BML-277 (516480-79-8) is a potent selective inhibitor of Chk2 (IC50 = 15 nM). BML-277 has been screened against a panel of 35 kinases, and shows less that 25% inhibition of any other kinase at 10 μM, demonstrating the selectivity1. Also displays radioprotective activity, preventing apoptosis in human T-cells that were subjected to ionizing radiation (EC50 = 3.0-7.6 μM).
1) Arienti et al. (2005), Checkpoint kinases inhibitors: SAR and radioprotective properties of a series of 2-arylbenzimidazoles; J. Med. Chem., 48 1873
2) Pereg et al. (2006), Differential roles of ATM- and Chk2-mediated phosphorylations of Hdmx in response to DNA damage; Mol. Cell. Biol., 26 6819