracell Vesicles, 2021, 10(8):e12091
S1020 PD184352 (CI-1040) PD184352 (CI-1040) is an ATP non-competitive MEK1/2 inhibitor with IC50 of 17 nM in cell-based assays, 100-fold more selective for MEK1/2 than MEK5. PD184352 (CI-1040) selectively induces apoptosis. Phase 2.
Proc Natl Acad Sci U S A, 2022, 119(3)e2114134119
Cell Syst, 2021, S2405-4712(21)00111-3
Elife, 2021, 10e66596
S1021 Dasatinib (BMS-354825) Dasatinib (BMS-354825) is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM in cell-free assays, respectively. Dasatinib induces autophagy and apoptosis with anti-tumor activity.
ACS Appl Mater Interfaces, 2022, 10.1021/acsami.1c22138
J Immunol, 2022, ji2100400
Nat Immunol, 2021, 10.1038/s41590-021-00948-8
S1025 Gefitinib (ZD1839) Gefitinib (ZD-1839, Iressa) is an EGFR inhibitor for Tyr1173, Tyr992, Tyr1173 and Tyr992 in the NR6wtEGFR and NR6W cells with IC50 of 37 nM, 37nM, 26 nM and 57 nM, respectively. Gefitinib promotes autophagy and apoptosis of lung cancer cells via blockade of the PI3K/AKT/mTOR pathway.
Cell Death Dis, 2022, 13(1):41
Cancer Med, 2022, 10.1002/cam4.4504
BMC Pulm Med, 2022, 22(1):27
S1029 Lenalidomide (CC-5013) Lenalidomide (CC-5013) is a TNF-α secretion inhibitor with IC50 of 13 nM in PBMCs. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide promotes cleaved caspase-3 expression and inhibit VEGF expression and induces apoptosis.
Blood Adv, 2022, bloodadvances.2021005772
Adv Sci (Weinh), 2021, e2004846
Sci Adv, 2021, 7(6)eabd6263
S1030 Panobinostat (LBH589) Panobinostat (LBH589, NVP-LBH589) is a novel broad-spectrum HDAC inhibitor with IC50 of 5 nM in a cell-free assay. Panobinostat (LBH589) induces autophagy and apoptosis. Panobinostat effectively disrupts HIV latency in vivo. Phase 3.
Neoplasia, 2022, 24(2):63-75
Nat Med, 2021, 10.1038/s41591-020-01212-6
Cell Stem Cell, 2021, 28(1):48-62.e6
S1038 PI-103 PI-103 is a multi-targeted PI3K inhibitor for p110α/β/δ/γ with IC50 of 2 nM/3 nM/3 nM/15 nM in cell-free assays, less potent to mTOR/DNA-PK with IC50 of 30 nM/23 nM. PI-103 induces apoptosis in murine T-cell Lymphoma.
Adv Healthc Mater, 2021, e2101944
Cell Chem Biol, 2021, S2451-9456(21)00254-3
Neurobiol Dis, 2021, 156:105407
S1040 Sorafenib (BAY 43-9006) tosylate Sorafenib (BAY 43-9006) tosylate is a multikinase inhibitor of Raf-1 and B-Raf with IC50 of 6 nM and 22 nM in cell-free assays, respectively. Sorafenib Tosylate inhibits VEGFR-2, VEGFR-3, PDGFR-β, Flt-3 and c-KIT with IC50 of 90 nM, 20 nM, 57 nM, 59 nM and 68 nM, respectively. Sorafenib Tosylate induces autophagy and apoptosis and activates ferroptosis with anti-tumor activity.
Cell Death Dis, 2022, 13(1):35
Cancer Cell, 2021, S1535-6108(21)00659-0
Leukemia, 2021, 10.1038/s41375-021-01308-z
S1042 Sunitinib (SU11248) malate Sunitinib (SU11248) malate is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM in cell-free assays, and also inhibits c-Kit. Sunitinib Malate effectively inhibits autophosphorylation of Ire1α. Sunitinib Malate increases both death receptor and mitochondrial-dependent apoptosis.
Cancer Cell, 2021, S1535-6108(21)00659-0
Adv Sci (Weinh), 2021, 8(2):2001596
Adv Sci (Weinh), 2021, 8(2):2001596
S1044 Temsirolimus (CCI-779) Temsirolimus (CCI-779, NSC 683864) is a specific mTOR inhibitor with IC50 of 1.76 μM in a cell-free assay. Temsirolimus induces autophagy and apoptosis.
Mol Syst Biol, 2021, 17(8):e10239
Cell Death Dis, 2021, 12(1):108
J Clin Endocrinol Metab, 2021, dgab020
S1046 Vandetanib (ZD6474) Vandetanib (ZD6474) is a potent inhibitor of VEGFR2 with IC50 of 40 nM in a cell-free assay. It also inhibits VEGFR3 and EGFR with IC50 of 110 nM and 500 nM, respectively. Not sensitive to PDGFRβ, Flt1, Tie-2 and FGFR1 with IC50 of 1.1-3.6 μM. No activity against MEK, CDK2, c-Kit, erbB2, FAK, PDK1, Akt and IGF-1R with IC50 above 10 μM. Vandetanib (ZD6474) increases apoptosis and induces autophagy by increasing the level of reactive oxygen species (ROS).
J Clin Endocrinol Metab, 2021, dgab020
Cell Chem Biol, 2021, S2451-9456(21)00303-2
Cancer Discov, 2021, candisc.1201.2020
S1052 Elesclomol (STA-4783) Elesclomol (STA-4783) is a novel potent oxidative stress inducer that elicits pro-apoptosis events among tumor cells. Phase 3.
J Exp Clin Cancer Res, 2021, 40(1):228
Mol Oncol, 2021, 10.1002/1878-0261.13079
Nat Commun, 2020, 15;11(1):2423
S1053 Entinostat (MS-275) Entinostat (MS-275, SNDX-275) strongly inhibits HDAC1 and HDAC3 with IC50 of 0.51 μM and 1.7 μM in cell-free assays, compared with HDACs 4, 6, 8, and 10. Entinostat induces autophagy and apoptosis. Phase 3.
Science, 2021, 372(6537)eaba1786
Nat Chem Biol, 2021, 10.1038/s41589-021-00772-z
Nat Commun, 2021, 12(1):2699
S1065 Pictilisib (GDC-0941) Pictilisib (GDC-0941, RG7321) is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM in cell-free assays, with modest selectivity against p110β (11-fold) and p110γ (25-fold). Pictilisib (GDC-0941) induces autophagy and apoptosis. Phase 2.
Nat Commun, 2022, 13(1):245
Cancer Cell, 2021, S1535-6108(21)00383-4
Cancer Cell, 2021, S1535-6108(21)00492-X
S1069 Luminespib (NVP-AUY922) Luminespib (AUY-922, NVP-AUY922, VER-52296) is a highly potent HSP90 inhibitor for HSP90α/β with IC50 of 13 nM /21 nM in cell-free assays, weaker potency against the HSP90 family members GRP94 and TRAP-1, exhibits the tightest binding of any small-molecule HSP90 ligand. Luminespib (AUY-922, NVP-AUY922) effectively downregulates and destabilizes the IGF-1Rβ protein and results in growth inhibition, autophagy and apoptosis. Phase 2.
Cell Rep, 2021, 34(11):108870
Haematologica, 2021, 10.3324/haematol.2021.278743
Cancers (Basel), 2021, 13(15)3850
S1078 MK-2206 2HCl MK-2206 2HCl is a highly selective inhibitor of Akt1/2/3 with IC50 of 8 nM/12 nM/65 nM in cell-free assays, respectively; no inhibitory activities against 250 other protein kinases observed. MK-2206 2HCl induces autophagy and apoptosis in cancer cells. Phase 2.
Nat Commun, 2022, 13(1):245
Cell Death Dis, 2022, 13(1):44
J Cell Mol Med, 2022, 10.1111/jcmm.17150
S1080 SU11274 SU11274 (PKI-SU11274) is a selective Met (c-Met) inhibitor with IC50 of 10 nM in cell-free assays, no effects on PGDFRβ, EGFR or Tie2. SU11274 induces autophagy, apoptosis and cell cycle arrest.
Cell Rep, 2021, 37(5):109905
Signal Transduct Target Ther, 2021, 6(1):401
Cell Chem Biol, 2021, S2451-9456(21)00303-2
S1105 LY294002 LY294002 (SF 1101, NSC 697286) is the first synthetic molecule known to inhibit PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM, respectively; more stable in solution than Wortmannin, and also blocks autophagosome formation. It not only binds to class I PI3Ks and other PI3K-related kinases, but also to novel targets seemingly unrelated to the PI3K family. LY294002 also inhibits CK2 with IC50 of 98 nM. LY294002 is a non-specific DNA-PKcs inhibitor and activates autophagy and apoptosis.
Immunity, 2022, 55(1):159-173.e9
Microbiol Spectr, 2022, e0188121
Cell Biol Toxicol, 2022, 10.1007/s10565-021-09670-5
S1107 Danusertib (PHA-739358) Danusertib (PHA-739358) is an Aurora kinase inhibitor for Aurora A/B/C with IC50 of 13 nM/79 nM/61 nM in cell-free assays, modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc. Danusertib induces apoptosis, cell cycle arrest, and autophagy. Phase 2.
Cancers (Basel), 2021, 13(6)1205
Life Sci Alliance, 2021, 4(8)e202101019
Mol Cell, 2020, 80(6):1104-1122.e9
S1108 TAE684 (NVP-TAE684) TAE684 (NVP-TAE684) is a potent and selective ALK inhibitor with IC50 of 3 nM in a cell-free assay, 100-fold more sensitive for ALK than InsR. TAE684 (NVP-TAE684) induces cell cycle arrest and apoptosis.
Cereb Cortex, 2021, bhab058
Cell Death Dis, 2021, 12(8):741
Mol Oncol, 2021, 15(8):2011-2025
S1109 BI 2536 BI-2536 is a potent Plk1 inhibitor with IC50 of 0.83 nM in a cell-free assay. BI-2536 inhibits Bromodomain 4 (BRD4) with Kd of 37 nM and potently suppresses c-Myc expression. BI-2536 induces apoptosis and attenuates autophagy. Phase 2.
Science, 2021, 371(6535)eabc5386
Nat Commun, 2021, 12(1):5356
Proc Natl Acad Sci U S A, 2021, 118(34)e2108145118
S1118 XL147 analogue XL147 analogue (SAR245408) is a selective and reversible class I PI3K inhibitor for PI3Kα/δ/γ with IC50 of 39 nM/36 nM/23 nM in cell-free assays, less potent to PI3Kβ. XL147 analogue induces apoptosis. Phase 1/2.
Hum Cell, 2021, 10.1007/s13577-021-00579-z
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Hum Cell, 2021, 34(6):1911-1918
S1119 Cabozantinib (BMS-907351) Cabozantinib (XL184, BMS-907351) is a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM in cell-free assays, respectively. Cabozantinib induces PUMA-dependent apoptosis in colon cancer cells via AKT/GSK-3β/NF-κB signaling pathway.
Sci Adv, 2021, 7(48):eabg9509
Clin Cancer Res, 2021, 27(9):2533-2548
Cancers (Basel), 2021, 13(3)E372
S1120 Everolimus (RAD001) Everolimus (RAD001, SDZ-RAD) is an mTOR inhibitor of FKBP12 with IC50 of 1.6-2.4 nM in a cell-free assay. Everolimus induces cell apoptosis and autophagy and inhibits tumor cells proliferation.
Cold Spring Harb Mol Case Stud, 2022, 8(1)a006140
Cell, 2021, 184(25):6119-6137.e26
Cancer Cell, 2021, S1535-6108(21)00659-0
S1122 Mocetinostat (MGCD0103) Mocetinostat (MGCD0103, MG0103) is a potent HDAC inhibitor with most potency for HDAC1 with IC50 of 0.15 μM in a cell-free assay, 2- to 10- fold selectivity against HDAC2, 3, and 11, and no activity to HDAC4, 5, 6, 7, and 8. Mocetinostat (MGCD0103) induces apoptosis and autophagy. Phase 2.
Cancer Cell, 2021, S1535-6108(20)30662-0
Nat Commun, 2021, 12(1):5056
Cell Rep, 2021, 37(12):110129
S1133 Alisertib (MLN8237) Alisertib (MLN8237) is a selective Aurora A inhibitor with IC50 of 1.2 nM in a cell-free assay. It has >200-fold higher selectivity for Aurora A than Aurora B. Alisertib induces cell cycle arrest, apoptosis and autophagy. Phase 3.
Mol Oncol, 2022, 16(1):219-249
Cancer Cell, 2021, S1535-6108(21)00383-4
Cancer Cell, 2021, S1535-6108(21)00492-X
S1135 Pemetrexed (LY-231514) disodium Pemetrexed (LY-231514) disodium is a novel antifolate and antimetabolite for TS, DHFR and GARFT with Ki of 1.3 nM, 7.2 nM and 65 nM in cell-free assays, respectively. Pemetrexed induces autophagy and apoptosis.
J Exp Clin Cancer Res, 2021, 40(1):344
Br J Cancer, 2021, 10.1038/s41416-021-01441-7
Cell Chem Biol, 2021, S2451-9456(21)00442-6
S1141 Tanespimycin (17-AAG) Tanespimycin (17-AAG, CP127374, NSC-330507, KOS 953) is a potent HSP90 inhibitor with IC50 of 5 nM in a cell-free assay, having a 100-fold higher binding affinity for HSP90 derived from tumour cells than HSP90 from normal cells. Tanespimycin (17-AAG) induces apoptosis, necrosis, autophagy and mitophagy. Phase 3.
ACS Appl Mater Interfaces, 2022, 10.1021/acsami.1c22138
Cell Stem Cell, 2021, S1934-5909(21)00294-0
Mol Cell, 2021, 81(6):1170-1186.e10
S1145 SNS-032 (BMS-387032) SNS-032 (BMS-387032) has firstly been described as a selective inhibitor of CDK2 with IC50 of 48 nM in cell-free assays and is 10- and 20-fold selective over CDK1/CDK4. It is also found to be sensitive to CDK7/9 with IC50 of 62 nM/4 nM, with little effect on CDK6. SNS-032 (BMS-387032) induces apoptosis. Phase 1.
Cancers (Basel), 2021, 13(15)3906
Cell Death Dis, 2021, 12(11):1048
Cells, 2021, 10(3)550
S1156 Capecitabine (RO 09-1978) Capecitabine (RO 09-1978) is a tumor-selective fluoropyrimidine carbamate, which achieves higher intratumoral 5-FU level with lower toxicity than 5-FU. Capecitabine treatment of HCT-15 cells causes condensation of DNA and induces apoptosis.
Adv Sci (Weinh), 2021, e2103360
Hum Cell, 2021, 10.1007/s13577-021-00579-z
Hum Cell, 2021, 10.1007/s13577-021-00639-4
S1159 Ganetespib (STA-9090) Ganetespib (STA-9090) is an HSP90 inhibitor with IC50 of 4 nM in OSA 8 cells, induces apoptosis of OSA cells while normal osteoblasts are not affected; active metabolite of STA-1474. Phase 3.
Nat Commun, 2021, 12(1):5919
Cell Death Dis, 2021, 12(1):126
Cell Death Dis, 2021, 12(1):126
S1181 ENMD-2076 ENMD-2076 has selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold selective for Aurora A than over Aurora B and less potent to RET, SRC, NTRK1/TRKA, CSF1R/FMS, VEGFR2/KDR, FGFR and PDGFRα. ENMD-2076 inhibits the growth of a wide range of human solid tumor and hematopoietic cancer cell lines with IC50 from 0.025 to 0.7 μM, which induces apoptosis and G2/M phase arrest. Phase 2.
Cell, 2021, 184(2):334-351.e20
Sci Adv, 2021, 7(4)eabd7851
J Pediatr Hematol Oncol, 2019, 41(6):e359-e370
S1185 Ritonavir (ABT-538) Ritonavir (ABT-538, A 84538, RTV, Norvir, Norvir Softgel) is a Cytochrome P450 3A and Protease Inhibitor; Also inhibits Cytochrome P450 2D6, P-Glycoprotein and induces Cytochrome P450 2C19, Cytochrome P450 1A2, Cytochrome P450 2C9, Cytochrome P450 2B6 and UDP Glucuronosyltransferases. Ritonavir induces apoptosis.
J Virol, 2022, JVI0173021
mBio, 2021, 12(1)e02754-20
Cell Chem Biol, 2021, S2451-9456(21)00441-4
S1186 BIBR 1532 BIBR 1532 is a potent, selective, non-competitive telomerase inhibitor with IC50 of 100 nM in a cell-free assay. No inhibition of DNA and RNA polymerases, including HIV reverse transcriptase are observed at concentrations vastly exceeding the IC50 for telomerase. BIBR 1532 induces apoptosis in cancer cells.
Med Oncol, 2021, 39(1):12
Neuro Oncol, 2020, noaa207
Oxid Med Cell Longev, 2020, 2020:6946037
S1191 Fulvestrant (ICI-182780) Fulvestrant (ICI-182780, ZD 9238, ZM 182780) is an estrogen receptor (ER) antagonist with IC50 of 0.94 nM in a cell-free assay. Fulvestrant also induces autophagy and apoptosis and has antitumor activity.
Mol Cancer Ther, 2022, 21(1):48-57
Biochim Biophys Acta Gen Subj, 2022, 1866(1):130046
Clin Cancer Res, 2021, 10.1158/1078-0432.CCR-20-2961
S1200 Decitabine (NSC 127716) Decitabine (NSC 127716, Deoxycytidine, Dacogen, 5-aza-2-deoxycytidine, 5-AZA-dC, 5-aza-CdR) is a DNA methyltransferase inhibitor, incorporating into DNA and resulting in hypomethylation of DNA and intra-S-phase arrest of DNA replication. It is used to treat myelodysplastic syndrome (MDS). Decitabine induces cell cycle arrest and apoptosis in various cancer cell lines.
Cancer Cell, 2021, S1535-6108(21)00659-0
Cell Metab, 2021, 33(1):110-127.e5
J Immunother Cancer, 2021, 9(7)e002528
S1208 Doxorubicin (Adriamycin) HCl Doxorubicin (Adriamycin, NSC 123127, DOX, Hydroxydaunorubicin) HCl is an antibiotic agent that inhibits DNA topoisomerase II and induces DNA damage, mitophagy and apoptosis in tumor cells. Doxorubicin reduces basal phosphorylation of AMPK. Doxorubicin is used in the concomitant treatment of HIV-infected patients but is found to be at high risk of HBV reactivation.
J Exp Clin Cancer Res, 2022, 41(1):11
Toxicol Appl Pharmacol, 2022, 435:115834
Oncol Rep, 2022, 47(1)18
S1209 Fluorouracil (5-Fluorouracil, 5-FU) Fluorouracil (5-Fluorouracil, 5-FU, NSC 19893) is a DNA/RNA synthesis inhibitor, which interrupts nucleotide synthetic by inhibiting thymidylate synthase (TS) in tumor cells. Fluorouracil induces apoptosis and can be used in the treatment of HIV.
Oncotarget, 2022, 13:92-104
Cell, 2021, 184(25):6119-6137.e26
Sci Adv, 2021, 7(36):eabh1684
S1218 Clofarabine Clofarabine (Clolar) inhibits the enzymatic activities of ribonucleotide reductase (RNR) (IC50 = 65 nM) and DNA polymerase. Clofarabine induces autophagy and apoptosis.
Hum Cell, 2021, 10.1007/s13577-021-00579-z
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Hum Cell, 2021, 34(6):1911-1918
S1223 Epirubicin (IMI 28) HCl Epirubicin HCl (IMI 28, NSC 256942, 4'-epidoxorubicin), a semisynthetic L-arabino derivative of doxorubicin, is an antineoplastic agent by inhibiting Topoisomerase. Epirubicin induces apoptosis.
Cancer Cell, 2021, S1535-6108(20)30609-7
Cell Rep, 2021, 34(10):108814
Biomolecules, 2021, 11(8)1128
S1225 Etoposide (VP-16) Etoposide (VP-16, VP-16213) is a semisynthetic derivative of podophyllotoxin, which inhibits DNA synthesis via topoisomerase II inhibition activity. Etoposide induces autophagy, mitophagy and apoptosis.
Nature, 2021, 10.1038/s41586-021-04204-9
Nature, 2021, 10.1038/s41586-021-04009-w
Cancer Cell, 2021, S1535-6108(21)00659-0
S1231 Topotecan (NSC609699) HCl Topotecan HCl (NSC609699, Nogitecan, SKFS 104864A) is a topoisomerase I inhibitor for MCF-7 Luc cells and DU-145 Luc cells with IC50 of 13 nM and 2 nM in cell-free assays, respectively. Topotecan HCl induces autophagy and apoptosis.
Cancer Cell, 2021, S1535-6108(21)00659-0
Cancer Res, 2021, canres.1540.2020
Cell Rep, 2021, 34(10):108814
S1233 2-Methoxyestradiol (2-MeOE2) 2-Methoxyestradiol (2-MeOE2, NSC 659853, 2-ME2) depolymerizes microtubules and blocks HIF-1α nuclear accumulation and HIF-transcriptional activity. 2-Methoxyestradiol induces both autophagy and apoptosis in various carcinogenic cell lines. Phase 2.
Cell Death Differ, 2021, 10.1038/s41418-021-00885-x
Cancers (Basel), 2021, 13(20)5232
Cell Death Discov, 2021, 7(1):242
S1237 Temozolomide (CCRG 81045) Temozolomide (CCRG81045, NSC 362856, TMZ) is a monofunctional SN-1 alkylating agent that can modify nitrogen atoms in the DNA ring and the extracyclic oxygen group, chemically converted to MTIC and degrades to methyldiazonium cation, which transfers methyl groups to DNA at physiologic pH. A DNA damage inducer in L-1210 and L-1210/BCNU cells. Temozolomide induces apoptosis and exhibits antitumor activity.
Mol Neurobiol, 2022, 10.1007/s12035-021-02674-6
Cancer Chemother Pharmacol, 2022, 10.1007/s00280-021-04380-5
Cell Res, 2021, 10.1038/s41422-021-00528-3
S1238 Tamoxifen (ICI 46474) Tamoxifen (ICI 46474, (Z)-Tamoxifen, trans-Tamoxifen) is a selective estrogen receptor modulator (SERM). Tamoxifen enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen induces apoptosis.
Clin Cancer Res, 2021, 10.1158/1078-0432.CCR-20-3905
Cancers (Basel), 2021, 13(9)2116
Cell Death Dis, 2021, 12(6):619
S1241 Vincristine (NSC-67574) sulfate Vincristine sulfate (NSC-67574, Leurocristine, Oncovin, 22-Oxovincaleukoblastine) is an inhibitor of polymerization of microtubules by binding to tubulin with IC50 of 32 μM in a cell-free assay. Vincristine sulfate induces apoptosis.
Mol Cell, 2022, 82(1):75-89.e9
Theranostics, 2021, 11(9):4281-4297
Cell Rep, 2021, 36(11):109718
S1242 CPTH2 CPTH2 is a potent histone acetyltransferase (HAT) inhibitor modulating Gcn5p network. CPTH2 induces apoptosis and decreases the invasiveness of a ccRCC cell line through the inhibition of KAT3B.
Transl Oncol, 2021, 14(11):101196
S1244 Amuvatinib (MP-470) Amuvatinib (MP-470, HPK 56) is a potent and multi-targeted inhibitor of c-Kit, PDGFRα and Flt3 with IC50 of 10 nM, 40 nM and 81 nM, respectively. Amuvatinib suppresses c-MET and c-RET. Amuvatinib is also active as a DNA repair protein Rad51 inhibitor with antineoplastic activity. Phase 2.
mBio, 2021, 12(6):e0322821
Hum Cell, 2021, 34(6):1911-1918
Hum Cell, 2021, 10.1007/s13577-021-00579-z
S1264 PD173074 PD173074 is a potent FGFR1 inhibitor with IC50 of ~25 nM and also inhibits VEGFR2 with IC50 of 100-200 nM in cell-free assays, ~1000-fold selective for FGFR1 than PDGFR and c-Src. PD173074 reduces proliferation and promotes apoptosis in gastric cancer cells.
Oncoimmunology, 2022, 11(1):2021619
Adv Sci (Weinh), 2021, 8(2):2002922
Nat Commun, 2021, 12(1):3017
S1273 Amarogentin

Amarogentin (AG), a secoiridoid glycoside mainly extracted from Swertia and Gentiana roots, exhibits anti-oxidative, anti-tumour, and anti-diabetic activities. Amarogentin is an agonist for the bitter taste receptor TAS2R1 and inhibits in LAD-2 cells substance P-induced production of newly synthesized TNF-α. Amarogentin induces apoptosis in human gastric cancer cells (SNU-16) through G2/M cell cycle arrest and PI3K/Akt signalling pathway. Amarogentin (AG) interacts with the α2 subunit of AMP-activated protein kinase (AMPK) and activates the trimeric kinase with EC50 of 277 pM.

