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Selective PTEFb/CDK9 inhibitor
Atuveciclib, also known as BAY1143572, is a highly selective, potent and orally available inhibitor of PTEFb/CDK9 currently in Phase I.- Cole Schonhofer, .et al. , Biochem Pharmacol, 2021, Apr;186:114462 PMID: 33577894
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Chk1 inhibitor
GDC-0575 (ARRY-575, RG7741) is a potent and selective CHK1 inhibitor with an IC50 of 1.2?nM. -
CDK inhibitor
PF-06873600 is an orally bioavailable, cyclin-dependent kinase (CDK) inhibitor, with potential antineoplastic activity.- Abeer J Al-Qasem, .et al. , NPJ Precis Oncol, 2022, Sep 24;6(1):68 PMID: 36153348
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CDK7 inhibitor
ICEC0942, also known as CT7001, is an Orally Bioavailable Selective Inhibitor of CDK7 for Cancer Treatment. It selectively inhibits CDK7, with an IC50 of 40nM; IC50 values for CDK1, CDK2, CDK5 and CDK9 were 45-, 15-, 230- and 30-fold higher. -
SRE activation inhibitor
CCG-203971 is an inhibitor of SRE activation in the prostate cancer cell line PC-3 (IC50 = 6.4 μM), with 87% inhibition of SRE activation achieved at 100 μM. -
Rac1 inhibitor
1A-116 is a specific Rac1 inhibitor, can prevent EGF-induced Rac1 activation and block Rac1-P-Rex1 interaction. 1A-116 can induce apoptosis and inhibit cell proliferation, migration and cycle progression in a concentration-dependent manner. 1A-116 also demonstrates a high antimetastatic activity in vivo.
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CDK4/6 inhibitor
Trilaciclib is a potential first-in-class short-acting CDK4/6 inhibitor in development to preserve hematopoietic stem cells and enhance immune system function during chemotherapy. -
CDK8 inhibitor
SEL120-34A is a potent and selective CDK8 inhibitor active in AML cells with high levels of serine phosphorylation of STAT1 and STAT5 transactivation domains. -
Ras inhibitor
Antineoplaston A 10 is a Ras inhibitor potentially for the treatment of glioma, lymphoma, astrocytoma and breast cancer. -
pan-RAS inhibitor
Ras-IN-3144 is a pan-RAS inhibitor which inhibits RAS signaling pathways in cancer cells and prevents the growth of RAS mutant mouse cancer xenografts. -
CDK inhibitor
Lerociclib (G1T38) is a potent and selective inhibitor of CDK4/6, with IC50s of 1 nM, 2 nM for CDK4/CyclinD1 and CDK6/CyclinD3, respectively. -
RAD51 inhibitor
AD51 Inhibitor B02 (B02) is an inhibitor of human RAD51 with an IC50 of 27.4 μM. -
ATP-competitive STK19 inhibitor
ZT-12-037-01 is a potent, selective, ATP-competitive STK19 inhibitor. ZT-12-037-01 effectively blocks oncogenic NRAS-driven melanocyte malignant transformation and melanoma growth in vitro and in vivo. -
CDK4/CDK6 inhibitor
Abemaciclib Metabolites M2 is a metabolite of abemaciclib, acts as a potent CDK4 and CDK6 inhibitor, with IC50s in the range of 1-3 nM. Anti-cancer activity. -
KRAS G12C inhibitor
KRAS G12C inhibitor 17 is a potent KRAS G12C inhibitor extracted from patent WO2019110751A1, compound 82, has an IC50 of 5 nM. -
KRAS G12C inhibitor
KRAS G12C inhibitor 16 is a potent KRAS G12C inhibitor extracted from patent WO2019110751A1, compound 39, has an IC50 of 97 nM. -
KRAS G12C inhibitor
KRAS G12C inhibitor 15 is a potent KRAS G12C inhibitor extracted from patent WO2019110751A1, compound 22, has an IC50 of 5 nM. -
CDK4/CDK6 inhibitor
CDK4/6-IN-2 is a potent CDK4 and CDK6 inhibitor with IC50s of 2.7 and 16 nM for CDK4 and CDK6, respectively. -
KRAS G12C covalent inhibitor
AMG-510 is a potent, orally bioavailable, and selective KRAS G12C covalent inhibitor with anti-tumor activity. -
KRas G12C inhibitor
KRAS G12C inhibitor 5 is a KRas G12C inhibitor extracted from patent WO2017201161A1, Compound example 147. -
CDK14 inhibitor
FMF-04-159-2 is a covalent CDK14 inhibitor. FMF-04-159-2 inhibits CDK14 and CDK2 with IC50s of 39.6 nM and 256 nM in NanoBRET assay, respectively. -
ROCK1/ROCK2 inhibitor
ROCK inhibitor-2 is a selective dual ROCK1 and ROCK2 inhibitor with IC50s of 17 nM and 2 nM, respectively. -
KRAS G12C covalent inhibitor
AMG-510 is a potent, orally bioavailable, and selective KRAS G12C covalent inhibitor with anti-tumor activity.