| E1051 |
MRTX1133
|
MRTX1133 is a highly selective inhibitor of mutant KRAS G12D and can reversibly binds to the activated and inactivated KRAS G12D mutants and inhibit their activity. The specificity of MRTX1133 to KRAS G12D is more than 1000 times that of wild-type KRAS.
|
| E1068 |
Nab-Paclitaxel
|
Nab-Paclitaxel is a novel solvent-free paclitaxel in which the binding ratio of paclitaxel to human albumin is approximately 1:9. It is an anti-microtubule drug that promotes microtubule aggregation in tubulin dimers and inhibits microtubule depolymerization to stabilize the microtubule system. Solutions are unstable and should be fresh-prepared. |
| E1386 |
KP-457
|
KP-457 (TNF-α-converting enzyme) is a selective inhibitor of ADAM17 with IC50 of 11.1 nM/L (cell-free assay). It also cleaves various molecules such as GPIbα, GPV, and TNF-α. |
| E1490 |
IAG933
|
IAG933 (YAP-TEAD-IN-3) is a small molecule and acts as a YAP/TAZ-TEAD inhibitor. It also inhibits NCI-H2052 and can be used in research of tumor invasion and metastatic spread of solid tumors. |
| E1597 |
RMC-6236 (Daraxonrasib)
|
Daraxonrasib (RMC-6236) is a RAS(ON) multi-selective noncovalent inhibitor of the active, GTP-bound state of both mutant and wild-type variants of canonical RAS isoforms with broad therapeutic potential. RMC-6236 exhibits strong anticancer efficacy in RAS-addicted cell lines, especially those with mutations at codon 12 of KRAS. |
| E1858 |
RMC-7977
|
RMC-7977 is a potent, reversible, tri-complex oral inhibitor that selectively targets active (GTP-bound) forms of KRAS, HRAS, and NRAS, which exhibits broad-spectrum activity against both mutant and wild-type variants (a RASMULTI (ON) inhibitor). It also exhibits significant anti-tumor efficacy in pancreatic ductal adenocarcinoma (PDAC). |
| E1962 |
Zoldonrasib (RMC-9805)
|
Zoldonrasib (RMC-9805) is an orally active inhibitor of KRAS G12D. RMC-9805 inhibits RAS signaling, leading to apoptosis in cancer cells with the KRAS G12D mutation. |
| P1205 |
GsMTx4
|
GsMTx4 (Grammostola spatulata mechanotoxin 4, M-theraphotoxin-Gr1a, M-TRTX-Gr1a) is a spider venom peptide that inhibits cationic mechanosensitive channels (MSCs) belonging to the Piezo and TRP channel families. |
| S1001 |
Navitoclax (ABT-263)
|
Navitoclax (ABT-263) is a potent inhibitor of Bcl-xL, Bcl-2 and Bcl-w with Ki of ≤ 0.5 nM, ≤1 nM and ≤1 nM in cell-free assays, but binds more weakly to Mcl-1 and A1. Phase 2. |
| S1045 |
TSA (Trichostatin A)
|
TSA (Trichostatin A) is an HDAC inhibitor with IC50 of ~1.8 nM in cell-free assays. |
| S1049 |
Y-27632 Dihydrochloride
|
Y-27632 2HCl is a selective ROCK1 and ROCK2 inhibitor with a Ki of 140 nM and 300nM in a cell-free assay, exhibits >200-fold selectivity over other kinases, including PKC, cAMP-dependent protein kinase, MLCK and PAK. |
| S1067 |
SB431542
|
SB431542 is a potent and selective inhibitor of ALK5 with IC50 of 94 nM in a cell-free assay, 100-fold more selective for ALK5 than p38 MAPK and other kinases. |
| S1077 |
SB202190
|
SB202190 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. |
| S1078 |
MK-2206 Dihydrochloride
|
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. |
| 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. |
| 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. |
| S1180 |
XAV-939
|
XAV-939 (NVP-XAV939) selectively inhibits Wnt/β-catenin-mediated transcription through tankyrase1/2 inhibition with IC50 of 11 nM/4 nM in cell-free assays, regulates axin levels and does not affect CRE, NF-κB or TGF-β. |
| S1263 |
CHIR-99021 (Laduviglusib)
|