S1288 Camptothecin (NSC-100880) Camptothecin (NSC-100880, CPT, Campathecin, (S)-(+)-Camptothecin) is a specific inhibitor of DNA topoisomerase I (Topo I) with IC50 of 0.68 μM in a cell-free assay. Camptothecin induces apoptosis in cancer cells via microRNA-125b-mediated mitochondrial pathways. Phase 2.
Nature, 2021, 10.1038/s41586-021-04204-9
Cancer Cell, 2021, S1535-6108(21)00659-0
Mol Cell, 2021, 81(20):4228-4242.e8
S1290 Celastrol (NSC 70931) Celastrol (NSC 70931, Tripterine) is a potent proteasome inhibitor for the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM. Celastrol induces apoptosis and autophagy via the ROS/JNK signaling pathway. Celastrol inhibits dopaminergic neuronal death of Parkinson's disease through activating mitophagy.
Mol Oncol, 2021, 10.1002/1878-0261.12936
Aging (Albany NY), 2021, 13(12):16816-16833
Molecules, 2021, 26(14)4124
S1299 Floxuridine (NSC 27640) Floxuridine (NSC 27640, Deoxyfluorouridine, FUDR) is a prodrug that is rapidly catabolized to 5-fluorouracil in vivo. Floxuridine is used to treat various cancers, particularly metastases to the liver. Floxuridine inhibits Poly(ADP-Ribose) polymerase and induces DNA damage and apoptosis. Floxuridine has antiviral effects against HSV and CMV.
Cell Chem Biol, 2021, S2451-9456(21)00306-8
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Hum Cell, 2021, 34(6):1911-1918
S1312 Streptozotocin (STZ) Streptozotocin (STZ, NSC-85998, Streptozocin, U 9889) is a glucosamine-nitrosourea derivative, which is a DNA-methylating, carcinogenic, antibiotic and diabetes inducing agent. Streptozotocin induces autophagy and apoptosis. Solutions are best fresh-prepared.
Hum Cell, 2021, 34(6):1911-1918
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Hum Cell, 2021, 10.1007/s13577-021-00579-z
S1314 Zoledronic acid (ZOL 446) Zoledronic acid (ZOL 446, ZA, Zoledronate, CGP-4244, GP42446A, Zometa, Zomera, Aclasta, Reclast), a potent osteoclast inhibitor, induces apoptosis in osteoclasts by inhibiting enzymes of the mevalonate pathway and preventing the isoprenylation of small GTP-binding proteins such as Ras and Rho. Zoledronic acid (ZA) also induces autophagy.
Oncol Lett, 2022, 23(2):51
Biomater Sci, 2021, 10.1039/d0bm02107e
Hum Cell, 2021, 10.1007/s13577-021-00579-z
S1362 Rigosertib (ON-01910) Rigosertib (ON-01910) is a non-ATP-competitive inhibitor of PLK1 with IC50 of 9 nM in a cell-free assay. It shows 30-fold greater selectivity against Plk2 and no activity to Plk3. Rigosertib inhibits PI3K/Akt pathway and activates oxidative stress signals. Rigosertib induces apoptosis in various cancer cells. Phase 3.
Elife, 2021, 10e70715
Immun Inflamm Dis, 2021, 10.1002/iid3.458
Mol Cell, 2020, 79(1):191-198.e3
S1378 Ruxolitinib (INCB018424) Ruxolitinib (INCB018424) is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM in cell-free assays, >130-fold selectivity for JAK1/2 versus JAK3. Ruxolitinib kills tumor cells through toxic mitophagy. Ruxolitinib induces autophagy and enhances apoptosis.
Blood, 2022, blood.2021012366
Mol Neurodegener, 2022, 17(1):7
J Exp Clin Cancer Res, 2022, 41(1):10
S1396 Resveratrol (SRT501) Resveratrol (SRT501, trans-Resveratrol) has a wide spectrum of targets including cyclooxygenases(i.e. COX, IC50=1.1 μM), lipooxygenases(LOX, IC50=2.7 μM), kinases, sirtuins and other proteins. It has anti-cancer, anti-inflammatory, blood-sugar-lowering and other beneficial cardiovascular effects. Resveratrol induces mitophagy/autophagy and autophagy-dependent apoptosis.
Int Immunopharmacol, 2022, 103:108489
Eur J Neurosci, 2022, 10.1111/ejn.15596
Adv Sci (Weinh), 2021, e2103360
S1413 Bafilomycin A1 (Baf-A1) Bafilomycin A1(Baf-A1) is a vacuolar H+-ATPase inhibitor with IC50 of 0.44 nM. Bafilomycin A1 is found to inhibit autophagy while induces apoptosis.
Adv Sci (Weinh), 2021, e2100779
Mol Cell, 2021, S1097-2765(21)00729-2
ACS Nano, 2021, 10.1021/acsnano.1c06452
S1443 Zileuton (A-64077) Zileuton (A-64077, Abbott 64077, ZYFLO) is an orally active inhibitor of 5-lipoxygenase, and thus inhibits leukotrienes (LTB4, LTC4, LTD4, and LTE4) formation, used to decrease the symptoms of asthma. Zileuton induces apoptosis while inhibits ferroptosis.
J Exp Clin Cancer Res, 2021, 40(1):344
Front Microbiol, 2020, 11:845
Front Immunol, 2019, 10:1904
S1451 Aurora A Inhibitor I (TC-S 7010) Aurora A Inhibitor I (TC-S 7010) is a novel, potent, and selective inhibitor of Aurora A with IC50 of 3.4 nM in a cell-free assay. It is 1000-fold more selective for Aurora A than Aurora B. Aurora A Inhibitor I (TC-S 7010) triggers apoptosis through the ROS-mediated UPR signaling pathway.
EMBO Rep, 2021, e52387
Cancer Lett, 2021, 509:89-104
Nat Commun, 2020, 11(1):1308
S1452 Ispinesib (SB-715992) Ispinesib (SB-715992, CK0238273) is a potent, specific and reversible inhibitor of kinesin spindle protein (KSP) with Ki app of 1.7 nM in a cell-free assay, no inhibition to CENP-E, RabK6, MCAK, MKLP1, KHC or Kif1A. Ispinesib induces mitotic arrest and apoptotic cell death. Phase 2.
Cell, 2020, 182(3):685-712.e19
Cell, 2020, 182(3):685-712.e19
Sci Transl Med, 2020, 12(562)eaba4434
S1460 SP600125 SP600125 (Nsc75890) is a broad-spectrum JNK inhibitor for JNK1, JNK2 and JNK3 with IC50 of 40 nM, 40 nM and 90 nM in cell-free assays, respectively; 10-fold greater selectivity against MKK4, 25-fold greater selectivity against MKK3, MKK6, PKB, and PKCα, and 100-fold selectivity against ERK2, p38, Chk1, EGFR etc. SP600125 is also a broad‐spectrum inhibitor of serine/threonine kinases including Aurora kinase AFLT3 and TRKA with of IC50 of 60 nM, 90 nM and 70 nM. SP600125 inhibits autophagy and activates apoptosis.
Cells, 2022, 11(1)134
Int J Biol Sci, 2022, 18(1):349-359
Biomed Pharmacother, 2022, 145:112437
S1487 PHA-793887 PHA-793887 is a novel and potent inhibitor of CDK2, CDK5 and CDK7 with IC50 of 8 nM, 5 nM and 10 nM. It is greater than 6-fold more selective for CDK2, 5, and 7 than CDK1, 4, and 9. PHA-793887 induces cell-cycle arrest and apoptosis. Phase 1.
Cell, 2020, 182(3):685-712.e19
Cell, 2020, 182(3):685-712.e19
Mol Cell Biol, 2020, 40(4)
S1491 Fludarabine (NSC 118218) Fludarabine (NSC 118218, FaraA, Fludarabinum) is a STAT1 activation inhibitor which causes a specific depletion of STAT1 protein (and mRNA) but not of other STATs. Also a DNA synthesis inhibitor in vascular smooth muscle cells. Fludarabine induces apoptosis.
Int J Biol Sci, 2022, 18(1):331-348
Cell Metab, 2021, 33(1):110-127.e5
Cell Rep, 2021, 34(1):108584
S1497 Pralatrexate (NSC 754230) Pralatrexate (NSC 754230) is an antifolate, and structurally a folate analog. Its IC50 is < 300 nM in some cell lines. Pralatrexate induces tumor cell apoptosis.
J Clin Endocrinol Metab, 2021, dgab424
Biomol Ther (Seoul), 2021, 29(3):268-272
Hum Cell, 2021, 34(6):1911-1918
S1501 Mycophenolate mofetil (RS-61443) Mycophenolate Mofetil (RS 61443, Mycophenolic acid morpholinoethyl ester, CellCept, TM-MMF) is a non-competitive, selective and reversible inhibitor of inosine monophosphate dehydrogenase I/II with IC50 of 39 nM and 27 nM, respectively. Mycophenolate Mofetil induces caspase-dependent apoptosis and cell cycle inhibition in multiple myeloma cells.
Clin Exp Rheumatol, 2021, N/A
Nat Commun, 2020, 11(1):3811
bioRxiv, 2020, 2020/9/20.4.7.30734
S1515 Pracinostat (SB939) Pracinostat (SB939) is a potent pan-HDAC inhibitor with IC50 of 40-140 nM with exception for HDAC6. It has no activity against the class III isoenzyme SIRT I. Pracinostat (SB939) induces apoptosis in tumor cells. Phase 2.
Cancer Lett, 2021, 521:268-280
Front Immunol, 2021, 12:771453
Cell, 2020, S0092-8674(20)31394-5
S1524 AT7519 AT7519 is a multi-CDK inhibitor for CDK1, 2, 4, 6 and 9 with IC50 of 10-210 nM. It is less potent to CDK3 and little active to CDK7. AT7519 also inhibits GSK3β with IC50 of 89 nM. AT7519 induces apoptosis. Phase 2.
J Am Chem Soc, 2021, 10.1021/jacs.1c05386
Sci Rep, 2021, 11(1):17029
Fundam Clin Pharmacol, 2021, 10.1111/fcp.12709
S1526 Quizartinib (AC220) Quizartinib (AC220) is a second-generation FLT3 inhibitor for Flt3(ITD/WT) with IC50 of 1.1 nM/4.2 nM in MV4-11 and RS4;11 cells, respectively, 10-fold more selective for Flt3 than KIT, PDGFRα, PDGFRβ, RET, and CSF-1R. Quizartinib (AC220) induces apoptosis of tumor cells. Phase 3.
Oncol Lett, 2022, 23(2):51
Mol Cell, 2021, S1097-2765(21)00507-4
Clin Cancer Res, 2021, 10.1158/1078-0432.CCR-20-3458
S1533 R406 (free base) R406 (free base) is a potent Syk inhibitor with IC50 of 41 nM in a cell-free assay, strongly inhibits Syk but not Lyn, 5-fold less potent to Flt3. R406 (free base) triggers apoptosis. Phase 1.
Free Radic Biol Med, 2022, S0891-5849(22)00004-1
Nat Genet, 2021, 53(4):500-510
Sci Transl Med, 2021, 13(596)eabf8654
S1555 AZD8055 AZD8055 is a novel ATP-competitive mTOR inhibitor with IC50 of 0.8 nM in MDA-MB-468 cells with excellent selectivity (∼1,000-fold) against PI3K isoforms and ATM/DNA-PK. AZD8055 induces caspase-dependent apoptosis and also induces autophagy. Phase 1.
Immunity, 2022, 55(1):159-173.e9
Nature, 2021, 591(7849):288-292
Immunity, 2021, S1074-7613(21)00069-8
S1567 Pomalidomide (CC-4047) Pomalidomide (CC-4047) inhibits LPS-induced TNF-α release with IC50 of 13 nM in PBMCs. Pomalidomide can be utilized in PROTAC as a ligand for targeting E3 ligase and inhibiting the E3 ligase protein cereblon (CRBN). Pomalidomide promotes apoptosis and cell cycle arrest.
Nat Cell Biol, 2021, 10.1038/s41556-021-00766-y
Mol Cell, 2021, 81(6):1170-1186.e10
Sci Adv, 2021, 7(6)eabd6263
S1576 Sulfasalazine (NSC 667219) Sulfasalazine (NSC 667219, Azulfidine, Salazopyrin, Sulphasalazine) is a sulfa derivative of mesalazine, used as an anti-inflammatory agent to treat bowel disease and rheumatoid arthritis. Sulfasalazine is a potent and specific inhibitor of nuclear factor kappa B (NF-κB), TGF-β and COX-2. Sulfasalazine induces ferroptosis, apoptosis and autophagy.
Cell Metab, 2021, S1550-4131(21)00233-3
Sci Adv, 2021, 7(35)eabj0364
Sci Adv, 2021, 7(27)eabh3032
S1623 Acetylcysteine (N-acetylcysteine) Acetylcysteine (N-acetyl-l-cysteine, NAC) is a ROS(reactive oxygen species) inhibitor that antagonizes the activity of proteasome inhibitors. It is also a tumor necrosis factor production inhibitor. Acetylcysteine(N-acetyl-l-cysteine) suppresses TNF-induced NF-κB activation through inhibition of IκB kinases. Acetylcysteine(N-acetyl-l-cysteine) induces apoptosis via the mitochondria-dependent pathway. Acetylcysteine(N-acetyl-l-cysteine) inhibits ferroptosis and virus replication.Solutions of Acetylcysteine are best fresh-prepared.
J Clin Invest, 2021, e152067
EMBO Mol Med, 2021, 13(9):e13193
Elife, 2021, 10e69795
S1629 Orlistat (Ro 18-0647) Orlistat (Ro 18-0647, Tetrahydrolipstatin) is a general lipase inhibitor with IC50 of 122 ng/ml for PL from human duodenal juice. Orlistat treatment reduces proliferation, induces apoptosis and arrests cell cycle.
Nat Commun, 2021, 12(1):3830
Cell Rep, 2021, 36(12):109742
Sci Rep, 2021, 11(1):22085
S1648 Cytarabine (U-19920A) Cytarabine (U-19920A, Cytarabin, Ara-C, Arabinofuranosyl Cytidine, Cytosine β-D-arabinofuranoside, Cytosine arabinoside, NSC 63878, NSC 287459) is an antimetabolic agent and DNA synthesis inhibitor with IC50 of 16 nM in wild-type CCRF-CEM cells. Cytarabine induces autophagy and apoptosis.
Leukemia, 2021, 10.1038/s41375-021-01361-8
Blood Cancer J, 2021, 11(6):111
Cell Rep, 2021, 36(7):109559
S1680 Disulfiram (NSC 190940) Disulfiram (NSC 190940, Tetraethylthiuram disulfide, TETD) is a specific inhibitor of aldehyde-dehydrogenase (ALDH) with IC50 of 0.15 μM and 1.45 μM for hALDH1 and hALDH2, respectively. Disulfiram is used for the treatment of chronic alcoholism by producing an acute sensitivity to alcohol. Disulfiram induces apoptosis. Disulfiram is also an inhibitor of pore formation by gasdermin D (GSDMD).
mBio, 2022, 10.1128/mbio.02739-21
Int Immunopharmacol, 2022, 102:108401
Cancer Res, 2021, canres.1337.2021
S1692 Busulfan (NSC-750) Busulfan (NSC-750) is a cell cycle non-specific alkylating antineoplastic agent. Busulfan induces apoptosis.
Breast Cancer Res, 2021, 23(1):100
Hum Cell, 2021, 34(6):1911-1918
Hum Cell, 2021, 10.1007/s13577-021-00579-z
S1714 Gemcitabine (LY-188011) Gemcitabine (LY-188011, NSC 613327), a nucleic acid synthesis inhibitor, is a very potent and specific deoxycytidine analogue, used as chemotherapy. Gemcitabine induces a potent p53-dependent apoptosis.
Nat Commun, 2021, 12(1):1602
Cancer Res, 2021, canres.1337.2021
Cell Rep, 2021, 34(10):108814
S1759 Pitavastatin (NK-104) calcium Pitavastatin Calcium (NK-104, P-872441, itavastatin, nisvastatin), a novel member of the medication class of statins, is a calcium salt formulation of pitavastatin which is a highly effective HMG-CoA reductase inhibitor. Pitavastatin Calcium attenuates AGEs-induced mitophagy via inhibition of ROS generation. Pitavastatin Calcium induces autophagy and apoptosis.
Nat Biotechnol, 2021, 10.1038/s41587-021-00860-4
Cancer Discov, 2021, candisc.0551.2021
Transl Oncol, 2021, 14(7):101107
S1786 Verteporfin (CL 318952) Verteporfin (CL 318952, Visudyne) is a small molecule that inhibits TEAD–YAP association and YAP-induced liver overgrowth. It is also a potent second-generation photosensitizing agent derived from porphyrin. Verteporfin is an autophagy inhibitor. Verteporfin inhibits cell proliferation and induces apoptosis.
Nat Commun, 2022, 13(1):50
Hum Mol Genet, 2022, ddab374
Exp Cell Res, 2022, 411(1):113000
S1792 Simvastatin (MK 733) Simvastatin (MK-0733, MK 733) is a competitive inhibitor of HMG-CoA reductase with Ki of 0.1-0.2 nM in cell-free assays. Simvastatin induces ferroptosis, mitophagy, autophagy and apoptosis.
Nat Biotechnol, 2021, 10.1038/s41587-021-00860-4
Theranostics, 2021, 11(4):1609-1625
Theranostics, 2021, 11(13):6560-6572
S1807 Aciclovir (BW 248U) Acyclovir (BW 248U, Acyclovir, Acycloguanosine, Zovirax, ACV, NSC 645011) is a synthetic nucleoside analogue active against herpesviruses. Acyclovir induces cell cycle perturbation and apoptosis in Jurkat leukemia cells.
Microbiol Spectr, 2021, 9(3):e0064621
Front Microbiol, 2021, 12:722748
Vet Microbiol, 2021, 265:109313
S1848 Curcumin Curcumin (Diferuloylmethane, Natural Yellow 3, Turmeric yellow) is the principal curcuminoid of the popular Indian spice turmeric, which is a member of the ginger family (Zingiberaceae). It is an inhibitor of p300 histone acetylatransferase(IC50~25 μM)and Histone deacetylase (HDAC); activates Nrf2 pathway and supresses the activation of NF-κB. Curcumin induces mitophagy, autophagy, apoptosis, and cell cycle arrest with antitumor activity. Curcumin reduces renal damage associated with rhabdomyolysis by decreasing ferroptosis-mediated cell death. Curcumin exhibits anti-infective properties against various human pathogens like the influenza virus, hepatitis C virus, HIV and so on.
Adv Sci (Weinh), 2021, e2103360
Front Immunol, 2021, 12:656242
Aging (Albany NY), 2021, 13(10):13968-14000
S1896 Hydroxyurea (NSC-32065) Hydroxyurea (NSC-32065, NCI-C04831, Hydroxycarbamide) is an antineoplastic agent that inhibits DNA synthesis through the inhibition of ribonucleoside diphosphate reductase. Hydroxyurea activates apoptosis and autophagy. Hydroxyurea is used to treat HIV infection.
Cancer Res, 2022, canres.1707.2021
Nat Commun, 2021, 12(1):5572
Cancer Res, 2021, canres.3761.2020
S1972 Tamoxifen (ICI 46474) Citrate Tamoxifen Citrate (ICI 46474) is a selective estrogen receptor modulator (SERM). Tamoxifen Citrate is also a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen induces apoptosis and autophagy.
Clin Cancer Res, 2021, 10.1158/1078-0432.CCR-20-3905
Cancers (Basel), 2021, 13(9)2116
Cell Death Dis, 2021, 12(6):619
S1999 Sodium butyrate Sodium butyrate (NaB, Butanoic acid sodium salt), sodium salt of butyric acid, is a histone deacetylase inhibitor and competitively binds to the zinc sites of class I and II histone deacetylases (HDACs). Sodium butyrate (NaB) inhibits cell cycle progression, promotes differentiation, and induces apoptosis and autophagy in several types of cancer cells.
Cell Mol Life Sci, 2021, 10.1007/s00018-021-03883-x
Front Cell Dev Biol, 2021, 9:662868
Int J Mol Sci, 2020, 21(2)
S2012 PCI-34051 PCI-34051 is a potent and specific HDAC8 inhibitor with IC50 of 10 nM in a cell-free assay. It has greater than 200-fold selectivity over HDAC1 and 6, more than 1000-fold selectivity over HDAC2, 3, and 10. PCI-34051 induces caspase-dependent apoptosis.
Cell Rep, 2021, 37(12):110129
Thyroid, 2021, 10.1089/thy.2020.0948
Tuberculosis (Edinb), 2021, 127:102062
S2013 PF-573228 PF-573228 is an ATP-competitive inhibitor of FAK with IC50 of 4 nM in a cell-free assay, ~50- to 250-fold selective for FAK than Pyk2, CDK1/7 and GSK-3β. PF-573228 induces apoptosis.
Proc Natl Acad Sci U S A, 2021, 118(40)e2105367118
Cell Rep, 2021, 35(7):109159
FASEB J, 2021, 35(5):e21598
S2077 Atorvastatin Calcium Atorvastatin Calcium is an inhibitor of HMG-CoA reductase used as a cholesterol-lowering medication that blocks the production of cholesterol. Atorvastatin Calcium induces apoptosis and autophagy.
Nat Biotechnol, 2021, 10.1038/s41587-021-00860-4
Oncol Lett, 2021, 21(2):82
Neurobiol Dis, 2021, 152:105294
S2161 RAF265 (CHIR-265) RAF265 (CHIR-265) is a potent selective inhibitor of C-Raf/B-Raf/B-Raf V600E with IC50 of 3-60 nM, and exhibits potent inhibition on VEGFR2 phosphorylation with EC50 of 30 nM in cell-free assays. RAF265 (CHIR-265) induces cell cycle arrest and apoptosis. Phase 2.
Drug Chem Toxicol, 2022, 1-10
J Clin Invest, 2021, e147849
J Clin Invest, 2021, e147849
S2194 R406 R406 is a potent Syk inhibitor with IC50 of 41 nM in cell-free assays, strongly inhibits Syk but not Lyn, 5-fold less potent to Flt3. R406 induces apoptosis. Phase 1.
Free Radic Biol Med, 2022, S0891-5849(22)00004-1
Cancer Cell, 2021, S1535-6108(21)00492-X
Sci Transl Med, 2021, 13(596)eabf8654
S2198 SGI-1776 free base SGI-1776 free base is a novel ATP competitive inhibitor of Pim1 with IC50 of 7 nM in a cell-free assay, 50- and 10-fold selective versus Pim2 and Pim3, also potent to Flt3 and haspin. SGI-1776 induces apoptosis and autophagy. Phase 1.
Cancer Res, 2021, canres.1023.2021
Commun Biol, 2021, 4(1):1221
Cell, 2020, 182(3):685-712.e19
S2214 AZ 960 AZ 960 is a novel ATP competitive JAK2 inhibitor with IC50 and Ki of <3 nM and 0.45 nM, 3-fold selectivity of AZ960 for JAK2 over JAK3. AZ 960 induces apoptosis and growth arrest.
BMC Cancer, 2021, 21(1):1213
Carcinogenesis, 2020, 41(7):993-1004
Nat Commun, 2019, 10(1):716
S2215 DAPT (GSI-IX) DAPT (GSI-IX, LY-374973) is a novel γ-secretase inhibitor, which inhibits Aβ production with IC50 of 20 nM in HEK 293 cells. DAPT enhances the apoptosis of human tongue carcinoma cells and regulates autophagy.
Adv Mater, 2022, e2106829
Hepatology, 2022, 10.1002/hep.32332
Sci Rep, 2022, 12(1):7
S2218 Torkinib (PP242) Torkinib (PP242) is a selective mTOR inhibitor with IC50 of 8 nM in cell-free assays; targets both mTOR complexes with >10- and 100-fold selectivity for mTOR than PI3Kδ or PI3Kα/β/γ, respectively. Torkinib (PP242) induces mitophagy and apoptosis.
Immunity, 2022, 55(1):159-173.e9
Methods Mol Biol, 2022, 2445:139-169
Immunity, 2021, 54(10):2354-2371.e8
S2219 Momelotinib (CYT387) Momelotinib (CYT387, LM-1149 , CYT11387) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, ~10-fold selectivity versus JAK3. Momelotinib (CYT387) induces apoptosis and autophagy. Phase 3.
Cell Stem Cell, 2021, S1934-5909(21)00344-1
Cancer Res, 2021, canres.0955.2021
J Transl Med, 2021, 19(1):396
S2235 Volasertib (BI 6727) Volasertib (BI 6727) is a highly potent Plk1 inhibitor with IC50 of 0.87 nM in a cell-free assay. It shows 6- and 65-fold greater selectivity against Plk2 and Plk3. Volasertib induces cell cycle arrest and apoptosis in various cancer cells. Phase 3.
Science, 2021, 371(6535)eabc5386
Mol Cell, 2021, S1097-2765(20)30946-1
Nat Commun, 2021, 12(1):5356
S2243 Degrasyn (WP1130) Degrasyn (WP1130) is a selective deubiquitinase (DUB: USP5, UCH-L1, USP9x, USP14, and UCH37) inhibitor and also suppresses Bcr/Abl, also a JAK2 transducer (without affecting 20S proteasome) and activator of transcription (STAT). Degrasyn (WP1130) induces apoptosis and blocks autophagy.
Br J Cancer, 2021, 10.1038/s41416-021-01421-x
Cell Chem Biol, 2021, S2451-9456(21)00213-0
Transl Lung Cancer Res, 2021, 10(10):3995-4011
S2247 Buparlisib (BKM120) Buparlisib (BKM120, NVP-BKM120) is a selective PI3K inhibitor of p110α/β/δ/γ with IC50 of 52 nM/166 nM/116 nM/262 nM in cell-free assays, respectively. Reduced potency against VPS34, mTOR, DNAPK, with little activity to PI4Kβ. Buparlisib induces apoptosis. Phase 2.
Cancer Cell, 2021, S1535-6108(21)00284-1
Adv Sci (Weinh), 2021, e2103360
Mol Cell, 2021, S1097-2765(21)00232-X
S2248 Silmitasertib (CX-4945) Silmitasertib (CX-4945) is a potent and selective inhibitor of CK2 (casein kinase 2) with IC50 of 1 nM in a cell-free assay, less potent to Flt3, Pim1 and CDK1 (inactive in cell-based assay). Silmitasertib induces autophagy and promotes apoptosis. Phase 1/2.
Cell Mol Gastroenterol Hepatol, 2022, S2352-345X(22)00003-0
Sci Rep, 2022, 12(1):7
Genes Dev, 2021, 35(15-16):1123-1141
S2271 Berberine chloride (NSC 646666) Berberine chloride (NSC 646666, Natural Yellow 18) is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.
Front Pharmacol, 2021, 12:632201
Molecules, 2021, 26(5)1210
Biology (Basel), 2021, 10(3)250
S2285 Cryptotanshinone Cryptotanshinone is a STAT3 inhibitor with IC50 of 4.6 μM in a cell-free assay, strongly inhibits phosphorylation of STAT3 Tyr705, with a small effect on STAT3 Ser727, but none against STAT1 nor STAT5. Cryptotanshinone induces ROS-dependent autophagy and mitochondria-mediated apoptosis.
Front Immunol, 2021, 12:712781
Int J Biol Sci, 2021, 17(10):2417-2429
J Cell Mol Med, 2021, 10.1111/jcmm.16250
S2290 Dihydroartemisinin (DHA) Dihydroartemisinin (DHA, Dihydroqinghaosu, β-Dihydroartemisinin, Artenimol) is a semi-synthetic derivative of artemisinin and isolated from the traditional Chinese herb Artemisia annua. Dihydroartemisinin induces autophagy and apoptosis by suppressing NF-κB activation.
Nat Immunol, 2021, 10.1038/s41590-021-00967-5
ACS Infect Dis, 2021, 10.1021/acsinfecdis.0c00580
Mol Med Rep, 2021, 23(1)40
S2310 Honokiol (NSC 293100) Honokiol (NSC 293100) is the active principle of magnolia extract that inhibits Akt-phosphorylation and promotes ERK1/2 phosphorylation. Honokiol causes G0/G1 phase arrest, induces apoptosis, and autophagy via the ROS/ERK1/2 signaling pathway. Honokiol inhibits hepatitis C virus (HCV) infection. Phase 3.
Cell Death Dis, 2021, 12(9):847
Front Cell Dev Biol, 2021, 9:619475
Carcinogenesis, 2021, bgab126
S2348 Rotenone (Barbasco) Rotenone (Barbasco, Dactinol, Paraderil, Rotenon, Rotocide) is a botanical insecticide that is an inhibitor of mitochondrial electron transport. Rotenone inhibits NADH/DB oxidoreductase and NADH oxidase with IC50 of 28.8 nM and 5.1 nM, respectively. Rotenone induces apoptosis through enhancing mitochondrial reactive oxygen species production.
Nature, 2021, 10.1038/s41586-021-04049-2
Sci Adv, 2021, 7(49):eabk0490
Sci Adv, 2021, 7(49):eabk0490
S2391 Quercetin (NSC 9221) Quercetin (NSC 9221, Sophoretin, C.I. 75720), a natural flavonoid present in vegetables, fruit and wine, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor with IC50 of 2.4-5.4 μM. Quercetin induces mitophagy, apoptosis and protective autophagy. Phase 4.
ACS Appl Mater Interfaces, 2022, 10.1021/acsami.1c22138
Nucleic Acids Res, 2021, gkab538
Redox Biol, 2021, 44:102010
S2485 Mitoxantrone (NSC-301739) 2HCl Mitoxantrone 2HCl (NSC-301739) is a dihydrochloride salt of Mitoxantrone. Mitoxantrone is an inhibitor of type II topoisomerase and protein kinase C (PKC) with IC50 of 8.5 μM for PKC. Mitoxantrone inhibits cell proliferative growth of MCF-7/wt cells with IC50 of 0.42 μM. Mitoxantrone also induces apoptosis.
Cancers (Basel), 2021, 13(8)1954
Cell Chem Biol, 2021, S2451-9456(21)00213-0
Pharmacol Res, 2021, 174:105927
S2606 Mifepristone (RU486) Mifepristone (RU486, C-1073, RU 38486, Mifegyne) is a remarkably active antagonist of progesterone receptor and glucocorticoid receptor with IC50 of 0.2 nM and 2.6 nM, respectively. Mifepristone promotes cell autophagy and apoptosis, decreases Bcl-2 level and increases Beclin1 level, accompanied by weakened interaction between Bcl-2 and Beclin1.
Nat Commun, 2021, 12(1):7041
Exp Eye Res, 2021, S0014-4835(21)00331-6
Oncol Rep, 2021, 46(3)202
S2619 MG-132 MG132 (Z-Leu-Leu-Leu-al) is a potent cell-permeable proteasome and calpain inhibitor with IC50s of 0.1 μM and 1.2 μM for the inhibition of proteasome and calpain, respectively. MG132 activates autophagy and induces apoptosis in tumor cells.
Sci Adv, 2022, 8(2):eabk1789
Nat Commun, 2022, 13(1):12
Nat Commun, 2022, 13(1):165
S2626 Rabusertib (LY2603618) Rabusertib (LY2603618, IC-83) is a highly selective Chk1 inhibitor with potential anti-tumor activity in a cell-free assay. IC50=7 nM, showing approximately 100-fold more potent against Chk1 than against any of the other protein kinases evaluated. Rabusertib (LY2603618) induces cell cycle arrest, DNA damage response and autophagy in cancer cells. Rabusertib (LY2603618) induces bak-dependent apoptosis in AML cell lines.
Nat Genet, 2021, 10.1038/s41588-021-00893-0
Cancer Cell, 2021, S1535-6108(21)00383-4
Nucleic Acids Res, 2021, gkab643
S2635 CCT128930 CCT128930 is a potent, ATP-competitive and selective inhibitor of Akt2 with IC50 of 6 nM in a cell-free assay, 28-fold greater selectivity for Akt2 than the closely related PKA kinase. CCT128930 induces cell cycle arrest, DNA damage, and autophagy independent of Akt inhibition. High dose of CCT128930 triggers cell apoptosis in HepG2 cells.
ACS Nano, 2021, 10.1021/acsnano.1c06452
Front Pharmacol, 2020, 11:593832
Biomed Pharmacother, 2020, 130:110544
S2662 ICG-001 ICG-001 antagonizes Wnt/β-catenin/TCF-mediated transcription and specifically binds to CREB-binding protein (CBP) with IC50 of 3 μM, but is not the related transcriptional coactivator p300. ICG-001 induces apoptosis.
Sci Rep, 2022, 12(1):7
Nat Cell Biol, 2021, 23(3):257-267
Gastroenterology, 2021, S0016-5085(21)03489-2
S2673 Trametinib (GSK1120212) Trametinib (GSK1120212, JTP-74057, Mekinist) is a highly specific and potent MEK1/2 inhibitor with IC50 of 0.92 nM/1.8 nM in cell-free assays, no inhibition of the kinase activities of c-Raf, B-Raf, ERK1/2. Trametinib activates autophagy and induces apoptosis.
Cell Death Dis, 2022, 13(1):54
Cancer Discov, 2022, 12(1):47-61
Cold Spring Harb Mol Case Stud, 2022, 8(1)a006140
S2696 Apitolisib (GDC-0980) Apitolisib (GDC-0980, RG7422, GNE 390) is a potent, class I PI3K inhibitor for PI3Kα/β/δ/γ with IC50 of 5 nM/27 nM/7 nM/14 nM in cell-free assays, respectively. Also a mTOR inhibitor with Ki of 17 nM in a cell-free assay, and highly selective versus other PIKK family kinases. Apitolisib activates autophagy and apoptosis simultaneously in pancreatic cancer cells. Phase 2.
Adv Sci (Weinh), 2021, e2103360
Cancers (Basel), 2021, 13(9)2139
Commun Biol, 2021, 4(1):1333
S2704 LY2109761 LY2109761 is a novel selective TGF-β receptor type I/II (TβRI/II) dual inhibitor with Ki of 38 nM and 300 nM in a cell-free assay, respectively; shown to negatively affect the phosphorylation of Smad2. LY2109761 blocks autophagy and induces apoptosis.
Nat Commun, 2021, 12(1):2102
Nucleic Acids Res, 2021, 49(22):12855-12869
Cell Rep, 2021, 34(12):108882
S2714 LY411575 LY411575 is a potent γ-secretase inhibitor with IC50 of 0.078 nM/0.082 nM (membrane/cell-based), also inhibits Notch cleavage with IC50 of 0.39 nM in APP or NΔE expressing HEK293 cells. LY411575 induces apoptosis.
Sci Rep, 2022, 12(1):7
Inflammation, 2022, 10.1007/s10753-021-01591-z
Nat Commun, 2021, 12(1):6839
S2727 Dacomitinib (PF-00299804) Dacomitinib (PF299804, PF299) is a potent, irreversible pan-ErbB inhibitor, mostly to EGFR with IC50 of 6 nM in a cell-free assay. Dacomitinib inhibits ERBB2 and ERBB4 with IC50 of 45.7 nM and 73.7 nM, respectively. Dacomitinib is effective against NSCLCs with EGFR or ERBB2 mutations (resistant to gefitinib) as well as those harboring the EGFR T790M mutation. Dacomitinib inhibits cell growth and induces apoptosis. Phase 2.
Cancer Med, 2022, 10.1002/cam4.4504
Int J Mol Sci, 2021, 23(1)81
Lung Cancer, 2021, 162:79-85
S2729 SB415286 SB415286 is a potent GSK3α inhibitor with IC50/Ki of 78 nM/31 nM with equally effective inhibition of GSK-3β. SB415286 causes MM cell growth arrest and apoptosis.
Sci Rep, 2022, 12(1):7
Int J Biol Macromol, 2021, 180:97-111
Toxicol Lett, 2021, 341:68-79
S2736 Fedratinib (TG101348) Fedratinib (SAR302503, TG101348) is a selective inhibitor of JAK2 with IC50 of 3 nM in cell-free assays, 35- and 334-fold more selective for JAK2 versus JAK1 and JAK3. Fedratinib also inhibits FMS-like tyrosine kinase 3 (FLT3) and RET (c-RET) with IC50 of 15 nM and 48 nM, respectively. Fedratinib has potential antineoplastic activity. Fedratinib inhibits proliferation and induces apoptosis. Phase 2.
Sci Rep, 2022, 12(1):7
Cell, 2021, 184(2):334-351.e20
Mol Cell, 2021, S1097-2765(21)01068-6
S2741 Niraparib (MK-4827) Niraparib (MK-4827) is a selective inhibitor of PARP1/2 with IC50 of 3.8 nM/2.1 nM, with great activity in cancer cells with mutant BRCA-1 and BRCA-2. It is >330-fold selective against PARP3, V-PARP and Tank1. Niraparib can form PARP–DNA complexes resulting in DNA damage, apoptosis, and cell death. Phase 3.
Sci Transl Med, 2021, 13(592)eabc7211
Sci Adv, 2021, 7(21)eabf0197
Cell Rep, 2021, 36(4):109429
S2743 PF-04691502 PF-04691502 (PF4691502) is an ATP-competitive PI3K(α/β/δ/γ)/mTOR dual inhibitor with Ki of 1.8 nM/2.1 nM/1.6 nM/1.9 nM and 16 nM in cell-free assays, little activity against either Vps34, AKT, PDK1, p70S6K, MEK, ERK, p38, or JNK. PF-04691502 induces apoptosis. Phase 2.
Cells, 2021, 10(5)1261
J Cell Physiol, 2021, 10.1002/jcp.30657
Front Pharmacol, 2021, 12:749242
S2746 AZ 628 AZ628 is a new pan-Raf inhibitor for BRAF, BRAFV600E, and c-Raf-1 with IC50 of 105 nM, 34 nM and 29 nM in cell-free assays, also inhibits VEGFR2, DDR2, Lyn, Flt1, FMS, etc. AZ628 induces apoptosis.
Drug Chem Toxicol, 2022, 1-10
Cell Rep, 2021, 35(11):109233
Cell Death Discov, 2021, 7(1):359
S2753 Tivantinib (ARQ 197) Tivantinib (ARQ 197) is the first non-ATP-competitive c-Met inhibitor with Ki of 0.355 μM in a cell-free assay, little activity to Ron, and no inhibition to EGFR, InsR, PDGFRα or FGFR1/4. Tivantinib (ARQ 197) induces a G2/M arrest and apoptosis. Phase 3.
Signal Transduct Target Ther, 2021, 6(1):401
J Cell Mol Med, 2021, 10.1111/jcmm.16953
Eur J Pharmacol, 2021, 906:174214
S2759 Fimepinostat (CUDC-907) CUDC-907 is a dual PI3K and HDAC inhibitor for PI3Kα and HDAC1/2/3/10 with IC50 of 19 nM and 1.7 nM/5 nM/1.8 nM/2.8 nM, respectively. CUDC-907 induces cell cycle arrest and apoptosis in breast cancer cells. Phase 1.
Blood Cancer J, 2021, 11(6):111
Cancer Chemother Pharmacol, 2021, 10.1007/s00280-020-04210-0
Exp Hematol Oncol, 2021, 10(1):19
S2775 Nocodazole (R17934) Nocodazole (R17934, Oncodazole, NSC238159) is a rapidly-reversible inhibitor of microtubule polymerization, also inhibits Abl, Abl(E255K) and Abl(T315I) with IC50 of 0.21 μM, 0.53 μM and 0.64 μM in cell-free assays, respectively. Nocodazole induces apoptosis.
Mol Cancer Res, 2022, molcanres.0612.2021
Cancer Cell, 2021, S1535-6108(21)00383-4
Nat Immunol, 2021, 10.1038/s41590-021-01090-1
S2776 Devimistat (CPI-613) Devimistat (CPI-613), a lipoate analog, inhibits mitochondrial enzymes pyruvate dehydrogenase (PDH) and α-ketoglutarate dehydrogenase in NCI-H460 cell line, disrupts tumor cell mitochondrial metabolism. CPI-613 induces apoptosis in pancreatic cancer cells. Phase 2.
J Exp Clin Cancer Res, 2021, 40(1):393
Front Immunol, 2021, 12:696101
Elife, 2020, 9e56749
S2783 Vistusertib (AZD2014) Vistusertib (AZD2014) is a novel mTOR inhibitor with IC50 of 2.8 nM in a cell-free assay; highly selective against multiple PI3K isoforms (α/β/γ/δ). AZD2014 showed no or weak binding to the majority of kinases when tested at 1 μM. AZD2014 induces proliferation suppression, apoptosis, cell cycle arrest, and autophagy in HCC cells with antitumor activity.
Adv Sci (Weinh), 2021, e2103360
Nat Commun, 2021, 12(1):1876
Cell Rep, 2021, 35(1):108940
S2788 Capmatinib (INCB28060) Capmatinib (INCB28060, INC280, NVP-INC280) is a novel, ATP-competitive inhibitor of c-MET with IC50 of 0.13 nM in a cell-free assay, inactive against RONβ, as well as EGFR and HER-3. Capmatinib (INCB28060) inhibits Wnt/β-catenin and EMT signaling pathways and induces apoptosis in diffuse gastric cancer positive for c-MET amplification. Phase 1.
Oncogene, 2022, 10.1038/s41388-021-02136-2
Cancer Cell, 2021, S1535-6108(21)00492-X
Clin Cancer Res, 2021, 27(20):5697-5707
S2789 Tofacitinib (CP-690550) Tofacitinib (CP-690550,Tasocitinib) is a novel inhibitor of JAK3 with IC50 of 1 nM in cell-free assays, 20- to 100-fold less potent against JAK2 and JAK1. Tofacitinib inhibits the expression of antiapoptotic BCL-A1 and BCL-XL in human plasmacytoid dendritic cells (PDC) and induced PDC apoptosis.
Blood, 2022, blood.2021012366
Nat Commun, 2021, 12(1):5183
Clin Cancer Res, 2021, clincanres.1978.2021
S2796 WP1066 WP1066 is a novel inhibitor of JAK2 and STAT3 with IC50 of 2.30 μM and 2.43 μM in HEL cells; shows activity to JAK2, STAT3, STAT5, and ERK1/2 not JAK1 and JAK3. WP1066 induces apoptosis. Phase 1.
Cell Death Differ, 2021, 10.1038/s41418-021-00880-2
J Cell Physiol, 2021, 10.1002/jcp.30373
Front Oncol, 2021, 11:705547
S2812 (R)-(-)-Gossypol acetic acid (R)-(-)-Gossypol (AT-101) acetic acid, the R-(-) enantiomer of Gossypol acetic acid, binds with Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.32 μM, 0.48 μM and 0.18 μM in cell-free assays; does not inhibit BIR3 domain and BID. AT-101 simultaneously triggers apoptosis and a cytoprotective type of autophagy. Phase 2.
Eur J Pharm Sci, 2020, 142:105105
Platelets, 2020, 10.1080/09537104.2020.1724276
Cancers (Basel), 2020, 12(8):E2298
S2817 Torin 2 Torin 2 is a potent and selective mTOR inhibitor with IC50 of 0.25 nM in p53−/− MEFs cell line; 800-fold greater selectivity for mTOR than PI3K and improved pharmacokinetic properties. Inhibition of ATM/ATR/DNA-PK with EC50 of 28 nM/35 nM/118 nM,in PC3 cell lines respectively. Torin 2 decreases cell viability and induces autophagy and apoptosis.
Nat Commun, 2021, 12(1):245
Cell Rep, 2021, 35(1):108940
Cell Death Dis, 2021, 12(11):1028
S2820 TAE226 (NVP-TAE226) TAE226 (NVP-TAE226) is a potent FAK inhibitor with IC50 of 5.5 nM and modestly potent to Pyk2, ~10- to 100-fold less potent against InsR, IGF-1R, ALK, and c-Met. TAE226 (NVP-TAE226) induces apoptosis.
Cancer Cell, 2021, S1535-6108(21)00492-X
Nat Commun, 2021, 12(1):3519
mBio, 2021, 12(4):e0149421
S2824 TPCA-1 TPCA-1 (GW683965) is an inhibitor of IKK-2 with IC50 of 17.9 nM in a cell-free assay, inhibits NF-κB pathway, exhibits 22-fold selectivity over IKK-1. TPCA-1 is also an inhibitor of STAT3 and enhances apoptosis.
Proc Natl Acad Sci U S A, 2022, 119(3)e2114134119
Cell Rep, 2021, 35(6):109112
Protein Cell, 2021, 10.1007/s13238-021-00858-3
S2853 Carfilzomib (PR-171) Carfilzomib (PR-171) is an irreversible proteasome inhibitor with IC50 of <5 nM in ANBL-6 cells, displayed preferential in vitro inhibitory potency against the ChT-L activity in the β5 subunit, but little or no effect on the PGPH and T-L activities. Carfilzomib activates prosurvival autophagy and induces cell apoptosis.
Cancer Cell, 2021, S1535-6108(20)30609-7
Sci Adv, 2021, 7(23)eabg2697
Autophagy, 2021, 1-14
S2891 GW441756 GW441756 is a potent, selective inhibitor of TrkA with IC50 of 2 nM, with very little activity to c-Raf1 and CDK2. GW441756 produces a relevant increase of caspase-3 that leads to apoptosis.
Biosci Biotechnol Biochem, 2021, 85(3):675-686
Cancer Res, 2020, canres.1992.2020
Mol Neurobiol, 2020, 10.1007/s12035-020-02156-1
S2893 NU7026 NU7026 (LY293646) is a potent DNA-PK inhibitor with IC50 of 0.23 μM in cell-free assays, 60-fold selective for DNA-PK than PI3K and inactive against both ATM and ATR. NU7026 enhances G2/M cell arrest and apoptosis.
Sci Signal, 2022, 15(715):eabh2290
Nucleic Acids Res, 2021, gkab584
Cell Rep, 2021, 37(3):109854
S2913 BAY 11-7082 BAY 11-7082 (BAY 11-7821) is a NF-κB inhibitor, inhibits TNFα-induced IκBα phosphorylation with IC50 of 10 μM in tumor cells. BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 with IC50 of 0.19 μM and 0.96 μM, respectively. BAY 11-7082 induces apoptosis and S phase arrest in gastric cancer cells.
Nat Cell Biol, 2021, 23(4):355-365
Nat Commun, 2021, 12(1):1394
EMBO Rep, 2021, 22(9):e52576
S2942 EB-3D EB-3D is a potent and selective inhibitor of choline kinase α (ChoKα) with IC50 of 1 μM for ChoKα1. EB-3D induces deregulation of the AMPK-mTOR pathway and apoptosis in leukemia T-cells.
S3020 Romidepsin (FK228, Depsipeptide) Romidepsin (FK228, Depsipeptide, FR 901228, NSC 630176) is a potent HDAC1 and HDAC2 inhibitor with IC50 of 36 nM and 47 nM in cell-free assays, respectively. Romidepsin (FK228/depsipeptide) controls growth and induces apoptosis in neuroblastoma tumor cells.
Hepatology, 2021, 10.1002/hep.32245
Hepatology, 2021, 10.1002/hep.32245
Nat Commun, 2021, 12(1):7213
S3035 Daunorubicin (RP 13057) HCl Daunorubicin HCl (Daunomycin, RP 13057, Rubidomycin) inhibits both DNA and RNA synthesis and inhibits DNA synthesis with Ki of 0.02 μM in a cell-free assay. Daunorubicin is a topoisomerase II inhibitor that induces apoptosis.
Blood, 2021, 138(9):790-805
Int J Mol Sci, 2021, 22(3)1362
Sci Rep, 2021, 11(1):12148
S3168New cis-Resveratrol cis-Resveratrol (cis-RESV, cRes, (Z)-Resveratrol) is the Cis isomer of Resveratrol. Resveratrol is a natural phenolic compound with anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol is an inhibitor of pregnane X receptor (PXR) and an activator of Nrf2 and SIRT1 and may induce apoptosis. Resveratrol also inhibits a wide spectrum of targets including 5-lipoxygenase (LOX), cyclooxygenase (COX), IKKβ, DNA polymerases α and δ with IC50 of 2.7 μM, <1 μM, 1 μM, 3.3 μM and 5 μM, respectively.
S3224 Cinobufagin Cinobufagin (Cinobufagine), an active ingredient of Venenum Bufonis, inhibits tumor development. Cinobufagin increases ATM and Chk2 and decreases CDC25C, CDK1, and cyclin B. Cinobufagin inhibits PI3K, AKT and Bcl-2 while increases levels of cleaved caspase-9 and caspase-3. Thus, Cinobufagin induces cell cycle arrest at the G2/M phase and apoptosis.
S3238 Resibufogenin Resibufogenin (Bufogenin, Recibufogenin), a component of huachansu with anticancer effect, triggers necroptosis through upregulating receptor-interacting protein kinase 3 (RIP3) and phosphorylating mixed lineage kinase domain-like protein at Ser358. Resibufogenin exerts cytotoxic effect by inducing reactive oxygen species (ROS) accumulation. Resibufogenin induces apoptosis and caspase-3 and caspase-8 activity. Resibufogenin increases Bax/Bcl-2 expression, and suppresses cyclin D1, cyclin E, PI3K, p-AKT, p-GSK3β and β-catenin protein expression.
S3245 Nodakenetin Nodakenetin (NANI), a plant-derived coumarin isolated from Angelica decursiva, inhibits α-glucosidase, PTP1B, rat lens aldose reductase (RLAR), AChE, BChE, and β-site amyloid precursor protein cleaving enzyme 1 (BACE1). Nodakenetin alters the protein expression of Bax and Bcl-2, and prompts mitochondrial apoptosis. Nodakenetin exhibits anti-tumor activity.
S3256 Tectochrysin Tectochrysin (Techtochrysin, NSC 80687) is one of the major flavonoids of Alpinia oxyphylla Miquel. Tectochrysin significantly increases the expression of DR3, DR4 and Fas and inhibits activity of NF-κB. Tectochrysin induces apoptotic cell death.
S3271 Caudatin Caudatin (Cauldatin), one species of C‑21 steroidal from Cynanchum auriculatum (C. auriculatum), effectively inhibits human glioma growth in vitro and in vivo through triggering cell cycle arrest and apoptosis.
S3287 Rosamultin Rosamultin is a 19 α-hydroxyursane-type triterpenoid isolated from Potentilla anserina L. that inhibits HIV-1 protease. Rosamultin has protective effects on H2O2-induced oxidative damage and apoptosis.
S3289 Daphnoretin Daphnoretin (Dephnoretin, Thymelol), a biologically active compound isolated from Wikstroemia indica C.A. Mey., is a protein kinase C (PKC) activator. Daphnoretin inhibits the proliferation, invasion, and migration of tumor cells and promote its apoptosis by regulating the activity of Akt signal pathway.
S3296 Hispidulin Hispidulin (Dinatin), an active natrual ingredient in a number of traditional Chinese medicinal herbs, exhibits inhibitory activity against the oncogenic protein kinase Pim-1 with IC50 of 2.71 μM. Hispidulin induces apoptosis through mitochondrial dysfunction and inhibition of P13k/Akt signalling pathway in HepG2 cancer cells. Hispidulin exerts anti-osteoporotic and bone resorption attenuating effects via activating the AMPK signaling pathway.
S3300 Desoxyrhaponticin Desoxyrhaponticin (DC, DES), a stilbene glycoside from Rheum tanguticum Maxim. ex Balf. (rhubarb) which is a traditional Chinese nutritional food, is a fatty acid synthase (FAS/FASN) inhibitor. Desoxyrhaponticin (DC, DES) is also a competitive inhibitor of glucose uptake with IC50 of 148.3 μM and 30.9 μM in rabbit intestinal membrane vesicles and in rat everted gut sleeves, respectively. Desoxyrhaponticin has apoptotic effect on human cancer cells.
Nat Metab, 2021, 10.1038/s42255-021-00479-4
S3336 Heptadecanoic acid

