MK-8776 (SCH 900776)

Description: MK-8776 (also known as SCH 900776) is a novel, highly potent and selective Chk1 (cell cycle checkpoint kinase 1) inhibitor with IC50 of 3 nM in a cell-free assay. It shows 500-fold selectivity against Chk2. SCH900776 (MK-8776) is an agent with potential radiosensitization and chemosensitization activities. MK-8776 specifically binds to and inhibits Chk1, which may result in tumor cells bypassing Chk1-dependent cell cycle arrest in the S and G2/M phases to undergo DNA repair prior to entry into mitosis; tumor cells may thus be sensitized to the DNA-damaging effects of ionizing radiation and alkylating chemotherapeutic agents.

References: Mol Cancer Ther. 2011 Apr; 10(4):591-602.

Related CAS#: 891494-64-7 (S-isomer); 891494-63-6 (free base)