Checkpoint kinase 1 (Chk1) regulates S and G2-M phase cell cycle checkpoints in response to DNA damage. SCH 900776 is a functionally selective inhibitor of Chk1 (Kd = 2 nM, IC50 = 3 nM). In comparison, 18-fold and 500-fold higher concentrations of this compound are required to inhibit CDK2 and Chk2. At 5-50 mg/kg,...

Soluble in DMSO or ethanol. SCH900776 is a selective Chk1 inhibitor with an IC(50) of 3nM. It shows 50-fold selectivity for Chk1 versus Chk2. Target: Chk1 , Kinase Group: CAMK , Substrate: Serine-Threonine

SCH-900776 is an inhibitor of CHK1 that exhibits anticancer activity. SCH-900776 may also exhibit chemotherapeutic benefit as it is currently in clinical trials as a potential co-administered treatment for cancer. With other chemotherapeutics, SCH-900776 induces ds DNA strand breaks and cell death.

Description: SCH900776 (MK-8776) is an agent targeting cell cycle checkpoint kinase 1 (Chk1) with potential radiosensitization and chemosensitization activities. Target: Chk, CDK. Smiles: Cn1cc(cn1)-c1cnn2c(N)c(Br)c(nc12)[C@@H]1CCCNC1. References: Guzi TJ, et al. Mol Cancer Ther, 2011, 10(4), 591-602.