Heptadecanoic acid (C17:0), an odd chain saturated fatty acid, significantly inhibits cell proliferation, and migration, while promoting apoptosis in PC‑9 and PC‑9/GR cells. Heptadecanoic acid is associated with several diseases, including the incidence of coronary heart disease, prediabetes and type 2 diabetes as well as multiple sclerosis.

S3357 Elaidic acid

Elaidic acid is a major trans fatty acid that inhibits cell viability, elevates cell apoptosis by enhancing oxidative stress. Elaidic acid can be used as a pharmaceutical solvent.

S3604 Triptolide (PG490) Triptolide (PG490, NSC 163062) is a diterpene triepoxide, immunosuppresive agent extracted from the Chinese herb Tripterygium wilfordii. It functions as a NF-κB inhibitor with dual actions by disruption of p65/CBP interaction and by reduction of p65 protein. Triptolide (PG490) abrogates the transactivation function of heat shock transcription factor 1 (HSF1). Triptolide inhibits MDM2 and induces apoptosis through a p53-independent pathway.
Sci Adv, 2021, 7(7)eabd2645
EMBO Rep, 2021, e52023
Acta Pharmacol Sin, 2021, 10.1038/s41401-021-00657-w
S3829 Isoalantolactone Isoalantolactone, one of the major sesquiterpene lactone compounds, is isolated from the roots of Anula helenium and possesses multiple biological activities including antifungal, anthelmintic, antimicrobial, anti-inflammatory, antitrypanosomal activities and antiproliferative effects on several cancer cell lines, such as colon, melanoma, ovary, prostate, lung, and leukemia. Isoalantolactone is an apoptosis inducer, which also acts as an alkylating agent.
S3984 Nordihydroguaiaretic acid (NDGA) Nordihydroguaiaretic acid (NDGA) is a phenolic antioxidant found in the leaves and twigs of the evergreen desert shrub, Larrea tridentata (Sesse and Moc. ex DC) Coville (creosote bush). It is a recognized inhibitor of lipoxygenase (LOX) and has antioxidant and free radical scavenging properties. Nordihydroguaiaretic acid (NDGA) is a cytotoxic insulin-like growth factor-I receptor (IGF-1R)/HER2 inhibitor and induces apoptosis. Nordihydroguaiaretic acid (NDGA) inhibits p300 and activates autophagy. Nordihydroguaiaretic acid (NDGA) protects cells from ferroptosis.
S4001 Cabozantinib malate (XL184) Cabozantinib malate (XL184) is the malate of Cabozantinib, a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret (c-Ret), Kit (c-Kit), Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM in cell-free assays, respectively. Cabozantinib malate (XL184) induces apoptosis.
Cancer Cell, 2021, S1535-6108(21)00659-0
Clin Cancer Res, 2021, 27(9):2533-2548
Cancers (Basel), 2021, 13(14)3635
S4269 Vinorelbine ditartrate (KW-2307) Vinorelbine Tartrate (KW-2307, Nor-5'-anhydrovinblastine ditartrate) is a semi-synthetic vinca alkaloid, and inhibits mitosis through interaction with tubulin. Vinorelbine Tartrate exhibits anti-tumor activities via inducing the mitotic apoptosis, autophagy and inflammation.
Cancer Res, 2021, canres.0955.2021
Br J Cancer, 2021, 10.1038/s41416-021-01420-y
J Neurochem, 2021, 156(5):642-657
S4423New Emamectin Benzoate Emamectin Benzoate (EMB, MK-244) activates gamma-amino butyric acid (GABA) transporter. Emamectin Benzoate induces of reactive oxygen species (ROS)-mediated DNA damage and apoptosis.
S4476New PCNA-I1 PCNA-I1 is a selective inhibitor of proliferating cell nuclear antigen (PCNA, a potential anticancer target). PCNA-I1 selectively binds to PCNA trimers with Kd of ~0.2 to 0.4 μM. PCNA-I1 inhibits the growth of tumor cells of various tissue types with IC50 of ~0.2 μM. PCNA-I1 induces DNA damage and apoptosis in both LNCaP and PC-3 cells. PCNA-I1 also induces autophagy in PC-3 cells.
S4505 Vinblastine (NSC-49842) sulfate Vinblastine sulfate (NSC49842, Vincaleukoblastine sulfate salt, 29060-LE, Exal, Velban, Velbe) inhibits microtubule formation and suppresses nAChR activity with IC50 of 8.9 μM in a cell-free assay, used to treat certain kinds of cancer. Vinblastine sulfate induces autophagy and apoptosis.
Nat Chem Biol, 2021, 10.1038/s41589-021-00751-4
Cancer Res, 2021, canres.0955.2021
Hum Cell, 2021, 10.1007/s13577-021-00579-z
S4613New Sodium Fluoride Sodium fluoride (NaF) induces apoptosis and autophagy via the endoplasmic reticulum (ER) stress pathway in MC3T3-E1 osteoblastic cells.
S4701 2-Deoxy-D-glucose (2-DG) 2-Deoxy-D-glucose (2-DG, 2-deoxyglucose, NSC 15193, 2-Deoxy-D-arabino-hexose, D-Arabino-2-deoxyhexose), an analog of glucose, is a glycolytic inhibitor with antiviral activity. 2-Deoxy-D-glucose induces apoptosis and inhibits Herpes Simplex Virus type-1 (HSV-1) receptor expression.
Nat Commun, 2021, 12(1):3258
Clin Cancer Res, 2021, clincanres.2092.2021
Autophagy, 2021, 1-19
S4732 MPTP hydrochloride MPTP hydrochloride is a dopaminergic neurotoxin and cause selective destruction of dopaminergic neurons in animal models of parkinsonism. MPTP hydrochloride induces apoptosis.
Neuropharmacology, 2021, 196:108360
J Neuroinflammation, 2020, 17(1):272
Brain Res Bull, 2020, 164:55-64
S5144 Neferine Neferine ((R)-1,2-Dimethoxyaporphine), a natural component of Nelumbo nucifera, has antitumor efficiency. Neferine induces apoptosis in renal cancer cells. Neferine prevents autophagy through activation of Akt/mTOR pathway and Nrf2 in muscle cells. Neferine strongly inhibits NF-κB activation. Neferine possesses a number of therapeutic effects such as anti-diabetic, anti-aging, anti-microbial, anti-thrombotic, anti-arrhythmic, anti-inflammatory and even anti-HIV.
Oncol Rep, 2020, 44(3):1116-1126
S5243 Ruxolitinib Phosphate Ruxolitinib Phosphate (INCB018424, INC424) is the phosphate salt form of Ruxolitinib. Ruxolitinib is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM in cell-free assays, >130-fold selectivity for JAK1/2 versus JAK3. Ruxolitinib kills tumor cells through toxic mitophagy. Ruxolitinib induces autophagy and enhances apoptosis.
Blood, 2022, blood.2021012366
Mol Neurodegener, 2022, 17(1):7
J Exp Clin Cancer Res, 2022, 41(1):10
S5248 Apatinib Apatinib (Rivoceranib, YN968D1) is a potent inhibitor of the VEGF signaling pathway with IC50 values of 1 nM, 13 nM, 429 nM and 530 nM for VEGFR-2, Ret (c-Ret), c-Kit and c-Src, respectively. Apatinib induces both autophagy and apoptosis.
Front Oncol, 2021, 11:739139
Biochem Biophys Res Commun, 2021, 586:177-184
Cells, 2020, 9(6):E1452
S5554 Lanatoside C Lanatoside C is a cardiac glycoside with antiviral and anti-tumor activity. Lanatoside C induces G2/M cell cycle arrest and induces autophagy and apoptosis via attenuating MAPK, Wnt, JAK-STAT, and PI3K/AKT/mTOR signaling pathways.
S5584 Citronellol Citronellol (Dihydrogeraniol, (±)-β-Citronellol), a constituent of rose and geranium oils, is used in perfumes and insect repellents. Citronellol can cause necrotic apoptosis of NCI-H1299 cells by up-regulating TNF-α, RIP1 / RIP3 activities, and down-regulating caspase-3 / caspase-8 activities. Citronellol also results in a biphasic increase in ROS production at 1 h and at 12 h in NCI-H1299 cells.
S5958New Metformin Metformin (1,1-Dimethylbiguanide), a widely used drug for treatment of type 2 diabetes, activates AMP-activated protein kinase (AMPK) in hepatocytes. Metformin promotes mitophagy in mononuclear cells. Metformin induces apoptosis of lung cancer cells through activating JNK/p38 MAPK pathway and GADD153.
Cell Res, 2021, 10.1038/s41422-021-00565-y
Theranostics, 2021, 11(16):8112-8128
Autophagy, 2021, 1-14
S6615 ATB 346 ATB 346, a novel hydrogen sulphide-releasing derivative of naproxen with remarkably reduced toxicity, inhibits COX activity. ATB 346 is an anti-inflammatory agent that induces apoptosis of human melanoma cells.
S6721 JG98 JG-98 is an allosteric inhibitor of Hsp70 that binds tightly to a deep pocket that is conserved in members of the Hsp70 family. JG-98 induces classical apoptosis features, including morphological changes consistent with programmed cell death and positive annexin staining. JG-98 exhibits anticancer activity.
S6852 Gossypol Gossypol (BL 193) is an orally-active polyphenol isolated from cotton seeds and roots. Gossypol is a potent inhibitor of 5α-reductase 1 and 3α-hydroxysteroid dehydrogenase with IC50 of 3.33 μM and 0.52 μM in cell-free assay, respectively. Gossypol also inhibits the binding of BH3 peptide to Bcl protein with IC50 of 0.4 μM and 10 μM for Bcl-XL and Bcl-2, respectively. Gossypol induces apoptosis and cell growth inhibition in various cancer cells.
Mol Med Rep, 2021, 23(1)40
J Biol Chem, 2015, 290(34):20841-55
S6871 Sodium oxamate Sodium oxamate (SO, Aminooxoacetic acid, Oxamic acid) is an inhibitor of lactate dehydrogenase (LDH) that specificly inhibits LDH‑A. Sodium oxamate (SO) induces G2/M cell cycle arrest via downregulation of the CDK1/cyclin B1 pathway and promotes apoptosis through enhancement of mitochondrial ROS generation.
Aging (Albany NY), 2021, 13(24):25920-25930
Int J Biol Sci, 2021, 17(11):2756-2769
S6877 EOAI3402143 EOAI3402143 is a dose-dependent inhibitor of Usp9x, Usp24 and Usp5 that increases tumor cell apoptosis, and fully blocks or regresses myeloma tumors in mice.
Int J Biol Sci, 2021, 17(10):2417-2429
Transl Lung Cancer Res, 2021, 10(10):3995-4011
S6882 HI-TOPK-032 HI-TOPK-032 is a potent and specific inhibitor of TOPK. HI-TOPK-032 also reduces ERK-RSK phosphorylation, regulates of the abundance of p53, cleaved caspase-7, and cleaved PARP, and induces apoptosis in cancer cells.
S6885 Ailanthone Ailanthone (AIL, Δ13-Dehydrochaparrinone), a natural anti-hepatocellular carcinoma (HCC) component in Ailanthus altissima, induces G0/G1-phase cell cycle arrest by decreasing expression of cyclins and CDKs and increases expression of p21 and p27. Ailanthone triggers DNA damage characterized by activation of the ATM/ATR pathway. Ailanthone induces apoptosis which is mitochondrion-mediated and involves the PI3K/AKT signaling pathway in Huh7 cells. Ailanthone is also a potent inhibitor of both full-length Androgen Receptor (AR-FL) and constitutively active truncated AR splice variants (AR-Vs, AR1-651) with IC50 of 69 nM and 309 nM, respectively.
S6894 BCH BCH (2-Aminobicyclo-(2,2,1)-heptane-2-carboxylic acid, LAT1-IN-1) is a selective and competitive inhibitor of system L amino acid transporter 1 (LAT1). BCH (LAT1-IN-1) induces apoptosis in cancer cells.
EMBO Rep, 2021, e51436
S6899 Licochalcone D Licochalcone D (Lico D, LCD, LD), a flavonoid isolated from a Chinese medicinal plant Glycyrrhiza inflata, has antioxidant, anti-inflammatory and anti-cancer properties. Licochalcone D inhibit phosphorylation of NF-κB p65 in LPS signaling pathway. Licochalcone D inhibits JAK2, EGFR and Met (c-Met) activities and induces ROS-dependent apoptosis. Licochalcone D also induces caspases activation and poly (ADP-ribose) polymerase (PARP) cleavage.
S6919 Brevilin A Brevilin A (6-O-Angeloylplenolina), a sesquiterpene lactone isolated from Centipeda minima, is a selective inhibitor of STAT3 and attenuates the JAKs activity by blocking the JAKs tyrosine kinase domain JH1. Brevilin A induces apoptosis and autophagy of colon adenocarcinoma cell CT26 via mitochondrial pathway and PI3K/AKT/mTOR inactivation.
S6957 β-Elemene

β-Elemene ((-)-β-Elemene, Levo-β-elemene) is a sesquiterpene compound extracted from the herb Curcuma Rhizoma with antitumor activities. β-elemene can inhibit cell proliferation, arrest the cell cycle, and induce cell apoptosis or autophagy.

S6962 TPEN

TPEN (TPEDA) is a specific cell-permeable heavy metal chelator that induces apoptosis in NB4 cells via negatively regulating intracellular NO and Zn2+ signaling. TPEN (TPEDA) may be a potential therapeutic strategy for APL (acute promyelocytic leukemia).

Biomaterials, 2021, 271:120720
S6963 APTO-253

APTO-253 (LOR-253, LT-253) inhibits c-Myc expression and selectively induces CDKN1A (p21), promotes G0-G1 cell-cycle arrest, and triggers apoptosis in acute myeloid leukemia (AML) cells. APTO-253 is also an inducer of KLF4 (Krüppel-like factor 4).

S6990 Phytohemagglutinin

Phytohemagglutinin (PHA, Phaseolus vulgaris agglutinin) is expressed in Pichia pastoris using native signal peptides, or the Saccharomyces alpha-factor preprosequence, to direct proteins into the secretory pathway. Phytohemagglutinin induces apoptosis in human HEp-2 carcinoma cells via increasing proapoptotic protein Bax and activating caspases-3.

