Autophagy

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Catalog No. Product Name Information Product Use Citations Product Validations
S1013 Bortezomib (PS-341) Bortezomib (PS-341, Velcade, LDP-341, MLM341, NSC 681239) is a potent 20S proteasome inhibitor with Ki of 0.6 nM. It exhibits favorable selectivity towards tumor cells over normal cells. Bortezomib (PS-341) inhibits NF-κB and induces ERK phosphorylation to suppress cathepsin B and inhibit the catalytic process of autophagy in ovarian cancer and other solid tumors.
Mol Cell, 2022, S1097-2765(22)00433-6
Sci Immunol, 2022, 7(68):eabi6763
Sci Adv, 2022, 8(4):eabi7711
S1092 KU-55933 (ATM Kinase Inhibitor) KU-55933 (ATM Kinase Inhibitor) is a potent and specific ATM inhibitor with IC50/Ki of 12.9 nM/2.2 nM in cell-free assays, and is highly selective for ATM as compared to DNA-PK, PI3K/PI4K, ATR and mTOR. KU‑55933 (ATM Kinase Inhibitor) inhibits the activation of autophagy‑initiating kinase ULK1 and results in a significant decrease of autophagy.
Nat Commun, 2022, 13(1):360
Nucleic Acids Res, 2022, gkac375
Cancer Res, 2022, canres.2229.2021
S1102 U0126-EtOH U0126-EtOH is a highly selective inhibitor of MEK1/2 with IC50 of 0.07 μM/0.06 μM in cell-free assays, 100-fold higher affinity for ΔN3-S218E/S222D MEK than PD98059. U0126 inhibits autophagy and mitophagy with antiviral activity.
Adv Sci (Weinh), 2022, 10.1002/advs.202104055
Cell Rep, 2022, 38(11):110522
Elife, 2022, 11e76183
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
Adv Sci (Weinh), 2022, 10.1002/advs.202104055
Cancer Res, 2022, canres.2292.2021
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.
Sci Adv, 2022, 8(5):eabk0221
Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
J Med Chem, 2022, 65(5):4182-4200
S1113 GSK690693 GSK690693 is a pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 2 nM/13 nM/9 nM in cell-free assays, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes. GSK690693 also potently inhibits AMPK and DAPK3 from the CAMK family with IC50 of 50 nM and 81 nM, respectively. GSK690693 affects Unc-51-like autophagy activating kinase 1 (ULK1) activity, robustly inhibits STING-dependent IRF3 activation. Phase 1.
Am J Cancer Res, 2022, 12(4):1535-1555
Cell Death Discov, 2022, 8(1):197
Mech Ageing Dev, 2022, 202:111633
S1150 Paclitaxel (NSC 125973) Paclitaxel (NSC 125973, PTX, Taxol, Onxal, Abraxane) is a microtubule polymer stabilizer with IC50 of 0.1 pM in human endothelial cells.
Cell Res, 2022, 10.1038/s41422-022-00651-9
Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
Mol Cell, 2022, 82(1):75-89.e9
S1346 Heparin sodium Heparin sodium, a sulfated polysaccharide belonging to the family of glycosaminoglycans, has numerous important biological activities associated with its interaction with diverse proteins. Heparin is used as an anticoagulant primarily through its interaction with AT III by enhancing AT-IIImediated inhibition of blood coagulation factors, including thrombin and factor Xa. Heparin prevents the induction of autophagy.
Stem Cells Transl Med, 2022, 11(5):552-565
Dev Biol, 2022, 487:99-109
J Extracell Vesicles, 2021, 10(8):e12091
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.
Nature, 2022, 603(7899):159-165
Cell Res, 2022, 32(2):119-138
Autophagy, 2022, 1-20
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.
Cancer Cell, 2022, S1535-6108(21)00662-0
Cancer Res, 2022, 82(9):1789-1802
Leukemia, 2022, 10.1038/s41375-022-01565-6
S1490 Ponatinib (AP24534) Ponatinib (AP24534) is a novel, potent multi-target inhibitor of Abl, PDGFRα, VEGFR2, FGFR1 and Src with IC50 of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM and 5.4 nM in cell-free assays, respectively. Ponatinib (AP24534) inhibits autophagy.
Nat Commun, 2022, 13(1):2500
J Immunother Cancer, 2022, 10(1)e003766
Cell Rep, 2022, 39(4):110721
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
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):3117
Nat Commun, 2022, 13(1):50
J Pathol, 2022, 10.1002/path.5910
S1835 Azithromycin (CP-62993) Azithromycin (CP-62993, XZ-450) is an antibiotic by inhibiting protein synthesis, used for the treatment of bacterial infections.
