Chk2 inhibitor II

Chk2 Inhibitor II (BML-277) is a potent, cell-permeable, and ATP-competitive small molecule inhibitor of checkpoint kinase 2 (Chk2). It exhibits high selectivity for Chk2, with an IC50 of 15 nM and a Ki of 37 nM, demonstrating approximately 1000-fold greater potency over related kinases such as Chk1, Cdk1/B, and CK1. Chk2 is a key serine/threonine kinase involved in the DNA damage response, cell cycle control, and apoptosis. By inhibiting Chk2, BML-277 can modulate DNA repair pathways and has been shown to protect human CD4+ and CD8+ T-cells from ionizing radiation-induced apoptosis. This compound is widely utilized as a research tool to investigate the biological functions of Chk2 and the cellular response to DNA damage, although it is not approved for clinical use or human administration.

Other names

2-(4-(4-chlorophenoxy)phenyl)-1H-benzimidazole-5-carboxamide