Laduviglusib (CHIR-99021, CT99021) is a GSK-3α and GSK-3β inhibitor with IC50 of 10 nM and 6.7 nM, respectively. CHIR99201 does not exhibit cross-reactivity against cyclin-dependent kinases (CDKs) and shows a 350-fold selectivity toward GSK-3β compared to CDKs. CHIR99021 functions as a Wnt/β-catenin activator and induces autophagy. |
| 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. |
| S1459 |
Thiazovivin (TZV)
|
Thiazovivin is a novel ROCK inhibitor with IC50 of 0.5 μM in a cell-free assay, promotes hESC survival after single-cell dissociation. |
| S1536 |
CP-673451
|
CP-673451 is a selective inhibitor of PDGFRα/β with IC50 of 10 nM/1 nM in cell-free assays, exhibits >450-fold selectivity over other angiogenic receptors, has antiangiogenic and antitumor activity. |
| S1786 |
Verteporfin
|
Verteporfin 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. |
| S2215 |
DAPT
|
DAPT 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. |
| S2230 |
Galunisertib (LY2157299)
|
Galunisertib (LY2157299) is a potent TGFβ receptor I (TβRI) inhibitor with IC50 of 56 nM in a cell-free assay. Phase 2/3. |
| S2619 |
MG132
|
MG132 ((S,R,S)-(-)-MG132, Z-Leu-D-Leu-Leu-al) is a potent proteasome (ChTL, TL, and PGPH) inhibitor. MG132 also inhibits calpain (IC50=1.2 μM). MG132 can be used to induce animal models of Parkinson’s disease.
|
| S4592 |
SBE-β-CD
|
SBE-β-CD is a novel, chemically modified cyclodextrin with a structure designed to optimize the solubility and stability of drugs. |
| S6702 |
Tween 80
|
Tween 80 is a polysorbate surfactant used for selective protein extraction and the isolation of nuclei from mammalian cell lines. Tween 80 has been used in drug vehicle solutions for specific injections in mice and rats. It has been used for the determination of esterase activity in bacterial cells. |
| S6965 |
Bavdegalutamide (ARV-110)
|
Bavdegalutamide (ARV-110) is an orally bioavailable, specific androgen receptor (AR) PROTAC degrader that leads to ubiquitination and degradation of AR. ARV-110 completely degrades androgen receptor (AR) in all cell lines tested with DC50 of < 1 nM. ARV-110 can be used for the research of prostate cancer. |
| S7023 |
Z-VAD-FMK
|
Z-VAD-FMK (Z-VAD(OMe)-FMK) is a cell-permeable, irreversible pan-caspase inhibitor, blocks all features of apoptosis in THP.1 and Jurkat T-cells. |
| S7037 |
Wnt-C59 (C59)
|
Wnt-C59 (C59) is a PORCN inhibitor for Wnt3A-mediated activation of a multimerized TCF-binding site driving luciferase with IC50 of 74 pM in HEK293 cells. |
| S7086 |
IWR-1-endo
|
IWR-1-endo (endo-IWR 1, IWR-1) is a Wnt pathway inhibitor with IC50 of 180 nM in L-cells expressing Wnt3A, induces Axin2 protein levels and promotes β-catenin phosphorylation by stabilizing Axin-scaffolded destruction complexes. |
| S7110 |
(+)-JQ1
|
(+)-JQ1 is a BET bromodomain inhibitor, with IC50 of 77 nM/33 nM for BRD4(1/2) in cell-free assays, binding to all bromodomains of the BET family, but not to bromodomains outside the BET family. (+)-JQ1 suppresses cell proliferation via inducing autophagy. (+)-JQ1 inhibits the expression of Nuclear receptor binding SET domain protein 3 (NSD3) target genes. |
| S7120 |
3-Deazaneplanocin A (DZNep) Hydrochloride
|
DZNeP (3-deazaneplanocin A) HCl, an analog of adenosine, is a competitive inhibitor of S-adenosylhomocysteine hydrolase with Ki of 50 pM in a cell-free assay. |
| S7223 |
RepSox (E-616452)
|
RepSox (E-616452, SJN 2511, ALK5 Inhibitor II) is a potent and selective inhibitor of the TGFβR-1/ALK5 with IC50 of 23 nM and 4 nM for ATP binding to ALK5 and ALK5 autophosphorylation in cell-free assays, respectively. |
| S7242 |
Erastin
|
Erastin is a ferroptosis activator by acting on mitochondrial VDAC, exhibiting selectivity for tumor cells bearing oncogenic RAS. Solutions are unstable and should be fresh-prepared. |
| S7311 |