J Cell Biochem, 2022, 10.1002/jcb.30213
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Hum Cell, 2021, 34(6):1911-1918
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
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 Immunol, 2022, 23(2):237-250
Nat Commun, 2022, 13(1):1017
Cell Mol Life Sci, 2022, 79(3):153
S2758 Wortmannin (KY 12420) Wortmannin (KY 12420, SL-2052, BRN 0067676, NSC 627609) is the first described PI3K inhibitor with IC50 of 3 nM in a cell-free assay, with little selectivity within the PI3K family. Wortmannin blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM in cell-free assays. Wortmannin also inhibits PLK1 activity.
Nat Commun, 2022, 13(1):2111
Cancer Res, 2022, canres.2292.2021
Cell Rep, 2022, 38(7):110373
S2767 3-Methyladenine (3-MA) 3-Methyladenine (3-MA, NSC 66389) is a selective PI3K inhibitor for Vps34 and PI3Kγ with IC50 of 25 μM and 60 μM in HeLa cells; blocks class I PI3K consistently, whereas suppression of class III PI3K is transient, and also blocks autophagosome formation. 3-Methyladenine (3-MA) is successfully used to suppress mitophagy. Solutions of 3-MA are best fresh-prepared by heating.
Bioact Mater, 2023, 19:690-702
Nature, 2022, 603(7899):159-165
Autophagy, 2022, 10.1080/15548627.2022.2055285
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.
Signal Transduct Target Ther, 2022, 7(1):97
Emerg Microbes Infect, 2022, 11(1):1135-1144
Front Cell Dev Biol, 2022, 10:817831
S2930 Pifithrin-μ Pifithrin-μ (NSC 303580, PFTμ, 2-Phenylethynesulfonamide) is a specific p53 inhibitor by reducing its affinity to Bcl-xL and Bcl-2, and also inhibits HSP70 function and autophagy.
J Biol Chem, 2022, 298(5):101875
Chin Med J (Engl), 2022, 135(5):606-618
Shock, 2021, 55(1):74-82
S3042 Purmorphamine Purmorphamine (Shh Signaling Antagonist VI), which directly binds and activates Smoothened, blocks BODIPY-cyclopamine binding to Smo with IC50 of ~ 1.5 μM in HEK293T cell and also is an inducer of osteoblast differentiation with EC50 of 1 μM. Purmorphamine can reduce both basal and induced autophagy.
Nat Commun, 2022, 13(1):1439
Adv Healthc Mater, 2022, e2200386
Oxid Med Cell Longev, 2022, 2022:9955677
S3233 Emetine hydrochloride Emetine hydrochloride (NSC 33669), a principal alkaloid extracted from the root of ipecac clinically used as an emetic and antiprotozoal drug, reduces HIFs (hypoxia-inducible factors; HIF-1α and HIF-2α), PDK1, RhoA, Rho-kinases (ROCK1 and ROCK2) and BRD4. Emetine hydrochloride inhibits cellular autophagy and has anti-malarial, anti-viral, anti-bacterial and anti-amoebic effect.
S3758 Sinomenine hydrochloride Sinomenine (SN, Cucoline, Kukoline, Sabianine A), extracted from the Chinese medicinal plant, sinomenium acutum, is a potent anti-inflammatory and neuroprotective agent.
Biomed Res Int, 2022, 2022:4914005
Cancer Manag Res, 2021, 13:1189-1204
Bioorg Med Chem, 2020, 31:115986
S4157 Chloroquine diphosphate Chloroquine diphosphate is a 4-aminoquinoline anti-malarial and anti-rheumatoid agent, also acting as an ATM activator. Chloroquine is also an inhibitor of toll-like receptors (TLRs).
Bioact Mater, 2022, 18:459-470
Phytomedicine, 2022, 98:153958
Bone, 2022, 154:116262
S4430 Hydroxychloroquine Sulfate (NSC 4375) Hydroxychloroquine Sulfate (NSC 4375, HCQ) is an antimalarial agent used for the treatment of systemic lupus erythematosus, rheumatoid arthritis and other autoimmune, inflammatory and dermatologic conditions. Also acts as an inhibitor of autophagy and toll-like receptor (TLR) 7/9.
