Chk2 Inhibitor II (BML-277)

Description: Chk2 Inhibitor II (also known as BML-277) is an ATP-competitive inhibitor of Chk2 (checkpoint kinase 2) with an IC50 of 15 nM. It is 1000-fold more selective towards Chk2 than Chk1 and Cdk1/B kinases. BML-277 dose dependently protects human CD4+ and CD8+ T-cells from apoptosis due to ionizing radiation. It can efficiently rescue both T-cell populations from radiation-induced apoptosis in a dose-dependent manner with an observed EC50 of 3?7.6 uM. The concentration of BML-277 required for radioprotection is consistent with the biochemical measurement of chk2 inhibition.

References: J Med Chem. 2005 Mar 24; 48(6):1873-85; Nat Commun. 2011 Jul 19; 2:402.

Related CAS#:516480-80-1 (BML277 Acid, a metabolite of BML277)