S7006 BAY-61-3606 BAY-61-3606 is a potent and selective inhibitor of Syk kinase (Ki = 7.5 nM). BAY-61-3606 induces cell cycle arrest and apoptosis.
JCI Insight, 2021, e149376
Biomed Res, 2021, 42(2):53-66
Nat Cell Biol, 2019, 21(6):778-790
S7007 Binimetinib (MEK162) Binimetinib (MEK162, ARRY-162, ARRY-438162) is a potent inhibitor of MEK1/2 with IC50 of 12 nM in a cell-free assay. Binimetinib induces G1 cell cycle arrest and apoptosis in human NSCLC cell lines and induces autophagy. Phase 3.
Cell, 2021, 184(25):6119-6137.e26
Nat Commun, 2021, 12(1):3707
Neuro Oncol, 2021, 23(5):770-782
S7015 Birinapant (TL32711) Birinapant (TL32711) is a SMAC mimetic antagonist, mostly to cIAP1 with Kd of <1 nM in a cell-free assay, less potent to XIAP. Birinapant helps to induce apoptosis in latent HIV-1-infected cells. Phase 2.
Sci Adv, 2021, 7(28)eabf4408
Nat Commun, 2021, 12(1):2482
EMBO Mol Med, 2021, e13466
S7024 Stattic Stattic, the first nonpeptidic small molecule, potently inhibits STAT3 activation and nuclear translocation with IC50 of 5.1 μM in cell-free assays, highly selectivity over STAT1. Stattic induces apoptosis.
Nature, 2021, 600(7888):314-318
Nat Commun, 2021, 12(1):4566
J Cell Biol, 2021, 220(9)e202004114
S7038 Epoxomicin (BU-4061T) Epoxomicin (BU-4061T, Aids010837) is a selective proteasome inhibitor with anti-inflammatory activity, inhibits primarily the CH-L activity of the 20S proteasome, while T-L and PGPH catalytic activities are also inhibited at 100- and 1000-fold reduced rate. Epoxomicin promotes apoptosis.
Nat Microbiol, 2021, 6(9):1163-1174
Cell, 2020, 30;181(3):637-652.e15.
Cell, 2020, 30;181(3):637-652e15
S7046 Brefeldin A Brefeldin A is a lactone antibiotic and ATPase inhibitor for protein transport with IC50 of 0.2 μM in HCT 116 cells, induces cancer cell differentiation and apoptosis. It could also improve the HDR(homology-directed repair) efficiency and be an enhancer of CRISPR-mediated HDR. Brefeldin A is also an inhibitor of autophagy and mitophagy.
Nat Cell Biol, 2021, 10.1038/s41556-021-00704-y
Nat Biomed Eng, 2021, 10.1038/s41551-020-00675-9
Cell Rep, 2021, 36(6):109516
S7076 T0901317 T0901317 is a potent and selective agonist for both LXR and FXR, with EC50 of ~50 nM and 5 μM, respectively. T0901317 is a dual inverse agonist of RORα and RORγ with Ki of 132 nM and 51 nM, respectively. T0901317 significantly suppresses cell proliferation and induces apoptosis.
Front Cardiovasc Med, 2021, 8:746989
Hepatology, 2020, 10.1002/hep.31594
Cell Mol Immunol, 2020, 10.1038/s41423-020-00546-y
S7090 GSK923295 GSK923295 is a first-in-class, specific allosteric inhibitor of CENP-E kinesin motor ATPase with Ki of 3.2 nM, and less potent to mutant I182 and T183. GSK923295 induces post-mitotic apoptosis. Phase 1.
Dis Model Mech, 2021, dmm.049001
Cancer Res, 2020, canres.1693.2020
Cancer Res, 2020, 20 pii: canres 883 2019
S7094 PF-3758309 PF-03758309 (PF-03758309) is a potent, ATP-competitive, pyrrolopyrazole inhibitor of PAK4 with IC50 of 1.3 nM. PF-3758309 is antiproliferative and induces apoptosis in a HCT116 tumor model.
Cancers (Basel), 2021, 14(1)160
Curr Biol, 2021, S0960-9822(21)00626-6
Mol Cancer Ther, 2021, molcanther.1105.2020
S7097 HSP990 (NVP-HSP990) HSP990 (NVP-HSP990) is a novel, potent and selective HSP90 inhibitor for HSP90α/β with IC50 of 0.6 nM/0.8 nM. NVP-HSP990 induces cell cycle arrest and apoptosis.
Mol Cancer Res, 2020, 18(7):1004-1017
Mol Cancer Res, 2020, 10.1158/1541-7786.MCR-19-0669
Theranostics, 2020, 10(18):8415-8429
S7104 AZD1208 AZD1208 is a potent, and orally available Pim kinase inhibitor with IC50 of 0.4 nM, 5 nM, and 1.9 nM for Pim1, Pim2, and Pim3 in cell-free assays, respectively. AZD1208 induces autophagy, cell cycle arrest and apoptosis. Phase 1.
Cell Rep, 2021, 35(8):109160
Cancers (Basel), 2021, 13(9)2139
FASEB J, 2021, 35(6):e21656
S7106 AZD3463 AZD3463 is a novel orally bioavailable ALK inhibitor with Ki of 0.75 nM, which also inhibits IGF1R with equivalent potency. AZD3463 suppresses cell viability by inducing both cell apoptosis and autophagy.
Cancers (Basel), 2020, 12(9)E2668
Aging (Albany NY), 2020, 7;12(9):8221-8240
Burns Trauma, 2020, 8:tkaa025
S7129 PYR-41 PYR-41 is the first cell-permeable inhibitor of ubiquitin-activating enzyme E1, with no activity at E2. PYR-41 induce apoptosis.
J Clin Invest, 2021, 146893
Biomaterials, 2021, 271:120720
Cell Chem Biol, 2021, S2451-9456(21)00213-0
S7152 C646 C646 is an inhibitor for histone acetyltransferase, and inhibits p300 with a Ki of 400 nM in a cell-free assay. Preferentially selective for p300 versus other acetyltransferases. C646 induces cell cycle arrest, apoptosis and autophagy.
Hepatology, 2021, 10.1002/hep.32245
Hepatology, 2021, 10.1002/hep.32245
Cancer Lett, 2021, 513:36-49
S7153 10058-F4 10058-F4 is a c-Myc inhibitor that specificallly inhibits the c-Myc-Max interaction and prevents transactivation of c-Myc target gene expression. 10058-F4 promotes a caspase-3-dependent apoptosis and modulates autophagy.
J Immunother Cancer, 2021, 9(7)e002528
Cancer Res, 2021, canres.1023.2021
Redox Biol, 2021, 39:101811
S7162 Mdivi-1 Mdivi-1 (Mitochondrial division inhibitor 1) is a selective cell-permeable inhibitor of mitochondrial division DRP1 (dynamin-related GTPase) and mitochondrial division Dynamin I (Dnm1) with IC50 of 1-10 μM. Mdivi-1 attenuates mitophagy and enhances apoptosis.
Cancer Discov, 2022, 12(1):250-269
Cell Rep, 2021, 37(13):110155
Autophagy, 2021, 1-19
S7165 UNC1999 UNC1999 is a potent, orally bioavailable and selective inhibitor of EZH2 and EZH1 with IC50 of 2 nM and 45 nM in cell-free assays, respectively, showing >1000-fold selectivity over a broad range of epigenetic and non-epigenetic targets. UNC1999 is a potent autophagy inducer. UNC1999 specifically suppresses H3K27me3/2 and induces a range of anti-leukemia effects including anti-proliferation, differentiation, and apoptosis.
J Immunol, 2022, 208(2):347-357
Hepatology, 2021, 10.1002/hep.32245
Hepatology, 2021, 10.1002/hep.32245
S7177 PF-543 PF-543, a novel sphingosine-competitive inhibitor of SphK1, inhibits SphK1 with IC50 and Ki of 2.0 nM and 3.6 nM, exhibits >100-fold selectivity over the SphK2 isoform. PF-543 induces apoptosis, necrosis, and autophagy.
J Pharmacol Exp Ther, 2021, 378(3):300-310
Phytother Res, 2021, 10.1002/ptr.7211
Cancer Biol Ther, 2020, 21(9):841-852
S7198 BIO BIO (GSK-3 Inhibitor IX, 6-bromoindirubin-3-oxime, 6-Bromoindirubin-3'-oxime, MLS 2052) is a specific inhibitor of GSK-3 with IC50 of 5 nM for GSK-3α/β in a cell-free assay, shows >16-fold selectivity over CDK5, also a pan-JAK inhibitor with IC50 of 30 nM for Tyk2. BIO induces apoptosis in human melanoma cells.
Development, 2022, 149(1)dev200021
Sci Rep, 2022, 12(1):7
Mol Cell, 2021, 81(18):3803-3819.e7
S7204 Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium Fosbretabulin (Combretastatin A4 Phosphate, CA4P, CA 4DP) Disodium is the water-soluble prodrug of Combretastatin A4 (CA4), which is a microtubule-targeting agent that binds β-tubulin with Kd of 0.4 μM in a cell-free assay. Fosbretabulin Disodium inhibits the polymerization of tubulin with IC50 of 2.4 μM, and also disrupts tumor vasculature. Fosbretabulin disodium induces mitotic arrest and apoptosis in endothelial cells. Phase 3.
Cell, 2020, 182(3):685-712.e19
Cell, 2020, 182(3):685-712.e19
J Drug Target, 2020, 10.1080/1061186X.2020.1818759
S7215 Losmapimod (GW856553X) Losmapimod (GW856553X, GW856553, GSK-AHAB) is a selective, potent, and orally active p38 MAPK inhibitor with pKi of 8.1 and 7.6 for p38α and p38β, respectively. P38 MAPKs are involved in cell differentiation, apoptosis and autophagy. Phase 3.
Free Radic Biol Med, 2021, 167:243-257
Cell, 2020, 182(3):685-712.e19
Cell, 2020, 182(3):685-712.e19
S7255 Onvansertib (NMS-P937) Onvansertib (NMS-P937, PCM-075, NMS1286937) is an orally available, selective Polo-like Kinase 1 (PLK1) inhibitor with IC50 of 2 nM, 5000-fold selectivity over PLK2/PLK3. Onvansertib (NMS-P937) potently causes a mitotic cell-cycle arrest followed by apoptosis in cancer cell lines and inhibits tumor growth. Phase 1.
Theranostics, 2021, 11(19):9571-9586
Cell Res, 2019, 29(9):725-738
Sci Rep, 2018, 8(1):3521
S7276 SGI-1027 SGI-1027 (DNA Methyltransferase Inhibitor II) is a DNMT inhibitor with IC50 of 6, 8, 7.5 μM for DNMT1, DNMT3A, and DNMT3B in cell-free assays, respectively. SGI‑1027 induces apoptosis.
Oxid Med Cell Longev, 2021, 2021:5550196
J Ethnopharmacol, 2021, 281:114559
J Med Chem, 2020, 31
S7281 JIB-04 JIB-04 (NSC 693627) is a pan-selective Jumonji histone demethylase inhibitor with IC50 of 230, 340, 855, 445, 435, 1100, and 290 nM for JARID1A, JMJD2E, JMJD3, JMJD2A, JMJD2B, JMJD2C, and JMJD2D in cell-free assays, respectively. JIB‑04 also induces cell apoptosis.
Mol Ther Oncolytics, 2021, 20:583-595
Sci Rep, 2021, 11(1):2942
Research Square, 2021, 10.21203/rs.3.rs-620216/v1
S7353 EPZ004777 EPZ004777 is a potent, selective DOT1L inhibitor with IC50 of 0.4 nM in a cell-free assay and demonstrates >1,200-fold selectivity for DOT1L over all other tested PMTs. EPZ004777 induces apoptosis.
Proc Natl Acad Sci U S A, 2021, 118(29)e2104013118
Nat Chem Biol, 2020, 10.1038/s41589-020-0618-6
Cancer Cell, 2019, 35(5):752-766
S7358 Poziotinib (HM781-36B) Poziotinib (HM781-36B, NOV120101) is an irreversible pan-HER inhibitor with IC50 of 3.2 nM, 5.3 nM and 23.5 nM for HER1, HER2, and HER4, respectively. Poziotinib also induces apoptosis and G1 cell cycle arrest. Phase 2.
Cancer Cell, 2021, S1535-6108(21)00284-1
Mol Cancer Ther, 2021, molcanther.0371.2021
Transl Lung Cancer Res, 2021, 10(8):3659-3670
S7362 AZD5582 AZD5582, a novel small-molecule IAP inhibitor, binds potently to the BIR3 domains of cIAP1, cIAP2, and XIAP with IC50 values of 15, 21, and 15
Sci Rep, 2022, 12(1):45
J Virol, 2021, JVI.01297-20
Life Sci Alliance, 2020, 28;3(6) pii: e202000735
S7369 4EGI-1 4EGI-1 is a competitive eIF4E/eIF4G interaction inhibitor by binding to eIF4E with KD of 25 μM. 4EGI-1 specifically inhibits the function of mTOR by blocking the activation of 4E-BP1. 4EGI-1 induces apoptosis.
FASEB J, 2021, 35(5):e21445
Mol Pharmacol, 2021, 99(1):1-16
J Cell Mol Med, 2021, 10.1111/jcmm.16307
S7379 E-64 E-64 is an irreversible and selective cysteine protease inhibitor, and also inhibits papain, calpain, and cathepsins B and H, but not serine proteases or aspartic proteases. The IC50 for papain is 9 nM. E-64 induces oxidative stress and apoptosis in Filarial Parasite.
Sci Adv, 2021, 7(3)eabc6364
Cell Chem Biol, 2021, S2451-9456(21)00213-0
Epigenetics Chromatin, 2021, 14(1):23
S7396 Calpeptin Calpeptin is a potent, cell-permeable calpain inhibitor with ID50 of 52 nM, 34 nM, 138 nM, and 40 nM for Calpain I (porcine erythrocytes), Calpain II (porcine kidney), Papainb, and Calpain I (human platelets), respectively. Calpeptin attenuates apoptosis and intracellular inflammatory changes in muscle cells.
Cell Death Discov, 2021, 7(1):374
Int J Mol Sci, 2021, 22(22)12134
Clin Res Hepatol Gastroenterol, 2021, S2210-7401(21)00158-3
S7397 Sorafenib (BAY 43-9006) Sorafenib (BAY 43-9006, NSC-724772) is a multikinase inhibitor of Raf-1 and B-Raf with IC50 of 6 nM and 22 nM in cell-free assays, respectively. Sorafenib inhibits VEGFR-2, VEGFR-3, PDGFR-β, Flt-3 and c-KIT with IC50 of 90 nM, 20 nM, 57 nM, 59 nM and 68 nM, respectively. Sorafenib induces autophagy and apoptosis and activates ferroptosis with anti-tumor activity.
Cell Death Dis, 2022, 13(1):35
Genome Biol, 2021, 22(1):41
Nat Chem Biol, 2021, 10.1038/s41589-021-00751-4
S7409 Anisomycin Anisomycin (Flagecidin, Wuningmeisu C) is a bacterial antibiotic isolated from Streptomyces griseolus, which inhibits protein synthesis, and also act as a JNK activator. Anisomycin upregulates autophagy and increases apoptosis.
Cell Rep, 2021, 36(7):109515
Acta Neuropathol Commun, 2021, 9(1):169
Int J Mol Sci, 2021, 22(12)6570
S7421 CGP 57380 CGP 57380 is a potent MNK1 inhibitor with IC50 of 2.2 μM, exhibiting no inhibitory activity on p38, JNK1, ERK1 and -2, PKC, or c-Src-like kinases. CGP 57380 upregulates β-catenin and potentiates radiation-induced apoptosis.
J Cancer, 2020, 11(4):990-996
Bioorg Med Chem, 2018, 26(16):4602-4614
Cancer Lett, 2016, 10.1016/j.canlet.2016.02.052
S7465 FTI 277 HCl FTI 277 HCl is the methyl ester of FTI 277, which is a potent and selective farnesyltransferase (FTase) inhibitor with IC50 of 500 pM, about 100-fold selectivity over the closely related GGTase I. FTI 277 HCl inhibits cell growth and induces apoptosis. FTI 277 HCl is effective in clearing HDV viremia.
PLoS Biol, 2021, 19(4):e3001134
Cell Struct Funct, 2021, 46(1):1-9
Nat Commun, 2019, 10(1):273
S7501 HO-3867 HO-3867, an analog of curcumin, is a selective STAT3 inhibitor that inhibits its phosphorylation, transcription, and DNA binding without affecting the expression of other active STATs. HO-3867 induces apoptosis.
Sci Rep, 2022, 12(1):7
Nature, 2021, 600(7888):314-318
Acta Pharm Sin B, 2021, 11(2):394-405
S7536 Lorlatinib (PF-6463922) Lorlatinib (PF-6463922) is a potent, dual ALK/ROS1 inhibitor with Ki of <0.02 nM, <0.07 nM, and 0.7 nM for ROS1, ALK (WT), and ALK (L1196M), respectively. PF-06463922 induces apoptosis. Phase 1.
Nature, 2021, 600(7888):319-323
Cancer Cell, 2021, S1535-6108(21)00492-X
Nat Commun, 2021, 12(1):6813
S7612 PX-478 2HCl PX-478 2HCl is an orally active, and selective hypoxia-inducible factor-1α (HIF-1α) inhibitor. PX-478 2HCl induces apoptosis and has anti-tumor activity. Phase 1.
Proc Natl Acad Sci U S A, 2021, 118(15)e2101080118
Front Immunol, 2021, 12:753092
Aging (Albany NY), 2021, 13(7):10431-10449
S7625 Niraparib (MK-4827) tosylate Niraparib tosylate (MK-4827, ZEJULA) is a selective inhibitor of PARP1/PARP2 with IC50 of 3.8 nM/2.1 nM. Niraparib increases formation of PARP-DNA complexes resulting in DNA damage, apoptosis, and cell death.
Sci Transl Med, 2021, 13(592)eabc7211
Sci Adv, 2021, 7(21)eabf0197
Proc Natl Acad Sci U S A, 2021, 118(40)e2109252118
S7648 OTS964 OTS964 is a potent TOPK inhibitor with high affinity and selectivity and IC50 value is 28 nM. OTS964 is also a potent inhibitor of the cyclin-dependent kinase CDK11 with Kd of 40 nM. OTS964 treatment activates autophagy in glioma cells and induces apoptosis of human lung cancer cells in mouse xenografts.
Mol Imaging Biol, 2019, 21(4):705-712
S7652 OTS514 hydrochloride OTS514 is a highly potent TOPK(T-LAK cell-originated protein kinase) inhibitor with an IC50 value of 2.6 nM. OTS514 induces cell cycle arrest and apoptosis.
Mol Oncol, 2021, 15(12):3721-3737
Oncogenesis, 2021, 10(1):9
Virchows Arch, 2021, 10.1007/s00428-021-03062-0
S7653 PND-1186 (VS-4718) PND-1186 (VS-4718, SR-2156) is a reversible and selective FAK inhibitor with IC50 of 1.5 nM. PND-1186 selectively promotes tumor cell apoptosis. Phase 1.
J Exp Clin Cancer Res, 2021, 40(1):364
J Exp Clin Cancer Res, 2021, 40(1):91
Front Pharmacol, 2021, 12:739501
S7668 Picropodophyllin (PPP) Picropodophyllin (PPP, AXL1717) is a IGF-1R inhibitor with IC50 of 1 nM. It displays selectivity for IGF-1R and does not coinhibit tyrosine phosphorylation the IR, or of a selected panel of receptors less related to IGF-IR(FGF-R, PDGF-R, OR EGF-R). Picropodophyllin (PPP) induces apoptosis with antineoplastic activity.
Sci Adv, 2021, 7(27)eabf1068
Cell Rep, 2021, 34(3):108657
Cell Rep, 2021, 34(3):108657
S7678 Sacubitril/valsartan (LCZ696) Sacubitril/valsartan (LCZ696, Sacubitril, Valsartan), consisting of valsartan and sacubitril in 1:1 molar ratio, is an orally bioavailable, dual-acting angiotensin receptor-neprilysin inhibitor (ARNi) for hypertension and heart failure. Phase 3.
Cardiovasc Res, 2021, 117(5):1391-1401
Neurotox Res, 2021, 10.1007/s12640-021-00414-1
J Mol Cell Cardiol, 2017, 108:138-148
S7680 SP2509 SP2509 (HCI-2509) is a selective histone demethylase LSD1 inhibitor with IC50 of 13 nM, showing no activity against MAO-A, MAO-B, lactate dehydrogenase and glucose oxidase. SP2509 induces apoptosis and promotes autophagy.
Cell Death Dis, 2021, 12(11):993
Front Cell Dev Biol, 2021, 9:694071
Acta Biochim Biophys Sin (Shanghai), 2021, gmab083
S7724 Eprenetapopt (APR-246) Eprenetapopt (APR-246, PRIMA-1MET) is a small organic molecule that has been shown to restore tumour-suppressor function primarily to mutant p53 and also to induce cell death in various cancer types. APR-246 induces apoptosis and autophagy.
Haematologica, 2021, 10.3324/haematol.2020.259531
Cancers (Basel), 2021, 13(17)4476
Int J Mol Sci, 2021, 22(11)5782
S7747 Ro-3306 RO-3306 is an ATP-competitive, and selective CDK1 inhibitor with Ki of 20 nM, >15-fold selectivity against a diverse panel of human kinases. RO-3306 enhances p53-mediated Bax activation and mitochondrial apoptosis.
Mol Cancer Res, 2022, molcanres.0612.2021
Commun Biol, 2022, 5(1):39
Science, 2021, 371(6535)eabc5386
S7776 Akti-1/2 Akti-1/2 (Akt Inhibitor VIII) is a highly selective Akt1/Akt2 inhibitor with IC50 of 58 nM/210 nM, respectively, about 36-fold selectivity for Akt1 over Akt3. Akti-1/2 induces apoptosis.
Cancer Lett, 2021, 519:130-140
J Cell Physiol, 2020, 235(2):1051-1064
Mol Ther Oncolytics, 2020, 18:282-294
S7781 Sunitinib (SU11248) Sunitinib (SU11248) is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit. Sunitinib is also a dose-dependent inhibitor of the autophosphorylation activity of IRE1α. Sunitinib induces autophagy and apoptosis.
Adv Sci (Weinh), 2021, e2100881
Nat Chem Biol, 2021, 10.1038/s41589-021-00947-8
Blood Cancer J, 2021, 11(3):57
S7785 Pemetrexed Disodium Hydrate Pemetrexed Disodium Hydrate (LY-231514) is a novel antifolate and antimetabolite for TS, DHFR and GARFT with Ki of 1.3 nM, 7.2 nM and 65 nM, respectively. Pemetrexed Disodium Hydrate stimulates autophagy and apoptosis.
Nat Biotechnol, 2021, 10.1038/s41587-021-00860-4
J Exp Clin Cancer Res, 2021, 40(1):344
Br J Cancer, 2021, 10.1038/s41416-021-01441-7
S7793 Purvalanol A Purvalanol A is a potent, and cell-permeable CDK inhibitor with IC50 of 4 nM, 70 nM, 35 nM, and 850 nM for cdc2-cyclin B, cdk2-cyclin A, cdk2-cyclin E, and cdk4-cyclin D1, respectively. Purvalanol A induces endoplasmic reticulum stress-mediated apoptosis and autophagy.
Cancer Res, 2022, canres.1707.2021
Cancer Lett, 2021, 526:53-65
Mol Neurobiol, 2021, 10.1007/s12035-021-02581-w
S7818 Pexidartinib (PLX3397) Pexidartinib (PLX3397) is an oral, potent mutil-targeted receptor tyrosine kinase inhibitor of CSF-1R, Kit (c-Kit), and FLT3 with IC50 of 20 nM, 10 nM and 160 nM, respectively. Pexidartinib (PLX3397) induces apoptosis and necrosis with antitumor activity. Phase 3.
Cell Death Dis, 2022, 13(1):33
Sci Transl Med, 2021, 13(598)eabd4550
J Exp Med, 2021, 218(8)e20210542
S7846 Dubermatinib(TP-0903) TP-0903 is a potent and selective AXL Inhibitor with IC50 of 27 nM. TP-0903 is highly effective in inducing apoptosis.
Cancer Cell, 2021, S1535-6108(21)00492-X
Exp Ther Med, 2021, 22(5):1321
Mol Cell, 2020, 7;S1097-2765(20)30269-0
S7867 Oleuropein Oleuropein is an antioxidant polyphenol isolated from olive leaf. Oleuropein exerts antioxidant, anti-inflammatory and anti-atherogenic effects and suppresses the adipocyte differentiation in vitro. Oleuropein inhibits PPARγ activity. Oleuropein exerts anti-adipogenic effect through direct inhibition of PPARγ transcriptional activity. Oleuropein also inhibits aromatase. Oleuropein induces apoptosis. Phase 2.
J Med Virol, 2019, 91(8):1440-1447
S7885 SBI-0206965 SBI-0206965 is a highly selective autophagy kinase ULK1 inhibitor with IC50 of 108 nM, about 7-fold selectivity over ULK2. SBI-0206965 inhibits autophagy and enhances apoptosis in human glioblastoma and lung cancer cells.
Mol Cell, 2021, S1097-2765(21)00729-2
Prog Neurobiol, 2021, S0301-0082(21)00137-4
Int J Mol Sci, 2021, 22(4)2046
S7888 Spautin-1 Spautin-1 is a potent and specific autophagy inhibitor, and inhibits the deubiquitinating activity of USP10 and USP13 with IC50 of ∼0.6-0.7 μM. Spautin-1 enhances apoptosis.
J Clin Invest, 2021, 146893
Protein Cell, 2021, 10.1007/s13238-021-00858-3
Autophagy, 2021, 1-19
S7889 Xanthohumol Xanthohumol, a prenylated chalcone from hop, inhibits COX-1 and COX-2 activity and shows chemopreventive effects. Xanthohumol inhibits diacylglycerol acyltransferase 1 (DGAT1) and DGAT2 with both IC50 of 40 μM. Xanthohumol is also a potent antiviral agent against a series of DNA and RNA viruses. Xanthohumol induces growth inhibition and apoptosis in cancer cells. Phase 1.
Int J Mol Sci, 2021, 22(22)12134
J-Cancer, 2020, 6;11-14-:4047-4058
Oncol Rep, 2020, 44(4):1365-1374
S7895 Thapsigargin Thapsigargin is a potent, non-competitive inhibitor of the sarco/endoplasmic reticulum Ca2+ ATPase (SERCA) with IC50 of 0.353 nM or 0.448 nM for the carbachol-evoked [Ca2+]i-transients with or without a KCl-prestimulation. Thapsigargin induces cell apoptosis. Thapsigargin is extracted from a plant, Thapsia garganica.
Cell Res, 2021, 10.1038/s41422-021-00565-y
Sci Adv, 2021, 7(3)eabc6364
Autophagy, 2021, 1-16
S7960 Larotrectinib (LOXO-101) sulfate Larotrectinib sulfate (LOXO-101, ARRY-470) is an oral potent and selective ATP-competitive inhibitor of tropomyosin receptor kinases (TRK). Larotrectinib inhibition of TRKs induces cellular apoptosis and G1 cell-cycle arrest.
Int J Mol Sci, 2021, 23(1)395
J Neuropathol Exp Neurol, 2021, nlab016
Journal of Cancer, 2021, 12(21): 6356-6362
S7963 TIC10 (ONC201) TIC10 (ONC201) inactivates Akt and ERK to induce TNF-related apoptosis-inducing ligand (TRAIL) through Foxo3a, possesses superior drug properties: delivery across the blood-brain barrier, superior stability and improved pharmacokinetics. Phase 1/2.
Mol Cell, 2020, 80(6):1104-1122.e9
ACS Chem Biol, 2019, 14(5):1020-1029
Eur J Pharmacol, 2019, 857:172423
S7985 PIM447 (LGH447) PIM447 (LGH447) is a novel pan-PIM kinase inhibitor with Ki values of 6 pM, 18 pM, 9 pM for PIM1, PIM2, PIM3 respectively. It also inhibits GSK3β, PKN1, and PKCτ, but at a significantly lower potency with IC50 between 1 and 5 μM (>105-fold differential relative to the Ki on PIMs). PIM447 induces apoptosis.
Cancer Res, 2021, canres.1023.2021
J Pediatr Surg, 2021, S0022-3468(21)00173-1
Chem Pharm Bull (Tokyo), 2021, 69(9):854-861
S8001 Ricolinostat (ACY-1215) Ricolinostat (ACY-1215, Rocilinostat) is a selective HDAC6 inhibitor with IC50 of 5 nM in a cell-free assay. It is >10-fold more selective for HDAC6 than HDAC1/2/3 (class I HDACs) with slight activity against HDAC8, minimal activity against HDAC4/5/7/9/11, Sirtuin1, and Sirtuin2. Ricolinostat (ACY-1215) suppresses cell proliferation and promotes apoptosis. Phase 2.
Cancer Res, 2021, 81(20):5325-5335
Blood Cancer J, 2021, 11(12):194
Elife, 2021, 10e63810
S8018 Nirogacestat (PF-03084014) Nirogacestat (PF-03084014, PF-3084014) is a selective gamma-secretase inhibitor with IC50 of 6.2 nM in a cell-free assay. Nirogacestat (PF-03084014, PF-3084014) induces apoptosis. Phase 2.
Stem Cell Res Ther, 2020, 11(1):258
Pharm Res, 2020, 37(10):185
Mol Ther Oncolytics, 2019, 13:58-66
S8024 Tyrphostin AG 1296 Tyrphostin AG 1296 is an inhibitor of PDGFR with IC50 of 0.3-0.5 μM, no activity to EGFR. Tyrphostin AG1296 inhibits FGFR and c-Kit with IC50 of 12.3 μM and 1.8 μM in Swiss 3T3 cells. Tyrphostin AG1296 induces dramatic apoptosis in A375R cells.
J Cardiovasc Dev Dis, 2021, 8(3)28
Mol Med Rep, 2021, 23(4):1
CellPress, 2021, None
S8041 Cobimetinib (GDC-0973) Cobimetinib (GDC-0973, RG7420) is a potent and highly selective MEK1 inhibitor with IC50 of 4.2 nM, showing more than 100-fold selectively for MEK1 over MEK2 and showed no significant inhibition when tested against a panel of more than 100 of serine-threonine and tyrosine kinases. Cobimetinib induces apoptosis. Phase 3.
Clin Cancer Res, 2021, 10.1158/1078-0432.CCR-21-2660
EMBO Mol Med, 2021, e11814
EMBO Mol Med, 2021, e13466
S8049 Tubastatin A Tubastatin A is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay. It is selective against all the other isozymes (1000-fold) except HDAC8 (57-fold). Tubastatin A promotes autophagy and increases apoptosis.
Sci Adv, 2021, 7(49):eabk0490
Sci Adv, 2021, 7(49):eabk0490
Thyroid, 2021, 10.1089/thy.2020.0948
S8058 Riviciclib hydrochloride (P276-00) Riviciclib hydrochloride (P276-00) is a novel CDK1, CDK4 and CDK9 inhibitor with IC50 of 79 nM, 63 nM and 20 nM, respectively. Riviciclib hydrochloride (P276-00) induces apoptosis. Phase 2/3.
Arthritis Res Ther, 2021, 23(1):47
BMC Genomics, 2021, 22(1):160
Mol Cell, 2020, 77(6):1322-1339
S8059 Nutlin-3a Nutlin-3a ((-)-Nutlin-3), the active enantiomer of Nutlin-3, inhibits the p53/MDM2 interaction with IC50 of 90 nM in a cell-free assay. Nutlin-3a induces autophagy and apoptosis in a p53-dependent manner.
PLoS Biol, 2021, 19(8):e3001364
Cell Death Dis, 2021, 12(7):663
Cell Death Dis, 2021, 12(4):364
S8075 GANT61 GANT61 (NSC 136476) is an inhibitor for GLI1 as well as GLI2-induced transcription, inhibits hedgehog with IC50 of 5 μM in GLI1 expressing HEK293T cell, displays selectivity over other pathways, such as TNF and glucocorticoid receptor gene transactivation. GANT61 induces apoptosis and activates protective autophagy in LX-2 cells.
Sci Rep, 2022, 12(1):7
Blood, 2021, blood.2020010207
Elife, 2021, 10e70729
S8078 Bardoxolone Methyl Bardoxolone Methyl (RTA 402, TP-155, NSC 713200, CDDO Methyl Ester, CDDO-Me) is an IKK inhibitor, showing potent proapoptotic and anti-inflammatory activities; Also a potent Nrf2 activator and nuclear factor-κB (NF-κB) inhibitor. Bardoxolone Methyl abrogates ferroptosis. Bardoxolone methyl induces apoptosis and autophagy in cancer cells.
Drug Des Devel Ther, 2021, 15:21-35
Cancers (Basel), 2020, 12(6):E1645
Antioxidants (Basel), 2020, 9(1)
S8117 GMX1778 (CHS828) GMX1778 (CHS828) is a potent and specific inhibitor of nicotinamide phosphoribosyltransferase (NAMPT) with IC50 and Kd of < 25 nM and 120 nM, respectively. GMX1778 induces programmed cell death with apoptotic features. Phase 1.
Cancer Res, 2020, 80(4):890-900
Acta Physiol (Oxf), 2020, 10.1111/apha.13439
Signal Transduct Target Ther, 2017, 2:17017
S8141 Cl-amidine Cl-amidine is an irreversible pan-peptidylarginine deiminase (PAD) inhibitor with IC50 values of 5.9 ± 0.3 μM, 0.8 ± 0.3 μM, 6.2 ± 1.0 μM for PAD4, PAD1 and PAD3, respectively. Cl-amidine induces apoptosis.
Theranostics, 2021, 11(19):9431-9451
Int J Mol Sci, 2021, 22(23)12852
Phytomedicine, 2021, 90:153635
S8146 Mitomycin C Mitomycin C is an antineoplastic antibiotic by inhibiting DNA synthesis, used to treat different cancers. Mitomycin C induces apoptosis in a caspases-dependent and Fas/CD95-independent manner.
Cell Res, 2021, 10.1038/s41422-021-00592-9
Cell Res, 2021, 1-13
Proc Natl Acad Sci U S A, 2021, 118(10)e2005568118
S8148 PD0166285 PD0166285 is a potent Wee1 and Chk1 inhibitor with activity at nanomolar concentrations (IC50=24 nM for Wee1 and 72 nM for Myt1). PD0166285 is also a novel G2 checkpoint abrogator. PD0166285 induces apoptosis.
Cancer Sci, 2020, 112(1):133-143
Nature, 2019, 10.1038/s41586-019-1607-3
Nature, 2019, 574(7777):268-272
S8149 NSC348884 NSC348884, as a nucleophosmin inhibitor, inhibit cell proliferation and induce apoptosis in various cancer cell lines with IC50 values ranging from 1.4-4 µM.
Nat Commun, 2020, 3;11(1):1669
Virulence, 2020, 11(1):1379-1393
Reproduction, 2020, 160(4):491-500
S8156 ARS-853 (ARS853) ARS-853 is a selective, covalent KRAS(G12C) inhibitor that inhibits mutant KRAS-driven signaling by binding to the GDP-bound oncoprotein and preventing activation. ARS-853 also induces apoptosis.
ProQuest, 2020, N/A
Mol Ther Oncolytics, 2019, 14:266-278
S8244 Etomoxir sodium salt Etomoxir sodium salt is an irreversible inhibitor of carnitine palmitoyltransferase-1 (CPT-1) on the outer face of the inner mitochondrial membrane. Etomoxir enhances palmitate-induced cell apoptosis.
Nat Commun, 2021, 12(1):5203
Proc Natl Acad Sci U S A, 2021, 118(22)e2014681118
Cell Rep, 2021, 36(8):109607
S8246 RK-33 RK-33 is a first-in-class small molecule inhibitor of DDX3 (a RNA helicase) and causes G1 cell cycle arrest, induces apoptosis, and promotes radiation sensitization in DDX3-overexpressing cells.
Nat Commun, 2021, 12(1):2475
Cancer Res, 2021, 81(13):3607-3620
Front Immunol, 2021, 12:616402
S8317 3BDO 3BDO, a butyrolactone derivative, could target FKBP1A and activate the mTOR signaling pathway. It inhibits autophagy in HUVECs. 3BDO inhibits oxLDL-induced apoptosis.
Front Oncol, 2021, 11:665420
Mol Med Rep, 2021, 24(2)592
Biomed Res Int, 2020, 2020:4035306
S8341 TAK-243 (MLN7243) TAK-243 (MLN7243) is a potent, mechanism-based small-molecule inhibitor of the ubiquitin activating enzyme (UAE) with an IC50 of 1 ± 0.2 nM in the UBCH10 E2 thioester assay. It has minimal inhibitory activity in a panel of kinase and receptor assays, as well as on human carbonic anhydrase type I and type II. TAK-243 (MLN7243) induces ER stress, abrogates NFκB pathway activation and promotes apoptosis.
Arch Toxicol, 2022, 10.1007/s00204-021-03195-w
Mol Cell, 2021, 81(7):1411-1424.e7
Elife, 2021, 10e72328
S8365 Apoptozole Apoptozole (Apoptosis Activator VII) is an inhibitor of heat shock protein 70(HSP70) and Hsc70 with dissociation constants Kd of 0.14 μM and 0.21 μM, respectively. It induces caspase-dependent apoptosis.
Nat Commun, 2018, 9(1):4700
Platelets, 2018, 29(6):610-621
S8375 AZD0156 AZD0156 is a potent and selective inhibitors of ATM kinase, with potential chemo-/radio-sensitizing and antineoplastic activities. AZD0156 prevents DNA damage checkpoint activation, disrupts DNA damage repair, induces tumor cell apoptosis, and leads to cell death of ATM-overexpressing tumor cells.
Cell Rep, 2022, 38(2):110216
Nat Neurosci, 2021, 10.1038/s41593-021-00923-4
Nucleic Acids Res, 2021, gkab643
S8400 Mivebresib (ABBV-075) Mivebresib (ABBV-075) is a novel BET family bromodomain inhibitor. It binds bromodomains of BRD2/4/T with similar affinities (Ki of 1-2.2 nM) and highly selective for 18 bromodomain proteins tested (Kd > 1 μM; more than 600-fold selectivity vs. BRD4), but exhibits roughly 10-fold weaker potency towards BRD3 (Ki of 12.2 nM) and has moderate activity towards CREBBP (Kd = 87 μM; 54-fold selectivity vs. BRD4). Mivebresib(ABBV-075) efficiently triggers apoptosis in various tumor cell.
Sci Rep, 2022, 12(1):7
Bioorg Chem, 2021, 115:105238
Cell Rep, 2020, 32(12):108166
S8401 Erdafitinib (JNJ-42756493) Erdafitinib (JNJ-42756493) is a potent and selective orally bioavailable, pan fibroblast growth factor receptor (FGFR) inhibitor with potential antineoplastic activity. Erdafitinib also binds to RET (c-RET), CSF-1R, PDGFR-α/PDGFR-β, FLT4, Kit (c-Kit) and VEGFR-2 and induces cellular apoptosis.
Oncoimmunology, 2022, 11(1):2021619
Nature, 2021, 10.1038/s41586-020-03085-8
Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x
S8402 KRIBB11 KRIBB11 abolishes the heat shock-induced luciferase activity with an IC50 of 1.2 μM. It is an inhibitor of the transcription factor Heat Shock Factor 1 (HSF1). KRIBB11 induces growth arrest and apoptosis.
Cell Metab, 2021, S1550-4131(21)00183-2
Br J Pharmacol, 2021, 178(5):1182-1199
Cancers (Basel), 2021, 13(12)2987
S8405 RRx-001 RRx-001 is a novel epigenetic modulator with potential radiosensitizing activity. It inhibits glucose 6-phosphate dehydrogenase(G6PD) in human tumor cells, binds hemoglobin and drives RBC-mediated redox reactions under hypoxia. RRx-001 triggers apoptosis and exhibits anticancer activity.
Cell Mol Immunol, 2021, 18(6):1425-1436
Cancer Lett, 2021, 521:29-38
Cancer Lett, 2021, 521:29-38
S8432 Troglitazone (CS-045) Troglitazone (Rezulin, Romglizone, Prelay, CS045, Romozin) is a potent agonist for the peroxisome proliferator-activated receptor-(PPAR) that is a ligand activated transcription factor regulating cell differentiation and growth. Troglitazone induces autophagy, apoptosis and necroptosis in bladder cancer cells. Troglitazone prevents RSL3-induced ferroptosis and lipid peroxidation in Pfa1 cells.
Free Radic Biol Med, 2021, 163:234-242
Biomed Pharmacother, 2020, 132:110741
Nat Commun, 2019, 11;10(1):4621
S8446 Importazole Importazole is a small molecule inhibitor of the transport receptor importin-β (Karyopherin beta) specifically blocking importin-β-mediated nuclear import. Importazole induces apoptosis and inhibits tumor growth.
J Virol, 2021, JVI0148121
Oncogene, 2019, 38(24):4700-4714
Sci Rep, 2019, 9(1):15728
S8495 WT161 WT161 is a potent, selective, and bioavailable HDAC6 inhibitor with IC50 values of 0.4 nM, 8.35 nM and 15.4 nM for HDAC6, HDAC1 and HDAC2, respectively; shown to have >100-fold selectivity over other HDACs. WT161 induces apoptosis.
Nat Metab, 2021, 3(1):75-89
S8523 GSK2256098 GSK2256098 is a potent, selective, reversible, and ATP competitive FAK kinase inhibitor with apparent Ki of 0.4 nM. GSK2256098 inhibits cancer cell growth and induces apoptosis.
Biomaterials, 2021, 279:121235
Int J Mol Sci, 2021, 22(2)E752
J Neurosci Methods, 2021, 356:109141
S8543 ARN-3236 ARN-3236 is a potent, orally available and selective inhibitor of salt-inducible kinase 2 (SIK2) with IC50 of <1 nM, 21.63 nM and 6.63 nM for SIK2, SIK1 and SIK3, respectively. ARN-3236 induces apoptosis in cancer cells.
S8591 FX1 FX1 is a selective BCL6 BTB inhibitor with an IC50 value of 35 μM in reporter assays. FX1 shows great selectivity against a panel of 50 different kinases. 10 μM FX1 fails to significantly inhibit of any of these kinases. FX1 induces apoptosis.
Nat Immunol, 2021, 22(6):757-768
Invest New Drugs, 2021, 10.1007/s10637-021-01196-1
Blood Adv, 2021, bloodadvances.2021005682
S8615 Sodium dichloroacetate (DCA) Sodium dichloroacetate (DCA, Dichloroacetic acid, bichloroacetic acid, BCA), a specific inhibitor of pyruvate dehydrogenase kinase (PDK) with IC50 values of 183 and 80 μM for PDK2 and PDK4 respectively, has been shown to derepress Na+-K+-2Cl- cotransporter and a mitochondrial potassium-ion channel axis. Sodium dichloroacetate increases reactive oxygen species (ROS) generation, triggers apoptosis in cancer cells, and inhibits tumor growth.
Mol Oncol, 2022, 16(1):219-249
J Exp Clin Cancer Res, 2021, 40(1):87
Cancer Sci, 2021, 10.1111/cas.15055
S8663 Takinib (EDHS-206) Takinib (EDHS-206) is a potent and selective TAK1 inhibitor with an IC50 of 9.5 nM, more than 1.5 log more potent than the second and third ranked targets, IRAK4 (120 nM) and IRAK1 (390 nM), respectively. Takinib induces apoptosis.
ACS Pharmacol Transl Sci, 2021, 4(4):1449-1461
bioRxiv, 2021, 10.1101/2021.01.13.426403
Cell Rep, 2020, 33(1):108221
S8722 Samuraciclib (ICEC0942) Samuraciclib (ICEC0942, CT7001) is a new, orally bioavailable CDK7 inhibitor with an IC50 of 40nM. The IC50 values for CDK1, CDK2, CDK5 and CDK9 were 45-, 15-, 230- and 30-fold higher. ICEC0942 (CT7001) promotes cell cycle arrest and apoptosis.
Clin Cancer Res, 2021, 10.1158/1078-0432.CCR-20-3458
S8760 Iberdomide (CC220) Iberdomide (CC-220) is a novel oral immunomodulatory compound that targets cereblon, part of the CRL4CRBN E3 ubiquitin ligase complex, with an IC50 of 60 nM in a competitive TR-FRET assay. Iberdomide (CC-220) induces apoptosis with antitumor and immunostimulatory activities.
Mol Cancer Ther, 2021, 10.1158/1535-7163.MCT-20-0831
Hemasphere, 2021, 5(7):e602
S8762 dBET6 dBET6 is a highly cell-permeable PROTAC degrader of BET bromodomains with an IC50 of 14 nM for BRD4 binding. dBET6 also induces c-MYC downregulation and apoptosis.
Sci Adv, 2021, 7(23)eabg4126
Bioorg Chem, 2021, 115:105238
bioRxiv, 2021, 2021.01.19.427194
S8808 DC661 DC661 is capable of deacidifying the lysosome and inhibiting autophagy significantly better than hydroxychloroquine (HCQ). DC661 induces apoptosis.
Biomed Pharmacother, 2022, 145:112432
Nature, 2021, 10.1038/s41586-021-04204-9
Cell Death Dis, 2021, 12(3):239
S8820 Unesbulin (PTC596) Unesbulin (PTC596) is a second-generation BMI-1 inhibitor that accelerates BMI-1 degradation. PTC596 downregulates MCL-1 and induces p53-independent mitochondrial apoptosis. IC50 values at 72 hours ranged from 68 to 340 nM in mantle cell lymphoma (MCL) cell lines.
Cell Death Dis, 2021, 12(5):495
Int J Mol Sci, 2021, 22(18)10107
S8961 Alobresib (GS-5829) Alobresib (GS-5829) is a novel BET inhibitor that represents a highly effective therapeutics agent against recurrent/chemotherapy-resistant USC-overexpressing c-Myc. Alobresib (GS-5829) inhibits CLL cell proliferation and induces leukemia cell apoptosis through deregulation of key signaling pathways, such as BLK, AKT, ERK1/2, and MYC. Alobresib (GS-5829) also inhibits NF-κB signaling.
S8965 BO-264 BO-264 is a potent and orally active inhibitor of transforming acidic coiled-coil 3 (TACC3) with IC50 of 188 nM and Kd of 1.5 nM. BO-264 specifically blocks the function of FGFR3-TACC3 fusion protein. BO-264 induces SAC-dependent mitotic arrest, apoptosis and DNA damage with antitumor activities.
S8981 NVP-2 NVP-2, a potent, selective, non-neurotoxic and ATP-competitive cyclin dependent kinase 9 (CDK9) inhibitor with IC50 of 0.514 nM for CDK9/CycT activity and induces cell apoptosis.
S8988 Rhosin hydrochloride Rhosin (G04) hydrochloride (HCl) is a potent, specific inhibitor of RhoA subfamily Rho GTPases with Kd of ~ 0.4 uM. Rhosin hydrochloride induces cell apoptosis.
S9054 Pectolinarin Pectolinarin is a major compound in Cirsium setidens with anti-inflammatory activity. Pectolinarin inhibits secretion of IL-6 and IL-8, as well as the production of PGE2 and NO. Pectolinarin induces apoptosis via inactivation of the PI3K/Akt pathway.
S9141 Berbamine Berbamine (BA), a traditional Chinese medicines extracted from Berberis amurensis (xiaoboan), is a novel inhibitor of bcr/abl fusion gene with potent anti-leukemia activity and also an inhibitor of NF-κB. Berbamine (BA) induces apoptosis in human myeloma cells and inhibits the growth of cancer cells by targeting Ca²⁺/calmodulin-dependent protein kinase II (CaMKII).
Onco Targets Ther, 2019, 12:11437-11451
S9190 Oroxin B Oroxin B (Hypocretin-2), one of flavonoids isolated from traditional Chinese herbal medicine Oroxylum indicum (L.) Vent, selectively induces tumor-suppressive ER stress in malignant lymphoma cells and has antioxidant activity. Oroxin B significantly inhibits proliferation and induce apoptosis, which may be strongly associated with the inhibiting COX-2/VEGF and PTEN/PI3K/AKT signaling pathway in SMMC-7721 cells, Oroxin B potentially be used as a novel therapeutic agent for liver cancer.COX-2, VEGF, PI3K, and p-AKT expression levels are downregulated, while PTEN is upregulated after Oroxin B treatment.
Theranostics, 2022, 12(2):910-928
J Cancer, 2021, 12(7):2140-2150
S9602 9-ing-41 9-ING-41 is a potent inhibitor of glycogen synthase kinase-3 (GSK-3) with antitumor activity. 9-ING-41 induces apoptosis and cell cycle arrest at prophase by targeting centrosomes and microtubule-bound GSK3β.
S9604 IM156 IM156 (HL156A), a metformin derivative, is a potent activator of AMPK that increases AMPK phosphorylation. IM156 blocks oxidative phosphorylation (OXPHOS) through the inhibition of complex I and increases apoptosis. IM156 ameliorates various types of fibrosis and inhibits tumors.
S9634 Phenoxodiol (Haginin E) Phenoxodiol (Haginin E, Idronoxil, Dehydroequol, NV 06, PXD) is an isoflavone analog with antineoplastic activity that activates the caspase system, inhibits XIAP (X-linked inhibitor of apoptosis), and disrupts FLICE inhibitory protein (FLIP) expression, resulting in tumor cell apoptosis. Phenoxodiol also inhibits DNA topoisomerase II.
Anticancer Res, 2018, 38(10):5709-5716
S9665 Motixafortide (BL-8040) Motixafortide (BL-8040, BKT140, TF 14016, 4-fluorobenzoyl, 4F-benzoyl-TN14003, T140) is an antagonist of CXCR4 with IC50 of ~1 nM. BL-8040 induces the apoptosis of AML blasts by down-regulating ERK, BCL-2, MCL-1 and cyclin-D1 via altered miR-15a/16-1 expression.
S9698 Ezatiostat Ezatiostat (TER199, TLK199, Telintra), a tripeptide analog of glutathione, is a peptidomimetic inhibitor of Glutathione S-transferase P1-1 (GSTP1-1). Ezatiostat activates c-Jun NH2 terminal kinase (JNK1) and ERK1/ERK2 and induces apoptosis.
S9700 Tapinarof Tapinarof (GSK2894512, Benvitimod, WBI 1001, DHPS, DMVT 505) is a natural agonist of aryl hydrocarbon receptor (AhR) and induces nuclear translocation of AhR in immortalized keratinocytes (HaCaT) with EC50 of 0.16 nM. Tapinarof induces cellular apoptosis in CD4+ T cells in a dosedependent manner with IC50 of 5.2 μM.
S9721 ASLAN003