Cell Rep, 2022, 39(3):110712
Cell Death Dis, 2022, 13(3):197
Neurosci Bull, 2022, 10.1007/s12264-022-00818-9
S4643 KB-R7943 mesylate KB-R7943 mesylate is a widely used inhibitor of the reverse Na+/Ca2+ exchanger (NCX(rev)) with IC50 of 5.7 μM. KB-R7943 mesylate promotes prostate cancer cell death by activating the JNK pathway and blocking autophagic flux.
S5920 CA-5f CA-5f is a potent late-stage macroautophagy/autophagy inhibitor via inhibiting autophagosome-lysosome fusion.
J Virol, 2021, JVI0155021
S5973 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.
S6471 Lucanthone Lucanthone is a novel autophagic inhibitor and also an orally available thioxanthone-based DNA intercalator and inhibitor of the DNA repair enzyme apurinic-apyrimidinic endonuclease 1.
Int J Mol Sci, 2021, 23(1)17
S6716 NSC 185058 NSC185058 inhibits ATG4B, the lipidation of LC3B, and autophagy without affecting the MTOR or PtdIns3K pathways.
S6912 Vacuolin-1 Vacuolin-1 is a potent and cell-permeable inhibitor that blocks the Ca(2+)-dependent exocytosis of lysosomes and prevents the release of lysosomal content without affecting the process of resealing. Vacuolin-1 is also a potent and selective PIKfyve inhibitor, and inhibits autophagy by impairing lysosomal maturation via PIKfyve inhibition.
S6999 Chloroquine (NSC-187208) Chloroquine (NSC-187208, Aralen, CHQ, CQ) is an antimalarial drug and autophagy/lysosome inhibitor. Chloroquine also suppresses Toll-like receptor-9 (TLR9) protein expression. Chloroquine is highly effective agianst SARS-CoV-2 (COVID-19) infection with EC50 of 1.13 μM in Vero E6 cells. Chloroquine has anti-HIV-1 activity.
Bioact Mater, 2022, 18:459-470
Redox Biol, 2022, 52:102292
Cell Death Dis, 2022, 13(2):150
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.
Nat Immunol, 2022, 23(3):431-445
Nat Cell Biol, 2022, 24(5):766-782
Front Cell Dev Biol, 2021, 9:769213
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, 2022, 24(5):766-782
Cell Mol Immunol, 2022, 10.1038/s41423-022-00841-w
PLoS One, 2022, 17(3):e0265805
S7146 DMH1 DMH1 is a selective BMP receptor inhibitor with IC50 of 107.9 nM for ALK2, exhibiting no inhibition on AMPK, ALK5, KDR (VEGFR-2) or PDGFR. DMH1 inhibits autophagy.
Atherosclerosis, 2022, 351:9-17
Nat Commun, 2021, 12(1):6374
Proc Natl Acad Sci U S A, 2021, 118(29)e2101783118
S7289 PFK15 PFK15 (PFK-015) is a potent and selective 6-phosphofructo-2-kinase (PFKFB3) inhibitor with IC50 of 207 nM.
J Exp Clin Cancer Res, 2022, 41(1):77
Cancer Lett, 2022, S0304-3835(22)00055-6
Autophagy, 2021, 1-19
S7381 Pepstatin A Pepstatin A (Pepstatin) is a potent aspartic protease inhibitor, and also inhibits HIV replication. Pepstatin A is also an inhibitor of cathepsins D and cathepsins E. Pepstatin A inhibits autophagy by suppressing lysosomal proteases.
J Immunother Cancer, 2022, 10(3)e004129
PLoS Pathog, 2022, 18(1):e1010204
Pharmacol Res, 2021, S1043-6618(21)00517-X
S7423 KN-93 Phosphate KN-93 Phosphate is a potent and specific inhibitor of Ca2+/calmodulin-dependent protein kinase II (CaMKII) with Ki of 0.37 μM, no remarkable inhibitory effects on APK, PKC, MLCK or Ca2+-PDE activities. KN-93 attenuates CaMKII-induced autophagy.
EMBO Rep, 2022, e53373
Commun Biol, 2022, 5(1):96
Nutr Neurosci, 2022, 1-19
S7455 Resatorvid (TAK-242) Resatorvid (TAK-242, CLI-095) is a small-molecule-specific inhibitor of Toll-like receptor (TLR) 4 signaling, blocking LPS-induced production of NO, TNF-α and IL-6 in macrophages with IC50 of 1.8 nM, 1.9 nM and 1.3 nM, respectively. Resatorvid downregulates expression of TLR4 downstream signaling molecules MyD88 and TRIF. Resatorvid inhibits autophagy.
