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Chk Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
E1991New BBI-355 BBI-355 is an oral, potent, and selective small molecule inhibitor of CHK1 with an IC50 of 0.3 nM. It demonstrates significant anti-tumor activity as a single agent and in combination with targeted therapies in multiple ecDNA+ oncogene amplified tumor models.
E1653 CCT241533 hydrochloride CCT241533 hydrochloride is an ATP competitive, potent, and selective inhibitor of CHK2 with an IC50 of 3 nM and a Ki of 1.16 nM and shows minimal cross-reactivity against a panel of kinases. CCT241533 inhibits CHK2 activity in human tumor cell lines when subjected to DNA damage.
S7740 SAR-020106 SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC50 of 13.3 nM.
E5832New BBI-2779 BBI-2779 is a potent, selective, and orally active inhibitor of CHK1 with an IC50 of 0.3 nM. It preferentially kills cancer cells containing extrachromosomal DNA (ecDNA) by inducing replication stress and cell death. In gastric cancer models with FGFR2 gene amplification on ecDNA, BBI-2779 suppresses tumor growth and prevents drug resistance.
E1667 LY2880070 LY2880070 is an orally active inhibitor of CHK1. This compound can be used as an anticancer agent and shows promise in preclinical models of pancreatic ductal adenocarcinoma (PDAC) when used in combination with DNA-damaging agents.
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). This compound is also a novel G2 checkpoint abrogator. It induces apoptosis.
iScience, 2025, 28(5):112292
Signal Transduct Target Ther, 2024, 9(1):181.
Nat Commun, 2024, 15(1):2089
S9639 VX-803 (M4344) VX-803 (M4344, ATR inhibitor 2) is an ATP-competitive, orally active, and selective inhibitor of ataxia telangiectasia and Rad3 related (ATR) kinase with Ki of < 150 pM. This compound potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (P-Chk1) phosphorylation with IC50 of 8 nM. It exhibits potential antineoplastic activity.
Mol Syst Biol, 2025, 21(3):231-253
iScience, 2025, 28(3):111943
Nat Biomed Eng, 2024, 10.1038/s41551-024-01277-5
S6740 DB07268 DB07268 is a potent and selective JNK1 inhibitor with an IC50 value of 9 nM and exhibits at least 70- to 90-fold greater potency against JNK1 than CHK1, CK2, and PLK.
S3224 Cinobufagin Cinobufagin (Cinobufagine), an active ingredient of Venenum Bufonis, inhibits tumor development. This compound increases ATM and Chk2 and decreases CDC25C, CDK1, and cyclin B. It inhibits PI3K, AKT and Bcl-2 while increases levels of cleaved caspase-9 and caspase-3. Thus, this chemical induces cell cycle arrest at the G2/M phase and apoptosis.