ASLAN003 (LAS 186323) is a potent and orally active inhibitor of DHODH (Dihydroorotate dehydrogenase) with IC50 of 35 nM for human DHODH enzyme activity. ASLAN003 impairs protein synthesis and induces the differentiation and apoptosis transcriptional program in acute myeloid leukemia (AML) cells via activation of AP-1 transcription factors.

bioRxiv, 2021, 10.1101/2021.06.28.450163
bioRxiv, 2021, 10.1101/2021.06.28.450163
S9785 Fatostatin

Fatostatin (125B11), a diarylthiazole derivative, is a specific inhibitor of Sterol regulatory element binding proteins (SREBPs) activation. Fatostatin binds to SCAP (SREBP cleavage-activating protein), and inhibits the ER-Golgi translocation of SREBPs. Fatostatin suppresses growth and enhances apoptosis in cancer cells.

EMBO Rep, 2021, e52537
Reproduction, 2021, 162(6):397-410
S5973New Methylprednisolone Acetate Methylprednisolone (NSC-19987, Medrol) acetate is a synthetic glucocorticoid receptor agonist, used to achieve prompt suppression of inflammation. Methylprednisolone activates ACE2 and reduces IL-6 levels, thus improves severe or critical COVID-19. Methylprednisolone markedly reduces autophagy and apoptosis.
S1204 Melatonin (NSC 113928) Melatonin (NSC 113928, NSC 56423, N-Acetyl-5-methoxytryptamine) is a MT receptor agonist, used as a dietary supplement. Melatonin is a selective ATF-6 inhibitor and downregulates COX-2. Melatonin enhances mitophagy and regulates the homeostasis of apoptosis and autophagy.
Cell Chem Biol, 2021, S2451-9456(21)00442-6
Int J Mol Sci, 2021, 22(11)5649
Int Immunopharmacol, 2021, 96:107787
S6889 Monomethyl Fumarate Monomethyl Fumarate (MMF, Monomethylfumarate, Fumaric acid monomethyl ester, Methyl hydrogen fumarate), the active metabolite of the psoriasis drug Fumaderm, is a potent GPR109A agonist. Monomethyl Fumarate prevents major dysfunctions associated with neurodegenerative diseases: oxidative stress, mitochondrial dysfunction, apoptosis and autophagy.
Aging (Albany NY), 2021, 13(13):17097-17117
S7307 GSK2606414 GSK2606414 is an orally available, potent, and selective PERK inhibitor with IC50 of 0.4 nM, displaying at least 100-fold selectivity over the other EIF2AKs assayed. GSK2606414 impairs GANT-61 induced autophagy in NB cells with MYCN amplification. GSK2606414 exacerbates ER stress-induced apoptosis in HCT116 cells while reduces the apoptosis in SIL1 KD HeLa cells.
EMBO Mol Med, 2021, e14502
Autophagy, 2021, 1-21
Free Radic Biol Med, 2021, S0891-5849(21)00773-5
S7686 ML141 ML141 (CID-2950007) is demonstrated to be a potent, selective and reversible non-competitive inhibitor of Cdc42 GTPase suitable for in vitro assays, with IC50 of 200 nM and selectivity against other members of the Rho family of GTPases (Rac1, Rab2, Rab7). ML141 is associated with an increase in p38 activation and may induce p38-dependent apoptosis/senescence. ML141 also protects neuroblastoma cells from metformin-induced apoptosis.
Cell Rep, 2021, 36(1):109254
FASEB J, 2021, 35(5):e21598
Sci Rep, 2021, 11(1):8168
E0213New Bruceine D

Bruceine D, isolated from Brucea javanica (L.) Merr. (Simaroubaceae), shows antineoplastic properties in various human cancers including pancreas, breast, lung, blood, bone, and liver. Bruceine D induces apoptosis in human chronic myeloid leukemia K562 cells via mitochondrial pathway.

E0216New Hinokiflavone

Hinokiflavone, isolated from Selaginella P. Beauv, Juniperus phoenicea and Rhus succedanea, possesses excellent pharmacological activities, including anti-inflammatory, antioxidant and antitumor activity. Hinokiflavone induces apoptosis and inhibits migration of breast cancer cells via EMT signalling pathway.

E0222New Glaucocalyxin A

Glaucocalyxin A is a biologically active ent-kauranoid diterpenoid isolated from Rabdosia japonica var. glaucocalyx with antitumor and anti-inflammatory activity. Glaucocalyxin A induces G2/M cell cycle arrest and apoptosis through the PI3K/Akt pathway in human bladder cancer cells.

E0225New Licochalcone B

Licochalcone B (Lico B), extracted from Glycyrrhiza uralensis Fisch, induces the cell cycle arrest and apoptosis in human hepatoma cell HepG2. Licochalcone B specifically inhibits the NLRP3 inflammasome by disrupting NEK7‐NLRP3 interaction.

E0020New Lupenone Lupenone (Lup-20(29)-en-3-one, lupeone) is an isolated compound exhibiting anti-oxidative, anti-inflammation, and anti-diabetic activities. Lupenone can protect SH-SY5y cells against METH-induced neuronal apoptosis through the PI3K/Akt pathway.
E0129New Oxysophocarpine Oxysophocarpine (OSC) is an alkaloid extracted from Sophora alopecuroides. Oxysophocarpine inhibits the growth and metastasis of oral squamous cell carcinoma (OSCC) by targeting the Nrf2/HO-1 axis. OSC protects cells against apoptosis and inflammatory responses and compromised miR-155 activity by attenuating MAPK and NF-κB pathways.
E0212New Cornuside

Cornuside is a bisiridoid glucoside compound isolated from the fruit of Cornus officinalis SIEB. et ZUCC. Cornuside suppresses lipopolysaccharide-induced inflammatory mediators by inhibiting NF-κB activation in RAW 264.7 macrophages. Cornuside attenuates apoptosis in rat cortical neurons.