Q-VD-Oph
|
Q-VD-Oph (Quinoline-Val-Asp-Difluorophenoxymethylketone) is a potent pan-caspase inhibitor with IC50 ranged from 25 to 400 nM for caspases 1,3,8, and 9. Q-VD-OPh can inhibits HIV infection. |
| S7417 |
Puromycin Dihydrochloride
|
Puromycin 2HCl is an aminonucleoside antibiotic derived from Streptomyces alboniger. It is an inhibitor of protein synthesis and has been used to study transcription regulatory mechanisms that control the sequential and coordinated expression of genes during cell differentiation. |
| S7418 |
Cycloheximide
|
Cycloheximide, an antifungal antibiotic, is an eukaryote protein synthesis inhibitor with IC50 of 532.5 nM and 2880 nM for protein synthesis and RNA synthesis in vivo, respectively. Cycloheximide suppresses ferroptosis and inhibits autophagy.Cycloheximide (NSC-185) can be used to induce animal models of Dysmnesia.Solutions are unstable and should be fresh-prepared.This product is a hazardous chemical (acute toxicity/flammable/skin corrosive). Please use it while wearing a protective face mask, gloves, and clothing. |
| S7655 |
Telaglenastat (CB-839)
|
Telaglenastat (CB-839) is a potent, selective, and orally bioavailable glutaminase inhibitor with IC50 of 24 nM for recombinant human GAC. CB-839(Telaglenastat) inudces autophagy and has antitumor activity. Phase 1. |
| S7692 |
A-83-01
|
A-83-01 is a potent inhibitor of TGF-β type I receptor (ALK5-TD) with IC50 of 12 nM. A-83-01 also inhibits the transcription induced by activin/nodal type I receptor (ALK4-TD) and nodal type I receptor (ALK7-TD) with IC50 of 45 nM and 7.5 nM, respectively.Solutions are unstable and should be fresh-prepared. |
| S7693 |
Ceralasertib (AZD6738)
|
Ceralasertib (AZD6738) is an orally active, and selective ATR kinase inhibitor with IC50 of 1 nM. Phase 1/2.
|
| S7699 |
Liproxstatin-1
|
Liproxstatin-1 is a potent ferroptosis inhibitor with an IC50 of 22 nM. |
| S7775 |
Emricasan (IDN-6556)
|
Emricasan (IDN-6556, PF 03491390, PF-03491390) is a potent irreversible pan-caspase inhibitor. Emricasan is an inhibitor of Zika virus infection. |
| S7791 |
PMA (Phorbol 12-myristate 13-acetate)
|
PMA (Phorbol 12-myristate 13-acetate), a potent activator of PKC, is active at nanomolar concentrations. Phorbol 12-myristate 13-acetate (PMA) induces sphingosine-1-phosphate (S1P).PMA has strong excitability on the skin and mucous membrane. Special protection is required when using PMA. Wear gloves and mask to avoid direct contact in any way. |
| S7858 |
Dibutyryl cAMP (Bucladesine) sodium
|
Bucladesine sodium is a cell-permeable PKA activator by mimicing the action of endogenous cAMP. Dibutyryl-cAMP (Bucladesine) is also a phosphodiesterase (PDE) inhibitor. |
| S8586 |
Nedisertib (M3814)
|
Nedisertib (M3814, Peposertib, MSC2490484A) is an orally bioavailable, highly potent and selective inhibitor of DNA activated protein kinase (DNA-PK) with IC50 of < 3 nM. |
| S8874 |
PLX5622
|
PLX5622 is a highly selective CSF-1R inhibitor (IC50 < 10 nmol/L), showing > 20-fold selectivity over KIT and FLT3. |
| S8877 |
IKE (Imidazole Ketone Erastin)
|
IKE(Imidazole ketone erastin) is a potent, selective, and metabolically stable system xc– inhibitor and inducer of ferroptosis. |
| S9870 |
STM2457
|
STM2457 is a highly potent and selective first-in-class catalytic inhibitor of RNA Methyltransferase METTL3 with an IC50 of 16.9 nM. STM2457 is highly specific for METTL3 and showed no inhibition of other RNA methyltransferases. |
| S9875 |
Saruparib (AZD5305)
|
Saruparib (AZD5305) is a highly selective and potent inhibitor of PARP1 with an IC50 of 3 nM in wild-type A549 lung cancer cells. AZD5305 shows no or minimal growth inhibitory effects in other cells (IC50s >10μM). |