Cell Death Dis, 2022, 13(4):333
Int J Cancer, 2022, 10.1002/ijc.34028
Sci Rep, 2022, 12(1):3056
S7660 Obeticholic Acid Obeticholic Acid (INT-747, 6-ECDCA, 6-Ethylchenodeoxycholic acid) is a potent and selective farnesoid X receptor (FXR) agonist with EC50 of 99 nM. Obeticholic Acid inhibits autophagy. Phase 3.
Nutrients, 2021, 13(3)940
Proc Natl Acad Sci U S A, 2020, 117(45):28263-28274
Nat Metab, 2020, 2(5):413-431
S7682 SAR405 SAR405 is a low-molecular-mass kinase inhibitor of PIK3C3/Vps34 (KD 1.5 nM) showing high selectivity and not be active up to 10 μM on class I and class II PI3Ks as well as on mTOR. SAR405 prevents autophagy and synergizes with MTOR (mechanistic target of rapamycin) inhibition in tumor cells.
Autophagy, 2022, 1-15
Autophagy, 2022, 10.1080/15548627.2022.2065617
Cell Death Dis, 2022, 13(4):398
S7683 PIK-III PIK-III (VPS34-IN2), which is a selective inhibitor of ​VPS34 enzymatic activity, inhibits autophagy and de novo lipidation of LC3 and leads to the stabilization of autophagy substrates. The IC50 values for VPS34 and PI(3)Kδ are 0.018 μM and 1.2 μM respectively.
Nat Commun, 2022, 13(1):83
Cell Death Dis, 2022, 13(4):398
Sci Adv, 2021, 7(40):eabj2485
S7751 VER155008 VER155008 (C07) is a potent Hsp70 family inhibitor with IC50 of 0.5 μM, 2.6 μM, and 2.6 μM in cell-free assays for HSP70, HSC70, and GRP78 (HSPA5, Bip), respectively, >100-fold selectivity over HSP90. VER155008 inhibits autophagy and causes reduced levels of HSP90 client proteins.
Exp Mol Med, 2022, 10.1038/s12276-022-00745-9
EMBO J, 2021, e106183
Oncogene, 2021, 10.1038/s41388-021-01914-2
S7811 MHY1485 MHY1485 is a potent, and cell-permeable mTOR activator, and also potently inhibits autophagy.
Hepatology, 2022, 75(6):1386-1401
Emerg Microbes Infect, 2022, 1-85
Front Pharmacol, 2022, 13:890974
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.
Cancer Cell, 2022, S1535-6108(21)00662-0
Mol Cell, 2021, S1097-2765(21)00729-2
Prog Neurobiol, 2021, S0301-0082(21)00137-4
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.
Autophagy, 2022, 1-20
Atherosclerosis, 2022, 343:10-19
J Clin Invest, 2021, 146893
S7948 MRT67307 HCl MRT67307 is a potent and dual IKKϵ and TBK1 inhibitor with IC50 of 160 and 19 nM, respectively. MRT67307 potently inhibits ULK1 and ULK2 and blocks autophagy.
Cancer Res, 2022, 82(10):1991-2002
Microbiol Spectr, 2022, e0219321
Cell, 2021, S0092-8674(21)00885-0
S7949 MRT68921 HCl MRT68921 is a potent and dual autophagy kinase ULK1/2 inhibitor with IC50 of 2.9 nM and 1.1 nM, respectively.
Mol Cell, 2021, 81(9):2013-2030.e9
Cell Rep, 2021, 36(13):109762
Front Pharmacol, 2021, 12:747975
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.
Cell Metab, 2022, S1550-4131(22)00054-7
Bone Res, 2022, 10(1):26
Cell Death Dis, 2022, 13(2):147
S8222 AS1842856 AS1842856 is a cell-permeable inhibitor that blocks the transcription activity of Foxo1 with IC50 of 33 nM. It could directly bind to the active Foxo1, but not the Ser256-phosphorylated form. AS1842856 suppresses autophagy.
Nucleic Acids Res, 2022, gkac179
Int J Mol Sci, 2022, 23(10)5728
J Agric Food Chem, 2022, 10.1021/acs.jafc.1c07483
S8274 STO-609 STO-609 is a specific inhibitor of the Ca2+/Calmodulin-dependent protein kinase kinase(CaM-KK) that inhibits the activities of recombinant CaM-KKα and CaM-KKβ isoforms, with Ki values of 80 and 15 ng/ml, respectively, and also inhibits their autophosphorylation activities. STO-609 inhibits AMPKK activity and inhibits autophagy.
