VER-158411 (V-158411) is a potent, selective, ATP-competitive Chk1 and Chk2 inhibitor with IC50 of 4.4 nM and 4.5 nM, respectively.
VER-158411 dispalys >1,000-fold selectivity over CDK1.
VER-158411 reduces pChk1 (S296) and pChk2 (S516) levels in a concentration dependent fashion in cells treated with etoposide with IC50s of 48 nM for Chk1 and 904 nM for Chk2.
VER-158411 potentiates the cytotoxicity of chemotherapeutic agents in a variety of p53 deficient human tumor cell lines (GI50=0.5-9.5 uM) and human colon tumor xenograft models.
