V158411

V158411 is a potent and selective small molecule inhibitor of checkpoint kinase 1 (Chk1) and checkpoint kinase 2 (Chk2), developed as an ATP-competitive inhibitor. It demonstrates nanomolar potency against Chk1 and Chk2 while showing high selectivity over other kinases such as CDK1. The drug abrogates DNA damage-induced cell cycle arrest by inhibiting Chk1 autophosphorylation and enhances the cytotoxicity of various chemotherapeutic agents—particularly in p53-deficient cancer cell lines—by increasing DNA damage and promoting apoptosis or permanent cell cycle arrest. In preclinical models including human colon tumor xenografts in mice, V158411 potentiated the anti-tumor activity of irinotecan without additional systemic toxicity. Its mechanism involves induction of replication stress-associated DNA damage responses leading to increased cancer cell death[1][3][6].

Other names

1174664-88-01-Benzyl-N-(5-{5-[3-(Dimethylamino)-2,2-Dimethylpropoxy]-1h-Indol-2-Yl}-6-Oxo-1,6-Dihydropyridin-3-Yl)-1h-Pyrazole-4-CarboxamideSCHEMBL950079SCHEMBL-950079SCHEMBL 950079BCP25319BCP-25319BCP 25319HY-18942HY18942HY 18942CS-0014655CS0014655CS 0014655Q27455647Q-27455647Q 27455647