EMBO Rep, 2022, e53373
Cell Res, 2021, 10.1038/s41422-021-00565-y
Autophagy, 2021, 1-14
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
Exp Ther Med, 2021, 21(6):581
Mol Med Rep, 2021, 24(2)592
S8369 Lys05 Lys05 is a new lysosomal autophagy inhibitor which potently accumulates within and deacidifies the lysosome of both cells and tumors, resulting in sustained inhibition of autophagy and tumor growth.
Blood Cancer J, 2021, 11(6):111
Surgery, 2021, S0039-6060(21)00795-9
Environ Toxicol, 2021, 10.1002/tox.23355
S8527 ROC-325 ROC-325 is an orally available novel inhibitor of lysosomal-mediated autophagy which diminishes AML cell viability with the IC50 range of 0.7-2.2 μM.
S8576 EAD1 EAD1 is a potent autophagy inhibitor with an IC50 of 5.8 μM in the BxPC3 cells. It has antiproliferative activities in lung and pancreatic cancer cells.
Mol Cancer Ther, 2022, 21(1):79-88
Autophagy, 2021, 1-17
S8596 Autophinib Autophinib is a potent autophagy inhibitor with a novel chemotype with IC50 values of 90 and 40 nM for autophagy in starvation induced autophagy assay and rapamycin induced autophagy assay. The IC50 value for Vps34 is 19 nM in vitro.
Nat Genet, 2021, 53(4):435-444
J Agric Food Chem, 2021, 69(40):11847-11855
J Steroid Biochem Mol Biol, 2021, 209:105826
S8744 PHY34 PHY34 is a late-stage autophagy inhibitor with nanomolar potency and significant antitumor efficacy as a single agent against HGSOC in vivo.
S8764 IITZ-01 IITZ-01 is a potent autophagy inhibitor, enhancing autophagosome accumulation but inhibiting autophagosomal degradation by impairing lysosomal function.
Cancers (Basel), 2020, 12(9):E2363
S8793 ULK-101 ULK-101 is a potent and selective ULK1 inhibitor with IC50 values of 8.3 nM and 30 nM for ULK1 and ULK2, respectively.
Biochim Biophys Acta Mol Cell Res, 2022, S0167-4889(22)00076-3
Mol Immunol, 2022, 147:1-9
J Virol, 2021, JVI0155021
S8807 PFK158 PFK158 is a potent and selective inhibitor of PFKFB3. It has improved PK properties and causes ~80% growth inhibition in several mouse models of human-derived tumors.
Front Oncol, 2022, 12:826655
Front Immunol, 2021, 12:669456
Cancer Metab, 2021, 9(1):33
S8808 DC661 DC661 is capable of deacidifying the lysosome and inhibiting autophagy significantly better than hydroxychloroquine (HCQ). DC661 induces apoptosis.
J Neurochem, 2022, 10.1111/jnc.15606
FEBS J, 2022, 10.1111/febs.16447
Biomed Pharmacother, 2022, 145:112432
S9150 Daurisoline Daurisoline, a bis-benzylisoquinoline alkaloid isolated from the rhizomes of Menispermum dauricum, is a potent autophagy blockers with antiarrhythmic effects.
S9424 Liensinine diperchlorate Liensinine, a major isoquinoline alkaloid, inhibits late-stage autophagy/mitophagy through blocking autophagosome-lysosome fusion. It is a novel autophagy/mitophagy inhibitor.
S0012 E260 E260 (Fer and FerT inhibitor E260) is a Fer kinase and FerT inhibitor that selectively evokes metabolic stress in cancer cells by imposing mitochondrial dysfunction and deformation, and onset of energy-consuming autophagy which decreases the cellular ATP level.
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.
Drug Dev Res, 2022, 10.1002/ddr.21927
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.
Signal Transduct Target Ther, 2022, 7(1):51
Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
Cell Death Differ, 2022, 10.1038/s41418-022-00995-0
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.
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Cell Rep Med, 2022, 3(1):100492
Cancer Lett, 2021, 507:80-88
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(11):1943-1959.e21
Cell, 2022, 185(1):169-183.e19
Mol Cell, 2022, S1097-2765(22)00085-5