S0231 NSC15364 NSC 15364 (compound 59) is an inhibitor that directly interacts with VDAC1 and prevents VDAC1 oligomerization, concomitant with an inhibition of apoptosis.
S0411 BAM 15 BAM 15 is a novel mitochondrial protonophore uncoupler capable of protecting mammals from acute renal ischemic-reperfusion injury and cold-induced microtubule damage. BAM 15 is also a potent AMPK activator. BAM 15 attenuates transportation-induced apoptosis in iPS-differentiated retinal tissue.
Neuroscience, 2012, 223:238-45
S0539 BTZO-1 BTZO-1 binds to macrophage migration inhibitory factor (MIF) with Kd of 68.6 nM. BTZO-1 activats antioxidant response element (ARE)-mediated gene expression and suppresses oxidative stress-induced cardiomyocyte apoptosis in vitro.
S0947 Cafestol Cafestol is a natural diterpenes extracted from coffee beans. Cafestol induces apoptosis and regulates a variety of inflammatory mediators to reduce inflammation. Cafestol inhibits PI3K/Akt pathway. Cafestol also can reduce the production of ROS in the leukemia cell line HL60.
S1077 SB202190 (FHPI) SB202190 (FHPI) is a potent p38 MAPK inhibitor targeting p38α/β with IC50 of 50 nM/100 nM in cell-free assays, sometimes used instead of SB 203580 to investigate potential roles for SAPK2a/p38 in vivo. SB202190 inhibits endothelial cell apoptosis via induction of autophagy and heme oxygenase-1. SB202190 significantly suppresses Erastin‐dependent ferroptosis.
Nature, 2021, 600(7888):314-318
Immunity, 2021, S1074-7613(21)00210-7
Nat Commun, 2021, 12(1):6941
S1132 3-Aminobenzamide 3-Aminobenzamide (3-ABA , 3-Amino Benzamide, 3-AB) is a potent inhibitor of Poly(ADP-ribose)polymerase (PARP) and inhibits cell apoptosis after SCI (Spinal Cord Injury) in caspase-independent way.
Cell Death Discov, 2021, 7(1):181
Acta Pharm Sin B, 2019, 9(4):782-793
J Cell Biochem, 2017, 118(11):3943-3952
S1386 Nafamostat mesilate (FUT-175) Nafamostat mesilate (FUT-175) is a synthetic serine protease inhibitor, used as an anticoagulant during hemodialysis. Nafamostat mesylate blocks activation of SARS-CoV-2 and is investigated as a new treatment option for COVID-19. Nafamostat Mesilate attenuates inflammation and apoptosis.
bioRxiv, 2021, 2021.03.31.437960
EMBO J, 2020, e2020106057
bioRxiv, 2020, 2020.10.02.324228
S1733 Methylprednisolone (NSC-19987) Methylprednisolone (NSC-19987) is a synthetic glucocorticoid receptor agonist, used to achieve prompt suppression of inflammation. Methylprednisolone activates ACE2 and reduces IL-6 levels, thus improves severe or critical COVID-19. Methylprednisolone markedly reduces autophagy and apoptosis.
Drug Test Anal, 2020, 10.1002/dta.2917
Nat Med, 2017, 23(4):424-428
Trop J Pharm Res, 2014, 13 (1): 53-59
S2872 GW5074 GW5074 is a potent and selective c-Raf inhibitor with IC50 of 9 nM, no effect on the activities of JNK1/2/3, MEK1, MKK6/7, CDK1/2, c-Src, p38 MAP, VEGFR2 or c-Fms is noted. GW5074 inhibits LK-induced apoptosis.
Cell Res, 2021, 10.1038/s41422-021-00532-7
Antibiotics (Basel), 2021, 10(10)1223
J Neurosci, 2020, 40(34):6522-6535
S3236 Mesaconitine Mesaconitine, one of the aconite alkaloids in Aconiti tuber, increases the [Ca2+]i level in endothelial cells by influx of Ca2+ from extracellular spaces.
S3267 Kaempferol-3-O-rutinoside Kaempferol-3-O-rutinoside (Nicotiflorin, Nikotoflorin, Kaempferol 3-O-β-rutinoside), a flavonoid extracted from Carthamus tinctorius, alters the shape and structure of injured neurons, decreases the number of apoptotic cells, down-regulates expression of p-JAK2, p-STAT3, caspase-3, and Bax and decreases Bax immunoredactivity, and increases Bcl-2 protein expression and immunoreactivity.
S3269 Acetylcorynoline Acetylcorynoline, a major alkaloid component derived from Corydalis bungeana which is a traditional Chinese medical herb, shows anti-inflammatory properties. Acetylcorynoline may decrease egl-1 expression to suppress apoptosis pathways and increase rpn5 expression to enhance the activity of proteasomes.
S3275 Senkyunolide I Senkyunolide I (SEI, SENI) is an orally active compound isolated from Ligusticum chuanxiong with analgesic, anti-migraine, neuroprotective, anti-oxidation and anti-apoptosis activities. Senkyunolide I (SEI, SENI) up-regulates the phosphorylation of Erk1/2 and induces Nrf2 nuclear translocation with enhanced HO-1 and NQO1 expressions. Senkyunolide I (SEI, SENI) promotes the ratio of Bcl-2/Bax and inhibits the expressions of cleaved caspase 3 and caspase 9.
Cell Commun Signal, 2021, 19(1):115
S3294 Demethyl-Coclaurine Demethyl-Coclaurine (Higenamine, Norcoclaurine), the key component of the Chinese herb aconite root, is a beta-2 adrenergic receptor (β2-AR) agonist. Demethyl-Coclaurine stimulates AKT phosphorylation and requires PI3K activation for the anti-apoptotic effect in cardiomyocytes.
S3576New TVB-3166 TVB-3166 is an orally-available, reversible, potent and selective inhibitor of fatty acid synthase (FASN) with IC50 of 0.042 μM in an in vitro biochemical assay. TVB-3166 induces apoptosis, and inhibits in-vivo xenograft tumor growth.
S4484New Trametinib DMSO solvate Trametinib (GSK1120212, JTP-74057, Mekinist) DMSO solvate is a highly specific and potent MEK1/2 inhibitor with IC50 of 0.92 nM/1.8 nM in cell-free assay. Trametinib activates autophagy and induces apoptosis.
S4513New RGD peptide (GRGDNP) RGD peptide (GRGDNP) is an inhibitor of binding of integrins to the extracellular matrixs. RGD peptide (GRGDNP) induces apoptosis presumably through direct activation of caspase-3.
S5971New Pemetrexed Pemetrexed (LY231514, Alimta) is a novel antifolate and antimetabolite for thymidylate synthase (TS), dihydrofolate reductase (DHFR) and glycinamide ribonucleotide formyltransferase (GARFT) with Ki of 1.3 nM, 7.2 nM and 65 nM in cell-free assays, respectively. Pemetrexed induces autophagy and apoptosis.
J Exp Clin Cancer Res, 2021, 40(1):344
Br J Cancer, 2021, 10.1038/s41416-021-01441-7
Front Oncol, 2021, 11:711043
S6812New Z-Guggulsterone Z-Guggulsterone, a constituent of Ayurvedic medicinal plant Commiphora mukul, inhibits angiogenesis in vitro and in vivo. Z-Guggulsterone exhibits anti-inflammatory effects in microglia. Z-Guggulsterone induces apoptosis in gastric cancer cells through the intrinsic mitochondria-dependent pathway.
S7033 GSK2656157 GSK2656157 is an ATP-competitive and highly selective inhibitor of PERK with IC50 of 0.9 nM in a cell-free assay, 500-fold greater against a panel of 300 kinases. GSK2656157 decreases apoptosis and inhibits excessive autophagy.
Neurobiol Dis, 2021, 156:105407
Cell Death Dis, 2020, 11(2):125
Sci Rep, 2020, 10(1):9666
S8037 Necrostatin-1 Necrostatin-1 (Nec-1) is a specific RIP1 (RIPK1) inhibitor and inhibits TNF-α-induced necroptosis with EC50 of 490 nM in 293T cells. Necrostatin-1 also blocks IDO and suppresses autophagy and apoptosis.
Cells, 2022, 11(1)134
Int J Mol Sci, 2022, 23(1)506
Cell, 2021, S0092-8674(21)00885-0
S8632 Chk2 Inhibitor II (BML-277) Chk2 Inhibitor II (BML-277) is an ATP-competitive inhibitor of Chk2 with IC50 of 15 nM. It is 1000-fold more selective toward Chk2 serine/threonine kinase than for Chk1 and Cdk1/B kinases. Chk2 Inhibitor II (BML-277) dose dependently protects human CD4(+) and CD8(+) T-cells from apoptosis due to ionizing radiation.
Mol Cancer Res, 2021, 10.1158/1541-7786.MCR-20-0791
DNA Repair (Amst), 2021, 110:103264
mBio, 2020, 11(3):e01190-20
S8974 GSK2795039 GSK2795039 is an inhibitor of NADPH oxidase 2 (NOX2) with pIC50 of 6.57 for NOX2-mediated activation of HRP/Amplex Red. GSK2795039 inhibits reactive oxygen species (ROS) production, NADPH consumption and reduces apoptosis.
S9631New Puromycin aminonucleoside Puromycin aminonucleoside (NSC 3056, PAN, Stylomycin aminonucleoside, ARDMA, SAN), the aminonucleoside portion of the antibiotic puromycin, is a reversible inhibitor of dipeptidyl-peptidase II and cytosol alanyl aminopeptidase that induces apoptosis in mesangial cells (MCs) accompanied by declined cell viability and enhanced inflammatory response.
S9668 PKR-IN-C16 PKR-IN-C16 (imoxin, C16, Imidazolo-oxindole PKR inhibitor C16) is a specific inhibitor of RNA-dependent protein kinase (PKR, Protein Kinase R, EIF2AK2). PKR-IN-C16 prevents apoptosis and IL-1β production in an acute excitotoxic rat model with a neuroinflammatory component.
Cell Chem Biol, 2021, S2451-9456(21)00303-2
Pulm Circ, 2021, 11(4):20458940211046156
S9724New SZL P1-41 SZL P1-41 (compound #25) is a specific inhibitor of S-phase kinase-associated protein 2 (Skp2) that indeed binds to Skp2, prevents Skp2-Skp1 interaction and inhibits Skp2 SCF E3 ligase activity, which consequently suppresses survival of cancer cells and cancer stem cells. SZL P1-41 causes higher apoptosis rates in cancer cells.
S9805New WM-3835 WM-3835 is a novel and high-specific small molecule Lysine Acetyltransferase 7 (KAT7, MYST2, HBO1) inhibitor, able to potently suppressed OS cell proliferation and migration, and leads to apoptosis activation.
S0056 (E/Z)-BCI (E/Z)-BCI (BCI, NSC 150117) is an inhibitor of dual specific phosphatase 1/6 (DUSP1/DUSP6) and mitogen-activated protein kinase with EC50 of 13.3 μM and 8.0 μM for DUSP6 and DUSP1 in cells, respectively. (E)-BCI induces apoptosis via generation of reactive oxygen species (ROS) and activation of intrinsic mitochondrial pathway in H1299 lung cancer cells.
S0103 ML327 ML327 is an isoxazole compound that blocks MYC expression and tumor formation in neuroblastoma. ML327 also restores E-cadherin expression with In-Cell Western EC50 of 1.0 μM. ML327 induces apoptosis.
S0149 C-DIM5 C-DIM5 (DIM-C-pPhOCH3) is an agonist of Nur77 (Nerve growth factor-induced Bα (NGFI-Bα)/nuclear receptor 4A1 (NR4A1)) which is an orphan nuclear receptor. C-DIM5 (DIM-C-pPhOCH3) decreases survival and induces apoptosis in RKO colon cancer cells.
S0278 SU5614 SU5614 (Chloro-SU5416, Chloro-Semaxanib) is a small molecule receptor tyrosine kinases (RTK) inhibitor of VEGFR-2, c-kit, and both wild-type and mutant FLT3. SU5614 reduces cell proliferation and induces apoptosis.
Adv Sci (Weinh), 2021, e2101848
S0354 Alsterpaullone Alsterpaullone (Alp, 9-Nitropaullone, NSC 705701) is a potent inhibitor of CDK with IC50 of 35 nM, 15 nM, 200 nM and 40 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E and CDK5/p35, respectively. Alsterpaullone also acts as a potent inhibitor of glycogen synthase kinase-3 (GSK-3) with IC50 of both 4 nM for GSK-3α and GSK-3β. Alsterpaullone induces apoptosis by activation of caspase-9. Alsterpaullone has antitumor activity and possesses potential for the treatment of neurodegenerative and proliferative disorders.
S0407 XCT790 XCT-790 (Compound 12) is a potent and selective inverse agonist for estrogen-related receptor α (ERRα) with IC50 of 0.37 μM. XCT-790 (Compound 12) is inactive against ERRγ and the estrogen receptors ERα and ERβ. XCT-790 (Compound 12) significantly inhibits in vivo tumor growth and angiogenesis, and induces apoptosis.
S0444 Indibulin Indibulin (ZIO 301, D 24851, Zybulin) is an orally applied inhibitor of tubulin assembly with potent anticancer activity. Indibulin induces mitotic arrest and apoptosis.
Bioorg Med Chem, 2020, 28(20):115712
S0445 SC-43 SC-43, a sorafenib derivative, is an agonist of Src-homology protein tyrosine phosphatase-1 (SHP-1/PTPN6) and reduces liver fibrosis. SC-43 reduces p-STAT3 and induces apoptosis with anti-tumor activity.
S0709 Tubastatin A TFA Tubastatin A TFA (Tubastatin A trifluoroacetate salt) is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay. It is selective against all the other isozymes (1000-fold) except HDAC8 (57-fold). Tubastatin A promotes autophagy and increases apoptosis.
S0765 MAZ51 MAZ51 is a potent and selective inhibitor of vascular endothelial growth factor receptor (VEGFR)-3 (Flt-4) tyrosine kinase. MAZ51 induces cell rounding and G2/M cell cycle arrest in glioma cells through phosphorylation of Akt/GSK3β and activation of RhoA. MAZ51 inhibits the proliferation and induces the apoptosis of a variety of non-VEGFR-3-expressing tumor cell lines.
S0817 SKI-V SKI V is a noncompetitive and potent inhibitor of non-lipid sphingosine kinase with IC50 of 2 μM for GST-hSK. SKI-V also inhibits PI3K with IC50 of 6 μM for hPI3k. SKI-V decreases formation of the mitogenic second messenger sphingosine-1-phosphate (S1P) and induces apoptosis with antitumor activity.
S0884 RA-9 RA-9 is a cell-permeable, potent and selective inhibitor of proteasome-associated deubiquitinating enzymes (DUBs) with favorable toxicity profile and anticancer activity. RA-9 selectively induces apoptosis in ovarian cancer cell lines.
S0913 4',5,7-Trimethoxyflavone 4',5,7-Trimethoxyflavone (5,​7,​4'-​Trimethoxyflavone, TMF) is a flavonoid isolated from Kaempferia parviflora (KP) that induces apoptosis. 4',5,7-Trimethoxyflavone increases sub-G1 phase, DNA fragmentation, annexin-V/PI staining and Bax/Bcl-xL ratio, activates caspase-3 and degrades poly (ADP-ribose) polymerase (PARP) protein.
S0918 Ginkgolic acid C17:1 Ginkgolic acid C17:1 (GAC 17:1) inhibits constitutive activation of STAT3 through the abrogation of upstream JAK2 and Src. Ginkgolic acid C17:1 can induce the substantial expression of PTEN and SHP-1. Ginkgolic acid C17:1 induces apoptosis of tumor cells.
S0931 Jaceosidin Jaceosidin, a flavonoid isolated from Artemisia vestita, possesses anti-tumor and anti-proliferative activities in many cancer cells. Jaceosidin induces apoptosis, activates Bax and down-regulates Mcl-1 and c-FLIP expression. Jaceosidin inhibits COX-2 expression and NF-κB activation.
S0949 Cucurbitacin IIb Cucurbitacin IIb (CuIIb, Dihydrocucurbitacin F, 25-deacetyl hemslecin A) inhibits phosphorylation of STAT3, JNK and Erk1/2, enhances the phosphorylation of IκB and NF-κB, blocks nuclear translocation of NF-κB and decreases mRNA levels of IκBα and TNF-α. Cucurbitacin IIb exhibits anti-inflammatory activity and induces apoptosis. Cucurbitacin IIb is isolated from Hemsleya amabilis.
S1002 ABT-737 ABT-737 is a BH3 mimetic inhibitor of Bcl-xL, Bcl-2 and Bcl-w with EC50 of 78.7 nM, 30.3 nM and 197.8 nM in cell-free assays, respectively; no inhibition observed against Mcl-1, Bcl-B or Bfl-1. ABT-737 induces mitochondrial pathway apoptosis and mitophagy. Phase 2.
ACS Appl Mater Interfaces, 2022, 10.1021/acsami.1c22138
Science, 2021, 371(6535)eabc5386
Cell Death Dis, 2021, 12(8):736
S1003 Linifanib (ABT-869) Linifanib (ABT-869, AL39324, RG3635) is a novel, potent ATP-competitive VEGFR/PDGFR inhibitor for KDR, CSF-1R, Flt-1/3 and PDGFRβ with IC50 of 4 nM, 3 nM, 3 nM/4 nM and 66 nM respectively, mostly effective in mutant kinase-dependent cancer cells (i.e. FLT3). Linifanib (ABT-869) induces autophagy and apoptosis. Phase 3.
Cancer Lett, 2021, 507:80-88
Hum Cell, 2021, 34(6):1911-1918
Hum Cell, 2021, 10.1007/s13577-021-00639-4
S1004 Veliparib (ABT-888) Veliparib (ABT-888, NSC 737664) is a potent inhibitor of PARP1 and PARP2 with Ki of 5.2 nM and 2.9 nM in cell-free assays, respectively. It is inactive to SIRT2. Veliparib increases autophagy and apoptosis. Phase 3.
Cell, 2022, 185(1):169-183.e19
Transl Oncol, 2022, 15(1):101283
Sci Transl Med, 2021, 13(592)eabc7211
S1008 Selumetinib (AZD6244) Selumetinib (AZD6244, ARRY-142886) is a potent, highly selective MEK inhibitor with IC50 of 14 nM for MEK1 and Kd value of 530 nM for MEK2. It also inhibits ERK1/2 phosphorylation with IC50 of 10 nM, no inhibition to p38α, MKK6, EGFR, ErbB2, ERK2, B-Raf, etc. Selumetinib suppresses cell proliferation, migration and trigger apoptosis. Phase 3.
Proc Natl Acad Sci U S A, 2022, 119(3)e2114134119
Nat Cell Biol, 2021, 23(4):377-390
J Extracell Vesicles, 2021, 10(8):e12091
S1020 PD184352 (CI-1040) PD184352 (CI-1040) is an ATP non-competitive MEK1/2 inhibitor with IC50 of 17 nM in cell-based assays, 100-fold more selective for MEK1/2 than MEK5. PD184352 (CI-1040) selectively induces apoptosis. Phase 2.
Proc Natl Acad Sci U S A, 2022, 119(3)e2114134119
Cell Syst, 2021, S2405-4712(21)00111-3
Elife, 2021, 10e66596
S1021 Dasatinib (BMS-354825) Dasatinib (BMS-354825) is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM in cell-free assays, respectively. Dasatinib induces autophagy and apoptosis with anti-tumor activity.
ACS Appl Mater Interfaces, 2022, 10.1021/acsami.1c22138
J Immunol, 2022, ji2100400
Nat Immunol, 2021, 10.1038/s41590-021-00948-8
S1025 Gefitinib (ZD1839) Gefitinib (ZD-1839, Iressa) is an EGFR inhibitor for Tyr1173, Tyr992, Tyr1173 and Tyr992 in the NR6wtEGFR and NR6W cells with IC50 of 37 nM, 37nM, 26 nM and 57 nM, respectively. Gefitinib promotes autophagy and apoptosis of lung cancer cells via blockade of the PI3K/AKT/mTOR pathway.
Cell Death Dis, 2022, 13(1):41
Cancer Med, 2022, 10.1002/cam4.4504
BMC Pulm Med, 2022, 22(1):27
S1029 Lenalidomide (CC-5013) Lenalidomide (CC-5013) is a TNF-α secretion inhibitor with IC50 of 13 nM in PBMCs. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide promotes cleaved caspase-3 expression and inhibit VEGF expression and induces apoptosis.
Blood Adv, 2022, bloodadvances.2021005772
Adv Sci (Weinh), 2021, e2004846
Sci Adv, 2021, 7(6)eabd6263
S1030 Panobinostat (LBH589) Panobinostat (LBH589, NVP-LBH589) is a novel broad-spectrum HDAC inhibitor with IC50 of 5 nM in a cell-free assay. Panobinostat (LBH589) induces autophagy and apoptosis. Panobinostat effectively disrupts HIV latency in vivo. Phase 3.
Neoplasia, 2022, 24(2):63-75
Nat Med, 2021, 10.1038/s41591-020-01212-6
Cell Stem Cell, 2021, 28(1):48-62.e6
S1038 PI-103 PI-103 is a multi-targeted PI3K inhibitor for p110α/β/δ/γ with IC50 of 2 nM/3 nM/3 nM/15 nM in cell-free assays, less potent to mTOR/DNA-PK with IC50 of 30 nM/23 nM. PI-103 induces apoptosis in murine T-cell Lymphoma.
Adv Healthc Mater, 2021, e2101944
Cell Chem Biol, 2021, S2451-9456(21)00254-3
Neurobiol Dis, 2021, 156:105407
S1040 Sorafenib (BAY 43-9006) tosylate Sorafenib (BAY 43-9006) tosylate is a multikinase inhibitor of Raf-1 and B-Raf with IC50 of 6 nM and 22 nM in cell-free assays, respectively. Sorafenib Tosylate inhibits VEGFR-2, VEGFR-3, PDGFR-β, Flt-3 and c-KIT with IC50 of 90 nM, 20 nM, 57 nM, 59 nM and 68 nM, respectively. Sorafenib Tosylate induces autophagy and apoptosis and activates ferroptosis with anti-tumor activity.
Cell Death Dis, 2022, 13(1):35
Cancer Cell, 2021, S1535-6108(21)00659-0
Leukemia, 2021, 10.1038/s41375-021-01308-z
S1042 Sunitinib (SU11248) malate Sunitinib (SU11248) malate is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM in cell-free assays, and also inhibits c-Kit. Sunitinib Malate effectively inhibits autophosphorylation of Ire1α. Sunitinib Malate increases both death receptor and mitochondrial-dependent apoptosis.
Cancer Cell, 2021, S1535-6108(21)00659-0
Adv Sci (Weinh), 2021, 8(2):2001596
Adv Sci (Weinh), 2021, 8(2):2001596
S1044 Temsirolimus (CCI-779) Temsirolimus (CCI-779, NSC 683864) is a specific mTOR inhibitor with IC50 of 1.76 μM in a cell-free assay. Temsirolimus induces autophagy and apoptosis.
Mol Syst Biol, 2021, 17(8):e10239
Cell Death Dis, 2021, 12(1):108
J Clin Endocrinol Metab, 2021, dgab020
S1046 Vandetanib (ZD6474) Vandetanib (ZD6474) is a potent inhibitor of VEGFR2 with IC50 of 40 nM in a cell-free assay. It also inhibits VEGFR3 and EGFR with IC50 of 110 nM and 500 nM, respectively. Not sensitive to PDGFRβ, Flt1, Tie-2 and FGFR1 with IC50 of 1.1-3.6 μM. No activity against MEK, CDK2, c-Kit, erbB2, FAK, PDK1, Akt and IGF-1R with IC50 above 10 μM. Vandetanib (ZD6474) increases apoptosis and induces autophagy by increasing the level of reactive oxygen species (ROS).
J Clin Endocrinol Metab, 2021, dgab020
Cell Chem Biol, 2021, S2451-9456(21)00303-2
Cancer Discov, 2021, candisc.1201.2020
S1052 Elesclomol (STA-4783) Elesclomol (STA-4783) is a novel potent oxidative stress inducer that elicits pro-apoptosis events among tumor cells. Phase 3.
J Exp Clin Cancer Res, 2021, 40(1):228
Mol Oncol, 2021, 10.1002/1878-0261.13079
Nat Commun, 2020, 15;11(1):2423
S1053 Entinostat (MS-275) Entinostat (MS-275, SNDX-275) strongly inhibits HDAC1 and HDAC3 with IC50 of 0.51 μM and 1.7 μM in cell-free assays, compared with HDACs 4, 6, 8, and 10. Entinostat induces autophagy and apoptosis. Phase 3.
Science, 2021, 372(6537)eaba1786
Nat Chem Biol, 2021, 10.1038/s41589-021-00772-z
Nat Commun, 2021, 12(1):2699
S1065 Pictilisib (GDC-0941) Pictilisib (GDC-0941, RG7321) is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM in cell-free assays, with modest selectivity against p110β (11-fold) and p110γ (25-fold). Pictilisib (GDC-0941) induces autophagy and apoptosis. Phase 2.
Nat Commun, 2022, 13(1):245
Cancer Cell, 2021, S1535-6108(21)00383-4
Cancer Cell, 2021, S1535-6108(21)00492-X
S1069 Luminespib (NVP-AUY922) Luminespib (AUY-922, NVP-AUY922, VER-52296) is a highly potent HSP90 inhibitor for HSP90α/β with IC50 of 13 nM /21 nM in cell-free assays, weaker potency against the HSP90 family members GRP94 and TRAP-1, exhibits the tightest binding of any small-molecule HSP90 ligand. Luminespib (AUY-922, NVP-AUY922) effectively downregulates and destabilizes the IGF-1Rβ protein and results in growth inhibition, autophagy and apoptosis. Phase 2.
Cell Rep, 2021, 34(11):108870
Haematologica, 2021, 10.3324/haematol.2021.278743
Cancers (Basel), 2021, 13(15)3850
S1078 MK-2206 2HCl MK-2206 2HCl is a highly selective inhibitor of Akt1/2/3 with IC50 of 8 nM/12 nM/65 nM in cell-free assays, respectively; no inhibitory activities against 250 other protein kinases observed. MK-2206 2HCl induces autophagy and apoptosis in cancer cells. Phase 2.
Nat Commun, 2022, 13(1):245
Cell Death Dis, 2022, 13(1):44
J Cell Mol Med, 2022, 10.1111/jcmm.17150
S1080 SU11274 SU11274 (PKI-SU11274) is a selective Met (c-Met) inhibitor with IC50 of 10 nM in cell-free assays, no effects on PGDFRβ, EGFR or Tie2. SU11274 induces autophagy, apoptosis and cell cycle arrest.
Cell Rep, 2021, 37(5):109905
Signal Transduct Target Ther, 2021, 6(1):401
Cell Chem Biol, 2021, S2451-9456(21)00303-2
S1105 LY294002 LY294002 (SF 1101, NSC 697286) is the first synthetic molecule known to inhibit PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM, respectively; more stable in solution than Wortmannin, and also blocks autophagosome formation. It not only binds to class I PI3Ks and other PI3K-related kinases, but also to novel targets seemingly unrelated to the PI3K family. LY294002 also inhibits CK2 with IC50 of 98 nM. LY294002 is a non-specific DNA-PKcs inhibitor and activates autophagy and apoptosis.
Immunity, 2022, 55(1):159-173.e9
Microbiol Spectr, 2022, e0188121
Cell Biol Toxicol, 2022, 10.1007/s10565-021-09670-5
S1107 Danusertib (PHA-739358) Danusertib (PHA-739358) is an Aurora kinase inhibitor for Aurora A/B/C with IC50 of 13 nM/79 nM/61 nM in cell-free assays, modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc. Danusertib induces apoptosis, cell cycle arrest, and autophagy. Phase 2.
Cancers (Basel), 2021, 13(6)1205
Life Sci Alliance, 2021, 4(8)e202101019
Mol Cell, 2020, 80(6):1104-1122.e9
S1108 TAE684 (NVP-TAE684) TAE684 (NVP-TAE684) is a potent and selective ALK inhibitor with IC50 of 3 nM in a cell-free assay, 100-fold more sensitive for ALK than InsR. TAE684 (NVP-TAE684) induces cell cycle arrest and apoptosis.
Cereb Cortex, 2021, bhab058
Cell Death Dis, 2021, 12(8):741
Mol Oncol, 2021, 15(8):2011-2025
S1109 BI 2536 BI-2536 is a potent Plk1 inhibitor with IC50 of 0.83 nM in a cell-free assay. BI-2536 inhibits Bromodomain 4 (BRD4) with Kd of 37 nM and potently suppresses c-Myc expression. BI-2536 induces apoptosis and attenuates autophagy. Phase 2.
Science, 2021, 371(6535)eabc5386
Nat Commun, 2021, 12(1):5356
Proc Natl Acad Sci U S A, 2021, 118(34)e2108145118
S1118 XL147 analogue XL147 analogue (SAR245408) is a selective and reversible class I PI3K inhibitor for PI3Kα/δ/γ with IC50 of 39 nM/36 nM/23 nM in cell-free assays, less potent to PI3Kβ. XL147 analogue induces apoptosis. Phase 1/2.
Hum Cell, 2021, 10.1007/s13577-021-00579-z
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Hum Cell, 2021, 34(6):1911-1918
S1119 Cabozantinib (BMS-907351) Cabozantinib (XL184, BMS-907351) is a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM in cell-free assays, respectively. Cabozantinib induces PUMA-dependent apoptosis in colon cancer cells via AKT/GSK-3β/NF-κB signaling pathway.
Sci Adv, 2021, 7(48):eabg9509
Clin Cancer Res, 2021, 27(9):2533-2548
Cancers (Basel), 2021, 13(3)E372
S1120 Everolimus (RAD001) Everolimus (RAD001, SDZ-RAD) is an mTOR inhibitor of FKBP12 with IC50 of 1.6-2.4 nM in a cell-free assay. Everolimus induces cell apoptosis and autophagy and inhibits tumor cells proliferation.
Cold Spring Harb Mol Case Stud, 2022, 8(1)a006140
Cell, 2021, 184(25):6119-6137.e26
Cancer Cell, 2021, S1535-6108(21)00659-0
S1122 Mocetinostat (MGCD0103) Mocetinostat (MGCD0103, MG0103) is a potent HDAC inhibitor with most potency for HDAC1 with IC50 of 0.15 μM in a cell-free assay, 2- to 10- fold selectivity against HDAC2, 3, and 11, and no activity to HDAC4, 5, 6, 7, and 8. Mocetinostat (MGCD0103) induces apoptosis and autophagy. Phase 2.
Cancer Cell, 2021, S1535-6108(20)30662-0
Nat Commun, 2021, 12(1):5056
Cell Rep, 2021, 37(12):110129
S1133 Alisertib (MLN8237) Alisertib (MLN8237) is a selective Aurora A inhibitor with IC50 of 1.2 nM in a cell-free assay. It has >200-fold higher selectivity for Aurora A than Aurora B. Alisertib induces cell cycle arrest, apoptosis and autophagy. Phase 3.
Mol Oncol, 2022, 16(1):219-249
Cancer Cell, 2021, S1535-6108(21)00383-4
Cancer Cell, 2021, S1535-6108(21)00492-X
S1135 Pemetrexed (LY-231514) disodium Pemetrexed (LY-231514) disodium is a novel antifolate and antimetabolite for TS, DHFR and GARFT with Ki of 1.3 nM, 7.2 nM and 65 nM in cell-free assays, respectively. Pemetrexed induces autophagy and apoptosis.
J Exp Clin Cancer Res, 2021, 40(1):344
Br J Cancer, 2021, 10.1038/s41416-021-01441-7
Cell Chem Biol, 2021, S2451-9456(21)00442-6
S1141 Tanespimycin (17-AAG) Tanespimycin (17-AAG, CP127374, NSC-330507, KOS 953) is a potent HSP90 inhibitor with IC50 of 5 nM in a cell-free assay, having a 100-fold higher binding affinity for HSP90 derived from tumour cells than HSP90 from normal cells. Tanespimycin (17-AAG) induces apoptosis, necrosis, autophagy and mitophagy. Phase 3.
ACS Appl Mater Interfaces, 2022, 10.1021/acsami.1c22138
Cell Stem Cell, 2021, S1934-5909(21)00294-0
Mol Cell, 2021, 81(6):1170-1186.e10
S1145 SNS-032 (BMS-387032) SNS-032 (BMS-387032) has firstly been described as a selective inhibitor of CDK2 with IC50 of 48 nM in cell-free assays and is 10- and 20-fold selective over CDK1/CDK4. It is also found to be sensitive to CDK7/9 with IC50 of 62 nM/4 nM, with little effect on CDK6. SNS-032 (BMS-387032) induces apoptosis. Phase 1.
Cancers (Basel), 2021, 13(15)3906
Cell Death Dis, 2021, 12(11):1048
Cells, 2021, 10(3)550
S1156 Capecitabine (RO 09-1978) Capecitabine (RO 09-1978) is a tumor-selective fluoropyrimidine carbamate, which achieves higher intratumoral 5-FU level with lower toxicity than 5-FU. Capecitabine treatment of HCT-15 cells causes condensation of DNA and induces apoptosis.
Adv Sci (Weinh), 2021, e2103360
Hum Cell, 2021, 10.1007/s13577-021-00579-z
Hum Cell, 2021, 10.1007/s13577-021-00639-4
S1159 Ganetespib (STA-9090) Ganetespib (STA-9090) is an HSP90 inhibitor with IC50 of 4 nM in OSA 8 cells, induces apoptosis of OSA cells while normal osteoblasts are not affected; active metabolite of STA-1474. Phase 3.
Nat Commun, 2021, 12(1):5919
Cell Death Dis, 2021, 12(1):126
Cell Death Dis, 2021, 12(1):126
S1181 ENMD-2076 ENMD-2076 has selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold selective for Aurora A than over Aurora B and less potent to RET, SRC, NTRK1/TRKA, CSF1R/FMS, VEGFR2/KDR, FGFR and PDGFRα. ENMD-2076 inhibits the growth of a wide range of human solid tumor and hematopoietic cancer cell lines with IC50 from 0.025 to 0.7 μM, which induces apoptosis and G2/M phase arrest. Phase 2.
Cell, 2021, 184(2):334-351.e20
Sci Adv, 2021, 7(4)eabd7851
J Pediatr Hematol Oncol, 2019, 41(6):e359-e370
S1185 Ritonavir (ABT-538) Ritonavir (ABT-538, A 84538, RTV, Norvir, Norvir Softgel) is a Cytochrome P450 3A and Protease Inhibitor; Also inhibits Cytochrome P450 2D6, P-Glycoprotein and induces Cytochrome P450 2C19, Cytochrome P450 1A2, Cytochrome P450 2C9, Cytochrome P450 2B6 and UDP Glucuronosyltransferases. Ritonavir induces apoptosis.
J Virol, 2022, JVI0173021
mBio, 2021, 12(1)e02754-20
Cell Chem Biol, 2021, S2451-9456(21)00441-4
S1186 BIBR 1532 BIBR 1532 is a potent, selective, non-competitive telomerase inhibitor with IC50 of 100 nM in a cell-free assay. No inhibition of DNA and RNA polymerases, including HIV reverse transcriptase are observed at concentrations vastly exceeding the IC50 for telomerase. BIBR 1532 induces apoptosis in cancer cells.
Med Oncol, 2021, 39(1):12
Neuro Oncol, 2020, noaa207
Oxid Med Cell Longev, 2020, 2020:6946037
S1191 Fulvestrant (ICI-182780) Fulvestrant (ICI-182780, ZD 9238, ZM 182780) is an estrogen receptor (ER) antagonist with IC50 of 0.94 nM in a cell-free assay. Fulvestrant also induces autophagy and apoptosis and has antitumor activity.
Mol Cancer Ther, 2022, 21(1):48-57
Biochim Biophys Acta Gen Subj, 2022, 1866(1):130046
Clin Cancer Res, 2021, 10.1158/1078-0432.CCR-20-2961
S1200 Decitabine (NSC 127716) Decitabine (NSC 127716, Deoxycytidine, Dacogen, 5-aza-2-deoxycytidine, 5-AZA-dC, 5-aza-CdR) is a DNA methyltransferase inhibitor, incorporating into DNA and resulting in hypomethylation of DNA and intra-S-phase arrest of DNA replication. It is used to treat myelodysplastic syndrome (MDS). Decitabine induces cell cycle arrest and apoptosis in various cancer cell lines.
Cancer Cell, 2021, S1535-6108(21)00659-0
Cell Metab, 2021, 33(1):110-127.e5
J Immunother Cancer, 2021, 9(7)e002528
S1208 Doxorubicin (Adriamycin) HCl Doxorubicin (Adriamycin, NSC 123127, DOX, Hydroxydaunorubicin) HCl is an antibiotic agent that inhibits DNA topoisomerase II and induces DNA damage, mitophagy and apoptosis in tumor cells. Doxorubicin reduces basal phosphorylation of AMPK. Doxorubicin is used in the concomitant treatment of HIV-infected patients but is found to be at high risk of HBV reactivation.
J Exp Clin Cancer Res, 2022, 41(1):11
Toxicol Appl Pharmacol, 2022, 435:115834
Oncol Rep, 2022, 47(1)18
S1209 Fluorouracil (5-Fluorouracil, 5-FU) Fluorouracil (5-Fluorouracil, 5-FU, NSC 19893) is a DNA/RNA synthesis inhibitor, which interrupts nucleotide synthetic by inhibiting thymidylate synthase (TS) in tumor cells. Fluorouracil induces apoptosis and can be used in the treatment of HIV.
Oncotarget, 2022, 13:92-104
Cell, 2021, 184(25):6119-6137.e26
Sci Adv, 2021, 7(36):eabh1684
S1218 Clofarabine Clofarabine (Clolar) inhibits the enzymatic activities of ribonucleotide reductase (RNR) (IC50 = 65 nM) and DNA polymerase. Clofarabine induces autophagy and apoptosis.
Hum Cell, 2021, 10.1007/s13577-021-00579-z
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Hum Cell, 2021, 34(6):1911-1918
S1223 Epirubicin (IMI 28) HCl Epirubicin HCl (IMI 28, NSC 256942, 4'-epidoxorubicin), a semisynthetic L-arabino derivative of doxorubicin, is an antineoplastic agent by inhibiting Topoisomerase. Epirubicin induces apoptosis.
Cancer Cell, 2021, S1535-6108(20)30609-7
Cell Rep, 2021, 34(10):108814
Biomolecules, 2021, 11(8)1128
S1225 Etoposide (VP-16) Etoposide (VP-16, VP-16213) is a semisynthetic derivative of podophyllotoxin, which inhibits DNA synthesis via topoisomerase II inhibition activity. Etoposide induces autophagy, mitophagy and apoptosis.
Nature, 2021, 10.1038/s41586-021-04204-9
Nature, 2021, 10.1038/s41586-021-04009-w
Cancer Cell, 2021, S1535-6108(21)00659-0
S1231 Topotecan (NSC609699) HCl Topotecan HCl (NSC609699, Nogitecan, SKFS 104864A) is a topoisomerase I inhibitor for MCF-7 Luc cells and DU-145 Luc cells with IC50 of 13 nM and 2 nM in cell-free assays, respectively. Topotecan HCl induces autophagy and apoptosis.
Cancer Cell, 2021, S1535-6108(21)00659-0
Cancer Res, 2021, canres.1540.2020
Cell Rep, 2021, 34(10):108814
S1233 2-Methoxyestradiol (2-MeOE2) 2-Methoxyestradiol (2-MeOE2, NSC 659853, 2-ME2) depolymerizes microtubules and blocks HIF-1α nuclear accumulation and HIF-transcriptional activity. 2-Methoxyestradiol induces both autophagy and apoptosis in various carcinogenic cell lines. Phase 2.
Cell Death Differ, 2021, 10.1038/s41418-021-00885-x
Cancers (Basel), 2021, 13(20)5232
Cell Death Discov, 2021, 7(1):242
S1237 Temozolomide (CCRG 81045) Temozolomide (CCRG81045, NSC 362856, TMZ) is a monofunctional SN-1 alkylating agent that can modify nitrogen atoms in the DNA ring and the extracyclic oxygen group, chemically converted to MTIC and degrades to methyldiazonium cation, which transfers methyl groups to DNA at physiologic pH. A DNA damage inducer in L-1210 and L-1210/BCNU cells. Temozolomide induces apoptosis and exhibits antitumor activity.
Mol Neurobiol, 2022, 10.1007/s12035-021-02674-6
Cancer Chemother Pharmacol, 2022, 10.1007/s00280-021-04380-5
Cell Res, 2021, 10.1038/s41422-021-00528-3
S1238 Tamoxifen (ICI 46474) Tamoxifen (ICI 46474, (Z)-Tamoxifen, trans-Tamoxifen) is a selective estrogen receptor modulator (SERM). Tamoxifen enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen induces apoptosis.
Clin Cancer Res, 2021, 10.1158/1078-0432.CCR-20-3905
Cancers (Basel), 2021, 13(9)2116
Cell Death Dis, 2021, 12(6):619
S1241 Vincristine (NSC-67574) sulfate Vincristine sulfate (NSC-67574, Leurocristine, Oncovin, 22-Oxovincaleukoblastine) is an inhibitor of polymerization of microtubules by binding to tubulin with IC50 of 32 μM in a cell-free assay. Vincristine sulfate induces apoptosis.
Mol Cell, 2022, 82(1):75-89.e9
Theranostics, 2021, 11(9):4281-4297
Cell Rep, 2021, 36(11):109718
S1242 CPTH2 CPTH2 is a potent histone acetyltransferase (HAT) inhibitor modulating Gcn5p network. CPTH2 induces apoptosis and decreases the invasiveness of a ccRCC cell line through the inhibition of KAT3B.
Transl Oncol, 2021, 14(11):101196
S1244 Amuvatinib (MP-470) Amuvatinib (MP-470, HPK 56) is a potent and multi-targeted inhibitor of c-Kit, PDGFRα and Flt3 with IC50 of 10 nM, 40 nM and 81 nM, respectively. Amuvatinib suppresses c-MET and c-RET. Amuvatinib is also active as a DNA repair protein Rad51 inhibitor with antineoplastic activity. Phase 2.
mBio, 2021, 12(6):e0322821
Hum Cell, 2021, 34(6):1911-1918
Hum Cell, 2021, 10.1007/s13577-021-00579-z
S1264 PD173074 PD173074 is a potent FGFR1 inhibitor with IC50 of ~25 nM and also inhibits VEGFR2 with IC50 of 100-200 nM in cell-free assays, ~1000-fold selective for FGFR1 than PDGFR and c-Src. PD173074 reduces proliferation and promotes apoptosis in gastric cancer cells.
Oncoimmunology, 2022, 11(1):2021619
Adv Sci (Weinh), 2021, 8(2):2002922
Nat Commun, 2021, 12(1):3017
S1273 Amarogentin

Amarogentin (AG), a secoiridoid glycoside mainly extracted from Swertia and Gentiana roots, exhibits anti-oxidative, anti-tumour, and anti-diabetic activities. Amarogentin is an agonist for the bitter taste receptor TAS2R1 and inhibits in LAD-2 cells substance P-induced production of newly synthesized TNF-α. Amarogentin induces apoptosis in human gastric cancer cells (SNU-16) through G2/M cell cycle arrest and PI3K/Akt signalling pathway. Amarogentin (AG) interacts with the α2 subunit of AMP-activated protein kinase (AMPK) and activates the trimeric kinase with EC50 of 277 pM.

S1288 Camptothecin (NSC-100880) Camptothecin (NSC-100880, CPT, Campathecin, (S)-(+)-Camptothecin) is a specific inhibitor of DNA topoisomerase I (Topo I) with IC50 of 0.68 μM in a cell-free assay. Camptothecin induces apoptosis in cancer cells via microRNA-125b-mediated mitochondrial pathways. Phase 2.
Nature, 2021, 10.1038/s41586-021-04204-9
Cancer Cell, 2021, S1535-6108(21)00659-0
Mol Cell, 2021, 81(20):4228-4242.e8
S1290 Celastrol (NSC 70931) Celastrol (NSC 70931, Tripterine) is a potent proteasome inhibitor for the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM. Celastrol induces apoptosis and autophagy via the ROS/JNK signaling pathway. Celastrol inhibits dopaminergic neuronal death of Parkinson's disease through activating mitophagy.
Mol Oncol, 2021, 10.1002/1878-0261.12936
Aging (Albany NY), 2021, 13(12):16816-16833
Molecules, 2021, 26(14)4124
S1299 Floxuridine (NSC 27640) Floxuridine (NSC 27640, Deoxyfluorouridine, FUDR) is a prodrug that is rapidly catabolized to 5-fluorouracil in vivo. Floxuridine is used to treat various cancers, particularly metastases to the liver. Floxuridine inhibits Poly(ADP-Ribose) polymerase and induces DNA damage and apoptosis. Floxuridine has antiviral effects against HSV and CMV.
Cell Chem Biol, 2021, S2451-9456(21)00306-8
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Hum Cell, 2021, 34(6):1911-1918
S1312 Streptozotocin (STZ) Streptozotocin (STZ, NSC-85998, Streptozocin, U 9889) is a glucosamine-nitrosourea derivative, which is a DNA-methylating, carcinogenic, antibiotic and diabetes inducing agent. Streptozotocin induces autophagy and apoptosis. Solutions are best fresh-prepared.
Hum Cell, 2021, 34(6):1911-1918
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Hum Cell, 2021, 10.1007/s13577-021-00579-z
S1314 Zoledronic acid (ZOL 446) Zoledronic acid (ZOL 446, ZA, Zoledronate, CGP-4244, GP42446A, Zometa, Zomera, Aclasta, Reclast), a potent osteoclast inhibitor, induces apoptosis in osteoclasts by inhibiting enzymes of the mevalonate pathway and preventing the isoprenylation of small GTP-binding proteins such as Ras and Rho. Zoledronic acid (ZA) also induces autophagy.
Oncol Lett, 2022, 23(2):51
Biomater Sci, 2021, 10.1039/d0bm02107e
Hum Cell, 2021, 10.1007/s13577-021-00579-z
S1362 Rigosertib (ON-01910) Rigosertib (ON-01910) is a non-ATP-competitive inhibitor of PLK1 with IC50 of 9 nM in a cell-free assay. It shows 30-fold greater selectivity against Plk2 and no activity to Plk3. Rigosertib inhibits PI3K/Akt pathway and activates oxidative stress signals. Rigosertib induces apoptosis in various cancer cells. Phase 3.
Elife, 2021, 10e70715
Immun Inflamm Dis, 2021, 10.1002/iid3.458
Mol Cell, 2020, 79(1):191-198.e3
S1378 Ruxolitinib (INCB018424) Ruxolitinib (INCB018424) is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM in cell-free assays, >130-fold selectivity for JAK1/2 versus JAK3. Ruxolitinib kills tumor cells through toxic mitophagy. Ruxolitinib induces autophagy and enhances apoptosis.
Blood, 2022, blood.2021012366
Mol Neurodegener, 2022, 17(1):7
J Exp Clin Cancer Res, 2022, 41(1):10
S1396 Resveratrol (SRT501) Resveratrol (SRT501, trans-Resveratrol) has a wide spectrum of targets including cyclooxygenases(i.e. COX, IC50=1.1 μM), lipooxygenases(LOX, IC50=2.7 μM), kinases, sirtuins and other proteins. It has anti-cancer, anti-inflammatory, blood-sugar-lowering and other beneficial cardiovascular effects. Resveratrol induces mitophagy/autophagy and autophagy-dependent apoptosis.
Int Immunopharmacol, 2022, 103:108489
Eur J Neurosci, 2022, 10.1111/ejn.15596
Adv Sci (Weinh), 2021, e2103360
S1413 Bafilomycin A1 (Baf-A1) Bafilomycin A1(Baf-A1) is a vacuolar H+-ATPase inhibitor with IC50 of 0.44 nM. Bafilomycin A1 is found to inhibit autophagy while induces apoptosis.
Adv Sci (Weinh), 2021, e2100779
Mol Cell, 2021, S1097-2765(21)00729-2
ACS Nano, 2021, 10.1021/acsnano.1c06452
S1443 Zileuton (A-64077) Zileuton (A-64077, Abbott 64077, ZYFLO) is an orally active inhibitor of 5-lipoxygenase, and thus inhibits leukotrienes (LTB4, LTC4, LTD4, and LTE4) formation, used to decrease the symptoms of asthma. Zileuton induces apoptosis while inhibits ferroptosis.
J Exp Clin Cancer Res, 2021, 40(1):344
Front Microbiol, 2020, 11:845
Front Immunol, 2019, 10:1904
S1451 Aurora A Inhibitor I (TC-S 7010) Aurora A Inhibitor I (TC-S 7010) is a novel, potent, and selective inhibitor of Aurora A with IC50 of 3.4 nM in a cell-free assay. It is 1000-fold more selective for Aurora A than Aurora B. Aurora A Inhibitor I (TC-S 7010) triggers apoptosis through the ROS-mediated UPR signaling pathway.
EMBO Rep, 2021, e52387
Cancer Lett, 2021, 509:89-104
Nat Commun, 2020, 11(1):1308
S1452 Ispinesib (SB-715992) Ispinesib (SB-715992, CK0238273) is a potent, specific and reversible inhibitor of kinesin spindle protein (KSP) with Ki app of 1.7 nM in a cell-free assay, no inhibition to CENP-E, RabK6, MCAK, MKLP1, KHC or Kif1A. Ispinesib induces mitotic arrest and apoptotic cell death. Phase 2.
Cell, 2020, 182(3):685-712.e19
Cell, 2020, 182(3):685-712.e19
Sci Transl Med, 2020, 12(562)eaba4434
S1460 SP600125 SP600125 (Nsc75890) is a broad-spectrum JNK inhibitor for JNK1, JNK2 and JNK3 with IC50 of 40 nM, 40 nM and 90 nM in cell-free assays, respectively; 10-fold greater selectivity against MKK4, 25-fold greater selectivity against MKK3, MKK6, PKB, and PKCα, and 100-fold selectivity against ERK2, p38, Chk1, EGFR etc. SP600125 is also a broad‐spectrum inhibitor of serine/threonine kinases including Aurora kinase AFLT3 and TRKA with of IC50 of 60 nM, 90 nM and 70 nM. SP600125 inhibits autophagy and activates apoptosis.
Cells, 2022, 11(1)134
Int J Biol Sci, 2022, 18(1):349-359
Biomed Pharmacother, 2022, 145:112437
S1487 PHA-793887 PHA-793887 is a novel and potent inhibitor of CDK2, CDK5 and CDK7 with IC50 of 8 nM, 5 nM and 10 nM. It is greater than 6-fold more selective for CDK2, 5, and 7 than CDK1, 4, and 9. PHA-793887 induces cell-cycle arrest and apoptosis. Phase 1.
Cell, 2020, 182(3):685-712.e19
Cell, 2020, 182(3):685-712.e19
Mol Cell Biol, 2020, 40(4)
S1491 Fludarabine (NSC 118218) Fludarabine (NSC 118218, FaraA, Fludarabinum) is a STAT1 activation inhibitor which causes a specific depletion of STAT1 protein (and mRNA) but not of other STATs. Also a DNA synthesis inhibitor in vascular smooth muscle cells. Fludarabine induces apoptosis.
Int J Biol Sci, 2022, 18(1):331-348
Cell Metab, 2021, 33(1):110-127.e5
Cell Rep, 2021, 34(1):108584
S1497 Pralatrexate (NSC 754230) Pralatrexate (NSC 754230) is an antifolate, and structurally a folate analog. Its IC50 is < 300 nM in some cell lines. Pralatrexate induces tumor cell apoptosis.
J Clin Endocrinol Metab, 2021, dgab424
Biomol Ther (Seoul), 2021, 29(3):268-272
Hum Cell, 2021, 34(6):1911-1918
S1501 Mycophenolate mofetil (RS-61443) Mycophenolate Mofetil (RS 61443, Mycophenolic acid morpholinoethyl ester, CellCept, TM-MMF) is a non-competitive, selective and reversible inhibitor of inosine monophosphate dehydrogenase I/II with IC50 of 39 nM and 27 nM, respectively. Mycophenolate Mofetil induces caspase-dependent apoptosis and cell cycle inhibition in multiple myeloma cells.
Clin Exp Rheumatol, 2021, N/A
Nat Commun, 2020, 11(1):3811
bioRxiv, 2020, 2020/9/20.4.7.30734
S1515 Pracinostat (SB939) Pracinostat (SB939) is a potent pan-HDAC inhibitor with IC50 of 40-140 nM with exception for HDAC6. It has no activity against the class III isoenzyme SIRT I. Pracinostat (SB939) induces apoptosis in tumor cells. Phase 2.
Cancer Lett, 2021, 521:268-280
Front Immunol, 2021, 12:771453
Cell, 2020, S0092-8674(20)31394-5
S1524 AT7519 AT7519 is a multi-CDK inhibitor for CDK1, 2, 4, 6 and 9 with IC50 of 10-210 nM. It is less potent to CDK3 and little active to CDK7. AT7519 also inhibits GSK3β with IC50 of 89 nM. AT7519 induces apoptosis. Phase 2.
J Am Chem Soc, 2021, 10.1021/jacs.1c05386
Sci Rep, 2021, 11(1):17029
Fundam Clin Pharmacol, 2021, 10.1111/fcp.12709
S1526 Quizartinib (AC220) Quizartinib (AC220) is a second-generation FLT3 inhibitor for Flt3(ITD/WT) with IC50 of 1.1 nM/4.2 nM in MV4-11 and RS4;11 cells, respectively, 10-fold more selective for Flt3 than KIT, PDGFRα, PDGFRβ, RET, and CSF-1R. Quizartinib (AC220) induces apoptosis of tumor cells. Phase 3.
Oncol Lett, 2022, 23(2):51
Mol Cell, 2021, S1097-2765(21)00507-4
Clin Cancer Res, 2021, 10.1158/1078-0432.CCR-20-3458
S1533 R406 (free base) R406 (free base) is a potent Syk inhibitor with IC50 of 41 nM in a cell-free assay, strongly inhibits Syk but not Lyn, 5-fold less potent to Flt3. R406 (free base) triggers apoptosis. Phase 1.
Free Radic Biol Med, 2022, S0891-5849(22)00004-1
Nat Genet, 2021, 53(4):500-510
Sci Transl Med, 2021, 13(596)eabf8654
S1555 AZD8055 AZD8055 is a novel ATP-competitive mTOR inhibitor with IC50 of 0.8 nM in MDA-MB-468 cells with excellent selectivity (∼1,000-fold) against PI3K isoforms and ATM/DNA-PK. AZD8055 induces caspase-dependent apoptosis and also induces autophagy. Phase 1.
Immunity, 2022, 55(1):159-173.e9
Nature, 2021, 591(7849):288-292
Immunity, 2021, S1074-7613(21)00069-8
S1567 Pomalidomide (CC-4047) Pomalidomide (CC-4047) inhibits LPS-induced TNF-α release with IC50 of 13 nM in PBMCs. Pomalidomide can be utilized in PROTAC as a ligand for targeting E3 ligase and inhibiting the E3 ligase protein cereblon (CRBN). Pomalidomide promotes apoptosis and cell cycle arrest.
Nat Cell Biol, 2021, 10.1038/s41556-021-00766-y
Mol Cell, 2021, 81(6):1170-1186.e10
Sci Adv, 2021, 7(6)eabd6263
S1576 Sulfasalazine (NSC 667219) Sulfasalazine (NSC 667219, Azulfidine, Salazopyrin, Sulphasalazine) is a sulfa derivative of mesalazine, used as an anti-inflammatory agent to treat bowel disease and rheumatoid arthritis. Sulfasalazine is a potent and specific inhibitor of nuclear factor kappa B (NF-κB), TGF-β and COX-2. Sulfasalazine induces ferroptosis, apoptosis and autophagy.
Cell Metab, 2021, S1550-4131(21)00233-3
Sci Adv, 2021, 7(35)eabj0364
Sci Adv, 2021, 7(27)eabh3032
S1623 Acetylcysteine (N-acetylcysteine) Acetylcysteine (N-acetyl-l-cysteine, NAC) is a ROS(reactive oxygen species) inhibitor that antagonizes the activity of proteasome inhibitors. It is also a tumor necrosis factor production inhibitor. Acetylcysteine(N-acetyl-l-cysteine) suppresses TNF-induced NF-κB activation through inhibition of IκB kinases. Acetylcysteine(N-acetyl-l-cysteine) induces apoptosis via the mitochondria-dependent pathway. Acetylcysteine(N-acetyl-l-cysteine) inhibits ferroptosis and virus replication.Solutions of Acetylcysteine are best fresh-prepared.
J Clin Invest, 2021, e152067
EMBO Mol Med, 2021, 13(9):e13193
Elife, 2021, 10e69795
S1629 Orlistat (Ro 18-0647) Orlistat (Ro 18-0647, Tetrahydrolipstatin) is a general lipase inhibitor with IC50 of 122 ng/ml for PL from human duodenal juice. Orlistat treatment reduces proliferation, induces apoptosis and arrests cell cycle.
Nat Commun, 2021, 12(1):3830
Cell Rep, 2021, 36(12):109742
Sci Rep, 2021, 11(1):22085
S1648 Cytarabine (U-19920A) Cytarabine (U-19920A, Cytarabin, Ara-C, Arabinofuranosyl Cytidine, Cytosine β-D-arabinofuranoside, Cytosine arabinoside, NSC 63878, NSC 287459) is an antimetabolic agent and DNA synthesis inhibitor with IC50 of 16 nM in wild-type CCRF-CEM cells. Cytarabine induces autophagy and apoptosis.
Leukemia, 2021, 10.1038/s41375-021-01361-8
Blood Cancer J, 2021, 11(6):111
Cell Rep, 2021, 36(7):109559
S1680 Disulfiram (NSC 190940) Disulfiram (NSC 190940, Tetraethylthiuram disulfide, TETD) is a specific inhibitor of aldehyde-dehydrogenase (ALDH) with IC50 of 0.15 μM and 1.45 μM for hALDH1 and hALDH2, respectively. Disulfiram is used for the treatment of chronic alcoholism by producing an acute sensitivity to alcohol. Disulfiram induces apoptosis. Disulfiram is also an inhibitor of pore formation by gasdermin D (GSDMD).
mBio, 2022, 10.1128/mbio.02739-21
Int Immunopharmacol, 2022, 102:108401
Cancer Res, 2021, canres.1337.2021
S1692 Busulfan (NSC-750) Busulfan (NSC-750) is a cell cycle non-specific alkylating antineoplastic agent. Busulfan induces apoptosis.
Breast Cancer Res, 2021, 23(1):100
Hum Cell, 2021, 34(6):1911-1918
Hum Cell, 2021, 10.1007/s13577-021-00579-z
S1714 Gemcitabine (LY-188011) Gemcitabine (LY-188011, NSC 613327), a nucleic acid synthesis inhibitor, is a very potent and specific deoxycytidine analogue, used as chemotherapy. Gemcitabine induces a potent p53-dependent apoptosis.
Nat Commun, 2021, 12(1):1602
Cancer Res, 2021, canres.1337.2021
Cell Rep, 2021, 34(10):108814
S1759 Pitavastatin (NK-104) calcium Pitavastatin Calcium (NK-104, P-872441, itavastatin, nisvastatin), a novel member of the medication class of statins, is a calcium salt formulation of pitavastatin which is a highly effective HMG-CoA reductase inhibitor. Pitavastatin Calcium attenuates AGEs-induced mitophagy via inhibition of ROS generation. Pitavastatin Calcium induces autophagy and apoptosis.
Nat Biotechnol, 2021, 10.1038/s41587-021-00860-4
Cancer Discov, 2021, candisc.0551.2021
Transl Oncol, 2021, 14(7):101107
S1786 Verteporfin (CL 318952) Verteporfin (CL 318952, Visudyne) is a small molecule that inhibits TEAD–YAP association and YAP-induced liver overgrowth. It is also a potent second-generation photosensitizing agent derived from porphyrin. Verteporfin is an autophagy inhibitor. Verteporfin inhibits cell proliferation and induces apoptosis.
Nat Commun, 2022, 13(1):50
Hum Mol Genet, 2022, ddab374
Exp Cell Res, 2022, 411(1):113000
S1792 Simvastatin (MK 733) Simvastatin (MK-0733, MK 733) is a competitive inhibitor of HMG-CoA reductase with Ki of 0.1-0.2 nM in cell-free assays. Simvastatin induces ferroptosis, mitophagy, autophagy and apoptosis.
Nat Biotechnol, 2021, 10.1038/s41587-021-00860-4
Theranostics, 2021, 11(4):1609-1625
Theranostics, 2021, 11(13):6560-6572
S1807 Aciclovir (BW 248U) Acyclovir (BW 248U, Acyclovir, Acycloguanosine, Zovirax, ACV, NSC 645011) is a synthetic nucleoside analogue active against herpesviruses. Acyclovir induces cell cycle perturbation and apoptosis in Jurkat leukemia cells.
Microbiol Spectr, 2021, 9(3):e0064621
Front Microbiol, 2021, 12:722748
Vet Microbiol, 2021, 265:109313
S1848 Curcumin Curcumin (Diferuloylmethane, Natural Yellow 3, Turmeric yellow) is the principal curcuminoid of the popular Indian spice turmeric, which is a member of the ginger family (Zingiberaceae). It is an inhibitor of p300 histone acetylatransferase(IC50~25 μM)and Histone deacetylase (HDAC); activates Nrf2 pathway and supresses the activation of NF-κB. Curcumin induces mitophagy, autophagy, apoptosis, and cell cycle arrest with antitumor activity. Curcumin reduces renal damage associated with rhabdomyolysis by decreasing ferroptosis-mediated cell death. Curcumin exhibits anti-infective properties against various human pathogens like the influenza virus, hepatitis C virus, HIV and so on.
Adv Sci (Weinh), 2021, e2103360
Front Immunol, 2021, 12:656242
Aging (Albany NY), 2021, 13(10):13968-14000
S1896 Hydroxyurea (NSC-32065) Hydroxyurea (NSC-32065, NCI-C04831, Hydroxycarbamide) is an antineoplastic agent that inhibits DNA synthesis through the inhibition of ribonucleoside diphosphate reductase. Hydroxyurea activates apoptosis and autophagy. Hydroxyurea is used to treat HIV infection.
Cancer Res, 2022, canres.1707.2021
Nat Commun, 2021, 12(1):5572
Cancer Res, 2021, canres.3761.2020
S1972 Tamoxifen (ICI 46474) Citrate Tamoxifen Citrate (ICI 46474) is a selective estrogen receptor modulator (SERM). Tamoxifen Citrate is also a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen induces apoptosis and autophagy.
Clin Cancer Res, 2021, 10.1158/1078-0432.CCR-20-3905
Cancers (Basel), 2021, 13(9)2116
Cell Death Dis, 2021, 12(6):619
S1999 Sodium butyrate Sodium butyrate (NaB, Butanoic acid sodium salt), sodium salt of butyric acid, is a histone deacetylase inhibitor and competitively binds to the zinc sites of class I and II histone deacetylases (HDACs). Sodium butyrate (NaB) inhibits cell cycle progression, promotes differentiation, and induces apoptosis and autophagy in several types of cancer cells.
Cell Mol Life Sci, 2021, 10.1007/s00018-021-03883-x
Front Cell Dev Biol, 2021, 9:662868
Int J Mol Sci, 2020, 21(2)
S2012 PCI-34051 PCI-34051 is a potent and specific HDAC8 inhibitor with IC50 of 10 nM in a cell-free assay. It has greater than 200-fold selectivity over HDAC1 and 6, more than 1000-fold selectivity over HDAC2, 3, and 10. PCI-34051 induces caspase-dependent apoptosis.
Cell Rep, 2021, 37(12):110129
Thyroid, 2021, 10.1089/thy.2020.0948
Tuberculosis (Edinb), 2021, 127:102062
S2013 PF-573228 PF-573228 is an ATP-competitive inhibitor of FAK with IC50 of 4 nM in a cell-free assay, ~50- to 250-fold selective for FAK than Pyk2, CDK1/7 and GSK-3β. PF-573228 induces apoptosis.
Proc Natl Acad Sci U S A, 2021, 118(40)e2105367118
Cell Rep, 2021, 35(7):109159
FASEB J, 2021, 35(5):e21598
S2077 Atorvastatin Calcium Atorvastatin Calcium is an inhibitor of HMG-CoA reductase used as a cholesterol-lowering medication that blocks the production of cholesterol. Atorvastatin Calcium induces apoptosis and autophagy.
Nat Biotechnol, 2021, 10.1038/s41587-021-00860-4
Oncol Lett, 2021, 21(2):82
Neurobiol Dis, 2021, 152:105294
S2161 RAF265 (CHIR-265) RAF265 (CHIR-265) is a potent selective inhibitor of C-Raf/B-Raf/B-Raf V600E with IC50 of 3-60 nM, and exhibits potent inhibition on VEGFR2 phosphorylation with EC50 of 30 nM in cell-free assays. RAF265 (CHIR-265) induces cell cycle arrest and apoptosis. Phase 2.
Drug Chem Toxicol, 2022, 1-10
J Clin Invest, 2021, e147849
J Clin Invest, 2021, e147849
S2194 R406 R406 is a potent Syk inhibitor with IC50 of 41 nM in cell-free assays, strongly inhibits Syk but not Lyn, 5-fold less potent to Flt3. R406 induces apoptosis. Phase 1.
Free Radic Biol Med, 2022, S0891-5849(22)00004-1
Cancer Cell, 2021, S1535-6108(21)00492-X
Sci Transl Med, 2021, 13(596)eabf8654
S2198 SGI-1776 free base SGI-1776 free base is a novel ATP competitive inhibitor of Pim1 with IC50 of 7 nM in a cell-free assay, 50- and 10-fold selective versus Pim2 and Pim3, also potent to Flt3 and haspin. SGI-1776 induces apoptosis and autophagy. Phase 1.
Cancer Res, 2021, canres.1023.2021
Commun Biol, 2021, 4(1):1221
Cell, 2020, 182(3):685-712.e19
S2214 AZ 960 AZ 960 is a novel ATP competitive JAK2 inhibitor with IC50 and Ki of <3 nM and 0.45 nM, 3-fold selectivity of AZ960 for JAK2 over JAK3. AZ 960 induces apoptosis and growth arrest.
BMC Cancer, 2021, 21(1):1213
Carcinogenesis, 2020, 41(7):993-1004
Nat Commun, 2019, 10(1):716
S2215 DAPT (GSI-IX) DAPT (GSI-IX, LY-374973) is a novel γ-secretase inhibitor, which inhibits Aβ production with IC50 of 20 nM in HEK 293 cells. DAPT enhances the apoptosis of human tongue carcinoma cells and regulates autophagy.
Adv Mater, 2022, e2106829
Hepatology, 2022, 10.1002/hep.32332
Sci Rep, 2022, 12(1):7
S2218 Torkinib (PP242) Torkinib (PP242) is a selective mTOR inhibitor with IC50 of 8 nM in cell-free assays; targets both mTOR complexes with >10- and 100-fold selectivity for mTOR than PI3Kδ or PI3Kα/β/γ, respectively. Torkinib (PP242) induces mitophagy and apoptosis.
Immunity, 2022, 55(1):159-173.e9
Methods Mol Biol, 2022, 2445:139-169
Immunity, 2021, 54(10):2354-2371.e8
S2219 Momelotinib (CYT387) Momelotinib (CYT387, LM-1149 , CYT11387) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, ~10-fold selectivity versus JAK3. Momelotinib (CYT387) induces apoptosis and autophagy. Phase 3.
Cell Stem Cell, 2021, S1934-5909(21)00344-1
Cancer Res, 2021, canres.0955.2021
J Transl Med, 2021, 19(1):396
S2235 Volasertib (BI 6727) Volasertib (BI 6727) is a highly potent Plk1 inhibitor with IC50 of 0.87 nM in a cell-free assay. It shows 6- and 65-fold greater selectivity against Plk2 and Plk3. Volasertib induces cell cycle arrest and apoptosis in various cancer cells. Phase 3.
Science, 2021, 371(6535)eabc5386
Mol Cell, 2021, S1097-2765(20)30946-1
Nat Commun, 2021, 12(1):5356
S2243 Degrasyn (WP1130) Degrasyn (WP1130) is a selective deubiquitinase (DUB: USP5, UCH-L1, USP9x, USP14, and UCH37) inhibitor and also suppresses Bcr/Abl, also a JAK2 transducer (without affecting 20S proteasome) and activator of transcription (STAT). Degrasyn (WP1130) induces apoptosis and blocks autophagy.
Br J Cancer, 2021, 10.1038/s41416-021-01421-x
Cell Chem Biol, 2021, S2451-9456(21)00213-0
Transl Lung Cancer Res, 2021, 10(10):3995-4011
S2247 Buparlisib (BKM120) Buparlisib (BKM120, NVP-BKM120) is a selective PI3K inhibitor of p110α/β/δ/γ with IC50 of 52 nM/166 nM/116 nM/262 nM in cell-free assays, respectively. Reduced potency against VPS34, mTOR, DNAPK, with little activity to PI4Kβ. Buparlisib induces apoptosis. Phase 2.
Cancer Cell, 2021, S1535-6108(21)00284-1
Adv Sci (Weinh), 2021, e2103360
Mol Cell, 2021, S1097-2765(21)00232-X
S2248 Silmitasertib (CX-4945) Silmitasertib (CX-4945) is a potent and selective inhibitor of CK2 (casein kinase 2) with IC50 of 1 nM in a cell-free assay, less potent to Flt3, Pim1 and CDK1 (inactive in cell-based assay). Silmitasertib induces autophagy and promotes apoptosis. Phase 1/2.
Cell Mol Gastroenterol Hepatol, 2022, S2352-345X(22)00003-0
Sci Rep, 2022, 12(1):7
Genes Dev, 2021, 35(15-16):1123-1141
S2271 Berberine chloride (NSC 646666) Berberine chloride (NSC 646666, Natural Yellow 18) is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.
Front Pharmacol, 2021, 12:632201
Molecules, 2021, 26(5)1210
Biology (Basel), 2021, 10(3)250
S2285 Cryptotanshinone Cryptotanshinone is a STAT3 inhibitor with IC50 of 4.6 μM in a cell-free assay, strongly inhibits phosphorylation of STAT3 Tyr705, with a small effect on STAT3 Ser727, but none against STAT1 nor STAT5. Cryptotanshinone induces ROS-dependent autophagy and mitochondria-mediated apoptosis.
Front Immunol, 2021, 12:712781
Int J Biol Sci, 2021, 17(10):2417-2429
J Cell Mol Med, 2021, 10.1111/jcmm.16250
S2290 Dihydroartemisinin (DHA) Dihydroartemisinin (DHA, Dihydroqinghaosu, β-Dihydroartemisinin, Artenimol) is a semi-synthetic derivative of artemisinin and isolated from the traditional Chinese herb Artemisia annua. Dihydroartemisinin induces autophagy and apoptosis by suppressing NF-κB activation.
Nat Immunol, 2021, 10.1038/s41590-021-00967-5
ACS Infect Dis, 2021, 10.1021/acsinfecdis.0c00580
Mol Med Rep, 2021, 23(1)40
S2310 Honokiol (NSC 293100) Honokiol (NSC 293100) is the active principle of magnolia extract that inhibits Akt-phosphorylation and promotes ERK1/2 phosphorylation. Honokiol causes G0/G1 phase arrest, induces apoptosis, and autophagy via the ROS/ERK1/2 signaling pathway. Honokiol inhibits hepatitis C virus (HCV) infection. Phase 3.
Cell Death Dis, 2021, 12(9):847
Front Cell Dev Biol, 2021, 9:619475
Carcinogenesis, 2021, bgab126
S2348 Rotenone (Barbasco) Rotenone (Barbasco, Dactinol, Paraderil, Rotenon, Rotocide) is a botanical insecticide that is an inhibitor of mitochondrial electron transport. Rotenone inhibits NADH/DB oxidoreductase and NADH oxidase with IC50 of 28.8 nM and 5.1 nM, respectively. Rotenone induces apoptosis through enhancing mitochondrial reactive oxygen species production.
Nature, 2021, 10.1038/s41586-021-04049-2
Sci Adv, 2021, 7(49):eabk0490
Sci Adv, 2021, 7(49):eabk0490
S2391 Quercetin (NSC 9221) Quercetin (NSC 9221, Sophoretin, C.I. 75720), a natural flavonoid present in vegetables, fruit and wine, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor with IC50 of 2.4-5.4 μM. Quercetin induces mitophagy, apoptosis and protective autophagy. Phase 4.
ACS Appl Mater Interfaces, 2022, 10.1021/acsami.1c22138
Nucleic Acids Res, 2021, gkab538
Redox Biol, 2021, 44:102010
S2485 Mitoxantrone (NSC-301739) 2HCl Mitoxantrone 2HCl (NSC-301739) is a dihydrochloride salt of Mitoxantrone. Mitoxantrone is an inhibitor of type II topoisomerase and protein kinase C (PKC) with IC50 of 8.5 μM for PKC. Mitoxantrone inhibits cell proliferative growth of MCF-7/wt cells with IC50 of 0.42 μM. Mitoxantrone also induces apoptosis.
Cancers (Basel), 2021, 13(8)1954
Cell Chem Biol, 2021, S2451-9456(21)00213-0
Pharmacol Res, 2021, 174:105927
S2606 Mifepristone (RU486) Mifepristone (RU486, C-1073, RU 38486, Mifegyne) is a remarkably active antagonist of progesterone receptor and glucocorticoid receptor with IC50 of 0.2 nM and 2.6 nM, respectively. Mifepristone promotes cell autophagy and apoptosis, decreases Bcl-2 level and increases Beclin1 level, accompanied by weakened interaction between Bcl-2 and Beclin1.
Nat Commun, 2021, 12(1):7041
Exp Eye Res, 2021, S0014-4835(21)00331-6
Oncol Rep, 2021, 46(3)202
S2619 MG-132 MG132 (Z-Leu-Leu-Leu-al) is a potent cell-permeable proteasome and calpain inhibitor with IC50s of 0.1 μM and 1.2 μM for the inhibition of proteasome and calpain, respectively. MG132 activates autophagy and induces apoptosis in tumor cells.
Sci Adv, 2022, 8(2):eabk1789
Nat Commun, 2022, 13(1):12
Nat Commun, 2022, 13(1):165
S2626 Rabusertib (LY2603618) Rabusertib (LY2603618, IC-83) is a highly selective Chk1 inhibitor with potential anti-tumor activity in a cell-free assay. IC50=7 nM, showing approximately 100-fold more potent against Chk1 than against any of the other protein kinases evaluated. Rabusertib (LY2603618) induces cell cycle arrest, DNA damage response and autophagy in cancer cells. Rabusertib (LY2603618) induces bak-dependent apoptosis in AML cell lines.
Nat Genet, 2021, 10.1038/s41588-021-00893-0
Cancer Cell, 2021, S1535-6108(21)00383-4
Nucleic Acids Res, 2021, gkab643
S2635 CCT128930 CCT128930 is a potent, ATP-competitive and selective inhibitor of Akt2 with IC50 of 6 nM in a cell-free assay, 28-fold greater selectivity for Akt2 than the closely related PKA kinase. CCT128930 induces cell cycle arrest, DNA damage, and autophagy independent of Akt inhibition. High dose of CCT128930 triggers cell apoptosis in HepG2 cells.
ACS Nano, 2021, 10.1021/acsnano.1c06452
Front Pharmacol, 2020, 11:593832
Biomed Pharmacother, 2020, 130:110544
S2662 ICG-001 ICG-001 antagonizes Wnt/β-catenin/TCF-mediated transcription and specifically binds to CREB-binding protein (CBP) with IC50 of 3 μM, but is not the related transcriptional coactivator p300. ICG-001 induces apoptosis.
Sci Rep, 2022, 12(1):7
Nat Cell Biol, 2021, 23(3):257-267
Gastroenterology, 2021, S0016-5085(21)03489-2
S2673 Trametinib (GSK1120212) Trametinib (GSK1120212, JTP-74057, Mekinist) is a highly specific and potent MEK1/2 inhibitor with IC50 of 0.92 nM/1.8 nM in cell-free assays, no inhibition of the kinase activities of c-Raf, B-Raf, ERK1/2. Trametinib activates autophagy and induces apoptosis.
Cell Death Dis, 2022, 13(1):54
Cancer Discov, 2022, 12(1):47-61
Cold Spring Harb Mol Case Stud, 2022, 8(1)a006140
S2696 Apitolisib (GDC-0980) Apitolisib (GDC-0980, RG7422, GNE 390) is a potent, class I PI3K inhibitor for PI3Kα/β/δ/γ with IC50 of 5 nM/27 nM/7 nM/14 nM in cell-free assays, respectively. Also a mTOR inhibitor with Ki of 17 nM in a cell-free assay, and highly selective versus other PIKK family kinases. Apitolisib activates autophagy and apoptosis simultaneously in pancreatic cancer cells. Phase 2.
Adv Sci (Weinh), 2021, e2103360
Cancers (Basel), 2021, 13(9)2139
Commun Biol, 2021, 4(1):1333
S2704 LY2109761 LY2109761 is a novel selective TGF-β receptor type I/II (TβRI/II) dual inhibitor with Ki of 38 nM and 300 nM in a cell-free assay, respectively; shown to negatively affect the phosphorylation of Smad2. LY2109761 blocks autophagy and induces apoptosis.
Nat Commun, 2021, 12(1):2102
Nucleic Acids Res, 2021, 49(22):12855-12869
Cell Rep, 2021, 34(12):108882
S2714 LY411575 LY411575 is a potent γ-secretase inhibitor with IC50 of 0.078 nM/0.082 nM (membrane/cell-based), also inhibits Notch cleavage with IC50 of 0.39 nM in APP or NΔE expressing HEK293 cells. LY411575 induces apoptosis.
Sci Rep, 2022, 12(1):7
Inflammation, 2022, 10.1007/s10753-021-01591-z
Nat Commun, 2021, 12(1):6839
S2727 Dacomitinib (PF-00299804) Dacomitinib (PF299804, PF299) is a potent, irreversible pan-ErbB inhibitor, mostly to EGFR with IC50 of 6 nM in a cell-free assay. Dacomitinib inhibits ERBB2 and ERBB4 with IC50 of 45.7 nM and 73.7 nM, respectively. Dacomitinib is effective against NSCLCs with EGFR or ERBB2 mutations (resistant to gefitinib) as well as those harboring the EGFR T790M mutation. Dacomitinib inhibits cell growth and induces apoptosis. Phase 2.
Cancer Med, 2022, 10.1002/cam4.4504
Int J Mol Sci, 2021, 23(1)81
Lung Cancer, 2021, 162:79-85
S2729 SB415286 SB415286 is a potent GSK3α inhibitor with IC50/Ki of 78 nM/31 nM with equally effective inhibition of GSK-3β. SB415286 causes MM cell growth arrest and apoptosis.
Sci Rep, 2022, 12(1):7
Int J Biol Macromol, 2021, 180:97-111
Toxicol Lett, 2021, 341:68-79
S2736 Fedratinib (TG101348) Fedratinib (SAR302503, TG101348) is a selective inhibitor of JAK2 with IC50 of 3 nM in cell-free assays, 35- and 334-fold more selective for JAK2 versus JAK1 and JAK3. Fedratinib also inhibits FMS-like tyrosine kinase 3 (FLT3) and RET (c-RET) with IC50 of 15 nM and 48 nM, respectively. Fedratinib has potential antineoplastic activity. Fedratinib inhibits proliferation and induces apoptosis. Phase 2.
Sci Rep, 2022, 12(1):7
Cell, 2021, 184(2):334-351.e20
Mol Cell, 2021, S1097-2765(21)01068-6
S2741 Niraparib (MK-4827) Niraparib (MK-4827) is a selective inhibitor of PARP1/2 with IC50 of 3.8 nM/2.1 nM, with great activity in cancer cells with mutant BRCA-1 and BRCA-2. It is >330-fold selective against PARP3, V-PARP and Tank1. Niraparib can form PARP–DNA complexes resulting in DNA damage, apoptosis, and cell death. Phase 3.
Sci Transl Med, 2021, 13(592)eabc7211
Sci Adv, 2021, 7(21)eabf0197
Cell Rep, 2021, 36(4):109429
S2743 PF-04691502 PF-04691502 (PF4691502) is an ATP-competitive PI3K(α/β/δ/γ)/mTOR dual inhibitor with Ki of 1.8 nM/2.1 nM/1.6 nM/1.9 nM and 16 nM in cell-free assays, little activity against either Vps34, AKT, PDK1, p70S6K, MEK, ERK, p38, or JNK. PF-04691502 induces apoptosis. Phase 2.
Cells, 2021, 10(5)1261
J Cell Physiol, 2021, 10.1002/jcp.30657
Front Pharmacol, 2021, 12:749242
S2746 AZ 628 AZ628 is a new pan-Raf inhibitor for BRAF, BRAFV600E, and c-Raf-1 with IC50 of 105 nM, 34 nM and 29 nM in cell-free assays, also inhibits VEGFR2, DDR2, Lyn, Flt1, FMS, etc. AZ628 induces apoptosis.
Drug Chem Toxicol, 2022, 1-10
Cell Rep, 2021, 35(11):109233
Cell Death Discov, 2021, 7(1):359
S2753 Tivantinib (ARQ 197) Tivantinib (ARQ 197) is the first non-ATP-competitive c-Met inhibitor with Ki of 0.355 μM in a cell-free assay, little activity to Ron, and no inhibition to EGFR, InsR, PDGFRα or FGFR1/4. Tivantinib (ARQ 197) induces a G2/M arrest and apoptosis. Phase 3.
Signal Transduct Target Ther, 2021, 6(1):401
J Cell Mol Med, 2021, 10.1111/jcmm.16953
Eur J Pharmacol, 2021, 906:174214
S2759 Fimepinostat (CUDC-907) CUDC-907 is a dual PI3K and HDAC inhibitor for PI3Kα and HDAC1/2/3/10 with IC50 of 19 nM and 1.7 nM/5 nM/1.8 nM/2.8 nM, respectively. CUDC-907 induces cell cycle arrest and apoptosis in breast cancer cells. Phase 1.
Blood Cancer J, 2021, 11(6):111
Cancer Chemother Pharmacol, 2021, 10.1007/s00280-020-04210-0
Exp Hematol Oncol, 2021, 10(1):19
S2775 Nocodazole (R17934) Nocodazole (R17934, Oncodazole, NSC238159) is a rapidly-reversible inhibitor of microtubule polymerization, also inhibits Abl, Abl(E255K) and Abl(T315I) with IC50 of 0.21 μM, 0.53 μM and 0.64 μM in cell-free assays, respectively. Nocodazole induces apoptosis.
Mol Cancer Res, 2022, molcanres.0612.2021
Cancer Cell, 2021, S1535-6108(21)00383-4
Nat Immunol, 2021, 10.1038/s41590-021-01090-1
S2776 Devimistat (CPI-613) Devimistat (CPI-613), a lipoate analog, inhibits mitochondrial enzymes pyruvate dehydrogenase (PDH) and α-ketoglutarate dehydrogenase in NCI-H460 cell line, disrupts tumor cell mitochondrial metabolism. CPI-613 induces apoptosis in pancreatic cancer cells. Phase 2.
J Exp Clin Cancer Res, 2021, 40(1):393
Front Immunol, 2021, 12:696101
Elife, 2020, 9e56749
S2783 Vistusertib (AZD2014) Vistusertib (AZD2014) is a novel mTOR inhibitor with IC50 of 2.8 nM in a cell-free assay; highly selective against multiple PI3K isoforms (α/β/γ/δ). AZD2014 showed no or weak binding to the majority of kinases when tested at 1 μM. AZD2014 induces proliferation suppression, apoptosis, cell cycle arrest, and autophagy in HCC cells with antitumor activity.
Adv Sci (Weinh), 2021, e2103360
Nat Commun, 2021, 12(1):1876
Cell Rep, 2021, 35(1):108940
S2788 Capmatinib (INCB28060) Capmatinib (INCB28060, INC280, NVP-INC280) is a novel, ATP-competitive inhibitor of c-MET with IC50 of 0.13 nM in a cell-free assay, inactive against RONβ, as well as EGFR and HER-3. Capmatinib (INCB28060) inhibits Wnt/β-catenin and EMT signaling pathways and induces apoptosis in diffuse gastric cancer positive for c-MET amplification. Phase 1.
Oncogene, 2022, 10.1038/s41388-021-02136-2
Cancer Cell, 2021, S1535-6108(21)00492-X
Clin Cancer Res, 2021, 27(20):5697-5707
S2789 Tofacitinib (CP-690550) Tofacitinib (CP-690550,Tasocitinib) is a novel inhibitor of JAK3 with IC50 of 1 nM in cell-free assays, 20- to 100-fold less potent against JAK2 and JAK1. Tofacitinib inhibits the expression of antiapoptotic BCL-A1 and BCL-XL in human plasmacytoid dendritic cells (PDC) and induced PDC apoptosis.
Blood, 2022, blood.2021012366
Nat Commun, 2021, 12(1):5183
Clin Cancer Res, 2021, clincanres.1978.2021
S2796 WP1066 WP1066 is a novel inhibitor of JAK2 and STAT3 with IC50 of 2.30 μM and 2.43 μM in HEL cells; shows activity to JAK2, STAT3, STAT5, and ERK1/2 not JAK1 and JAK3. WP1066 induces apoptosis. Phase 1.
Cell Death Differ, 2021, 10.1038/s41418-021-00880-2
J Cell Physiol, 2021, 10.1002/jcp.30373
Front Oncol, 2021, 11:705547
S2812 (R)-(-)-Gossypol acetic acid (R)-(-)-Gossypol (AT-101) acetic acid, the R-(-) enantiomer of Gossypol acetic acid, binds with Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.32 μM, 0.48 μM and 0.18 μM in cell-free assays; does not inhibit BIR3 domain and BID. AT-101 simultaneously triggers apoptosis and a cytoprotective type of autophagy. Phase 2.
Eur J Pharm Sci, 2020, 142:105105
Platelets, 2020, 10.1080/09537104.2020.1724276
Cancers (Basel), 2020, 12(8):E2298
S2817 Torin 2 Torin 2 is a potent and selective mTOR inhibitor with IC50 of 0.25 nM in p53−/− MEFs cell line; 800-fold greater selectivity for mTOR than PI3K and improved pharmacokinetic properties. Inhibition of ATM/ATR/DNA-PK with EC50 of 28 nM/35 nM/118 nM,in PC3 cell lines respectively. Torin 2 decreases cell viability and induces autophagy and apoptosis.
Nat Commun, 2021, 12(1):245
Cell Rep, 2021, 35(1):108940
Cell Death Dis, 2021, 12(11):1028
S2820 TAE226 (NVP-TAE226) TAE226 (NVP-TAE226) is a potent FAK inhibitor with IC50 of 5.5 nM and modestly potent to Pyk2, ~10- to 100-fold less potent against InsR, IGF-1R, ALK, and c-Met. TAE226 (NVP-TAE226) induces apoptosis.
Cancer Cell, 2021, S1535-6108(21)00492-X
Nat Commun, 2021, 12(1):3519
mBio, 2021, 12(4):e0149421
S2824 TPCA-1 TPCA-1 (GW683965) is an inhibitor of IKK-2 with IC50 of 17.9 nM in a cell-free assay, inhibits NF-κB pathway, exhibits 22-fold selectivity over IKK-1. TPCA-1 is also an inhibitor of STAT3 and enhances apoptosis.
Proc Natl Acad Sci U S A, 2022, 119(3)e2114134119
Cell Rep, 2021, 35(6):109112
Protein Cell, 2021, 10.1007/s13238-021-00858-3
S2853 Carfilzomib (PR-171) Carfilzomib (PR-171) is an irreversible proteasome inhibitor with IC50 of <5 nM in ANBL-6 cells, displayed preferential in vitro inhibitory potency against the ChT-L activity in the β5 subunit, but little or no effect on the PGPH and T-L activities. Carfilzomib activates prosurvival autophagy and induces cell apoptosis.
Cancer Cell, 2021, S1535-6108(20)30609-7
Sci Adv, 2021, 7(23)eabg2697
Autophagy, 2021, 1-14
S2891 GW441756 GW441756 is a potent, selective inhibitor of TrkA with IC50 of 2 nM, with very little activity to c-Raf1 and CDK2. GW441756 produces a relevant increase of caspase-3 that leads to apoptosis.
Biosci Biotechnol Biochem, 2021, 85(3):675-686
Cancer Res, 2020, canres.1992.2020
Mol Neurobiol, 2020, 10.1007/s12035-020-02156-1
S2893 NU7026 NU7026 (LY293646) is a potent DNA-PK inhibitor with IC50 of 0.23 μM in cell-free assays, 60-fold selective for DNA-PK than PI3K and inactive against both ATM and ATR. NU7026 enhances G2/M cell arrest and apoptosis.
Sci Signal, 2022, 15(715):eabh2290
Nucleic Acids Res, 2021, gkab584
Cell Rep, 2021, 37(3):109854
S2913 BAY 11-7082 BAY 11-7082 (BAY 11-7821) is a NF-κB inhibitor, inhibits TNFα-induced IκBα phosphorylation with IC50 of 10 μM in tumor cells. BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 with IC50 of 0.19 μM and 0.96 μM, respectively. BAY 11-7082 induces apoptosis and S phase arrest in gastric cancer cells.
Nat Cell Biol, 2021, 23(4):355-365
Nat Commun, 2021, 12(1):1394
EMBO Rep, 2021, 22(9):e52576
S2942 EB-3D EB-3D is a potent and selective inhibitor of choline kinase α (ChoKα) with IC50 of 1 μM for ChoKα1. EB-3D induces deregulation of the AMPK-mTOR pathway and apoptosis in leukemia T-cells.
S3020 Romidepsin (FK228, Depsipeptide) Romidepsin (FK228, Depsipeptide, FR 901228, NSC 630176) is a potent HDAC1 and HDAC2 inhibitor with IC50 of 36 nM and 47 nM in cell-free assays, respectively. Romidepsin (FK228/depsipeptide) controls growth and induces apoptosis in neuroblastoma tumor cells.
Hepatology, 2021, 10.1002/hep.32245
Hepatology, 2021, 10.1002/hep.32245
Nat Commun, 2021, 12(1):7213
S3035 Daunorubicin (RP 13057) HCl Daunorubicin HCl (Daunomycin, RP 13057, Rubidomycin) inhibits both DNA and RNA synthesis and inhibits DNA synthesis with Ki of 0.02 μM in a cell-free assay. Daunorubicin is a topoisomerase II inhibitor that induces apoptosis.
Blood, 2021, 138(9):790-805
Int J Mol Sci, 2021, 22(3)1362
Sci Rep, 2021, 11(1):12148
S3168New cis-Resveratrol cis-Resveratrol (cis-RESV, cRes, (Z)-Resveratrol) is the Cis isomer of Resveratrol. Resveratrol is a natural phenolic compound with anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol is an inhibitor of pregnane X receptor (PXR) and an activator of Nrf2 and SIRT1 and may induce apoptosis. Resveratrol also inhibits a wide spectrum of targets including 5-lipoxygenase (LOX), cyclooxygenase (COX), IKKβ, DNA polymerases α and δ with IC50 of 2.7 μM, <1 μM, 1 μM, 3.3 μM and 5 μM, respectively.
S3224 Cinobufagin Cinobufagin (Cinobufagine), an active ingredient of Venenum Bufonis, inhibits tumor development. Cinobufagin increases ATM and Chk2 and decreases CDC25C, CDK1, and cyclin B. Cinobufagin inhibits PI3K, AKT and Bcl-2 while increases levels of cleaved caspase-9 and caspase-3. Thus, Cinobufagin induces cell cycle arrest at the G2/M phase and apoptosis.
S3238 Resibufogenin Resibufogenin (Bufogenin, Recibufogenin), a component of huachansu with anticancer effect, triggers necroptosis through upregulating receptor-interacting protein kinase 3 (RIP3) and phosphorylating mixed lineage kinase domain-like protein at Ser358. Resibufogenin exerts cytotoxic effect by inducing reactive oxygen species (ROS) accumulation. Resibufogenin induces apoptosis and caspase-3 and caspase-8 activity. Resibufogenin increases Bax/Bcl-2 expression, and suppresses cyclin D1, cyclin E, PI3K, p-AKT, p-GSK3β and β-catenin protein expression.
S3245 Nodakenetin Nodakenetin (NANI), a plant-derived coumarin isolated from Angelica decursiva, inhibits α-glucosidase, PTP1B, rat lens aldose reductase (RLAR), AChE, BChE, and β-site amyloid precursor protein cleaving enzyme 1 (BACE1). Nodakenetin alters the protein expression of Bax and Bcl-2, and prompts mitochondrial apoptosis. Nodakenetin exhibits anti-tumor activity.
S3256 Tectochrysin Tectochrysin (Techtochrysin, NSC 80687) is one of the major flavonoids of Alpinia oxyphylla Miquel. Tectochrysin significantly increases the expression of DR3, DR4 and Fas and inhibits activity of NF-κB. Tectochrysin induces apoptotic cell death.
S3271 Caudatin Caudatin (Cauldatin), one species of C‑21 steroidal from Cynanchum auriculatum (C. auriculatum), effectively inhibits human glioma growth in vitro and in vivo through triggering cell cycle arrest and apoptosis.
S3287 Rosamultin Rosamultin is a 19 α-hydroxyursane-type triterpenoid isolated from Potentilla anserina L. that inhibits HIV-1 protease. Rosamultin has protective effects on H2O2-induced oxidative damage and apoptosis.
S3289 Daphnoretin Daphnoretin (Dephnoretin, Thymelol), a biologically active compound isolated from Wikstroemia indica C.A. Mey., is a protein kinase C (PKC) activator. Daphnoretin inhibits the proliferation, invasion, and migration of tumor cells and promote its apoptosis by regulating the activity of Akt signal pathway.
S3296 Hispidulin Hispidulin (Dinatin), an active natrual ingredient in a number of traditional Chinese medicinal herbs, exhibits inhibitory activity against the oncogenic protein kinase Pim-1 with IC50 of 2.71 μM. Hispidulin induces apoptosis through mitochondrial dysfunction and inhibition of P13k/Akt signalling pathway in HepG2 cancer cells. Hispidulin exerts anti-osteoporotic and bone resorption attenuating effects via activating the AMPK signaling pathway.
S3300 Desoxyrhaponticin Desoxyrhaponticin (DC, DES), a stilbene glycoside from Rheum tanguticum Maxim. ex Balf. (rhubarb) which is a traditional Chinese nutritional food, is a fatty acid synthase (FAS/FASN) inhibitor. Desoxyrhaponticin (DC, DES) is also a competitive inhibitor of glucose uptake with IC50 of 148.3 μM and 30.9 μM in rabbit intestinal membrane vesicles and in rat everted gut sleeves, respectively. Desoxyrhaponticin has apoptotic effect on human cancer cells.
Nat Metab, 2021, 10.1038/s42255-021-00479-4
S3336 Heptadecanoic acid

Heptadecanoic acid (C17:0), an odd chain saturated fatty acid, significantly inhibits cell proliferation, and migration, while promoting apoptosis in PC‑9 and PC‑9/GR cells. Heptadecanoic acid is associated with several diseases, including the incidence of coronary heart disease, prediabetes and type 2 diabetes as well as multiple sclerosis.

S3357 Elaidic acid

Elaidic acid is a major trans fatty acid that inhibits cell viability, elevates cell apoptosis by enhancing oxidative stress. Elaidic acid can be used as a pharmaceutical solvent.

S3604 Triptolide (PG490) Triptolide (PG490, NSC 163062) is a diterpene triepoxide, immunosuppresive agent extracted from the Chinese herb Tripterygium wilfordii. It functions as a NF-κB inhibitor with dual actions by disruption of p65/CBP interaction and by reduction of p65 protein. Triptolide (PG490) abrogates the transactivation function of heat shock transcription factor 1 (HSF1). Triptolide inhibits MDM2 and induces apoptosis through a p53-independent pathway.
Sci Adv, 2021, 7(7)eabd2645
EMBO Rep, 2021, e52023
Acta Pharmacol Sin, 2021, 10.1038/s41401-021-00657-w
S3829 Isoalantolactone Isoalantolactone, one of the major sesquiterpene lactone compounds, is isolated from the roots of Anula helenium and possesses multiple biological activities including antifungal, anthelmintic, antimicrobial, anti-inflammatory, antitrypanosomal activities and antiproliferative effects on several cancer cell lines, such as colon, melanoma, ovary, prostate, lung, and leukemia. Isoalantolactone is an apoptosis inducer, which also acts as an alkylating agent.
S3984 Nordihydroguaiaretic acid (NDGA) Nordihydroguaiaretic acid (NDGA) is a phenolic antioxidant found in the leaves and twigs of the evergreen desert shrub, Larrea tridentata (Sesse and Moc. ex DC) Coville (creosote bush). It is a recognized inhibitor of lipoxygenase (LOX) and has antioxidant and free radical scavenging properties. Nordihydroguaiaretic acid (NDGA) is a cytotoxic insulin-like growth factor-I receptor (IGF-1R)/HER2 inhibitor and induces apoptosis. Nordihydroguaiaretic acid (NDGA) inhibits p300 and activates autophagy. Nordihydroguaiaretic acid (NDGA) protects cells from ferroptosis.
S4001 Cabozantinib malate (XL184) Cabozantinib malate (XL184) is the malate of Cabozantinib, a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret (c-Ret), Kit (c-Kit), Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM in cell-free assays, respectively. Cabozantinib malate (XL184) induces apoptosis.
Cancer Cell, 2021, S1535-6108(21)00659-0
Clin Cancer Res, 2021, 27(9):2533-2548
Cancers (Basel), 2021, 13(14)3635
S4269 Vinorelbine ditartrate (KW-2307) Vinorelbine Tartrate (KW-2307, Nor-5'-anhydrovinblastine ditartrate) is a semi-synthetic vinca alkaloid, and inhibits mitosis through interaction with tubulin. Vinorelbine Tartrate exhibits anti-tumor activities via inducing the mitotic apoptosis, autophagy and inflammation.
Cancer Res, 2021, canres.0955.2021
Br J Cancer, 2021, 10.1038/s41416-021-01420-y
J Neurochem, 2021, 156(5):642-657
S4423New Emamectin Benzoate Emamectin Benzoate (EMB, MK-244) activates gamma-amino butyric acid (GABA) transporter. Emamectin Benzoate induces of reactive oxygen species (ROS)-mediated DNA damage and apoptosis.
S4476New PCNA-I1 PCNA-I1 is a selective inhibitor of proliferating cell nuclear antigen (PCNA, a potential anticancer target). PCNA-I1 selectively binds to PCNA trimers with Kd of ~0.2 to 0.4 μM. PCNA-I1 inhibits the growth of tumor cells of various tissue types with IC50 of ~0.2 μM. PCNA-I1 induces DNA damage and apoptosis in both LNCaP and PC-3 cells. PCNA-I1 also induces autophagy in PC-3 cells.
S4505 Vinblastine (NSC-49842) sulfate Vinblastine sulfate (NSC49842, Vincaleukoblastine sulfate salt, 29060-LE, Exal, Velban, Velbe) inhibits microtubule formation and suppresses nAChR activity with IC50 of 8.9 μM in a cell-free assay, used to treat certain kinds of cancer. Vinblastine sulfate induces autophagy and apoptosis.
Nat Chem Biol, 2021, 10.1038/s41589-021-00751-4
Cancer Res, 2021, canres.0955.2021
Hum Cell, 2021, 10.1007/s13577-021-00579-z
S4613New Sodium Fluoride Sodium fluoride (NaF) induces apoptosis and autophagy via the endoplasmic reticulum (ER) stress pathway in MC3T3-E1 osteoblastic cells.
S4701 2-Deoxy-D-glucose (2-DG) 2-Deoxy-D-glucose (2-DG, 2-deoxyglucose, NSC 15193, 2-Deoxy-D-arabino-hexose, D-Arabino-2-deoxyhexose), an analog of glucose, is a glycolytic inhibitor with antiviral activity. 2-Deoxy-D-glucose induces apoptosis and inhibits Herpes Simplex Virus type-1 (HSV-1) receptor expression.
Nat Commun, 2021, 12(1):3258
Clin Cancer Res, 2021, clincanres.2092.2021
Autophagy, 2021, 1-19
S4732 MPTP hydrochloride MPTP hydrochloride is a dopaminergic neurotoxin and cause selective destruction of dopaminergic neurons in animal models of parkinsonism. MPTP hydrochloride induces apoptosis.
Neuropharmacology, 2021, 196:108360
J Neuroinflammation, 2020, 17(1):272
Brain Res Bull, 2020, 164:55-64
S5144 Neferine Neferine ((R)-1,2-Dimethoxyaporphine), a natural component of Nelumbo nucifera, has antitumor efficiency. Neferine induces apoptosis in renal cancer cells. Neferine prevents autophagy through activation of Akt/mTOR pathway and Nrf2 in muscle cells. Neferine strongly inhibits NF-κB activation. Neferine possesses a number of therapeutic effects such as anti-diabetic, anti-aging, anti-microbial, anti-thrombotic, anti-arrhythmic, anti-inflammatory and even anti-HIV.
Oncol Rep, 2020, 44(3):1116-1126
S5243 Ruxolitinib Phosphate Ruxolitinib Phosphate (INCB018424, INC424) is the phosphate salt form of Ruxolitinib. Ruxolitinib is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM in cell-free assays, >130-fold selectivity for JAK1/2 versus JAK3. Ruxolitinib kills tumor cells through toxic mitophagy. Ruxolitinib induces autophagy and enhances apoptosis.
Blood, 2022, blood.2021012366
Mol Neurodegener, 2022, 17(1):7
J Exp Clin Cancer Res, 2022, 41(1):10
S5248 Apatinib Apatinib (Rivoceranib, YN968D1) is a potent inhibitor of the VEGF signaling pathway with IC50 values of 1 nM, 13 nM, 429 nM and 530 nM for VEGFR-2, Ret (c-Ret), c-Kit and c-Src, respectively. Apatinib induces both autophagy and apoptosis.
Front Oncol, 2021, 11:739139
Biochem Biophys Res Commun, 2021, 586:177-184
Cells, 2020, 9(6):E1452
S5554 Lanatoside C Lanatoside C is a cardiac glycoside with antiviral and anti-tumor activity. Lanatoside C induces G2/M cell cycle arrest and induces autophagy and apoptosis via attenuating MAPK, Wnt, JAK-STAT, and PI3K/AKT/mTOR signaling pathways.
S5584 Citronellol Citronellol (Dihydrogeraniol, (±)-β-Citronellol), a constituent of rose and geranium oils, is used in perfumes and insect repellents. Citronellol can cause necrotic apoptosis of NCI-H1299 cells by up-regulating TNF-α, RIP1 / RIP3 activities, and down-regulating caspase-3 / caspase-8 activities. Citronellol also results in a biphasic increase in ROS production at 1 h and at 12 h in NCI-H1299 cells.
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