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Description

A cell-permeable disubstituted pyranone compound that acts as a potent and ATP-competitive inhibitor of ATM kinase (IC50 = 13 nM, Ki = 2.2 nM). Displays excellent selectivity over other PIKK family kinases (IC50 = 2.5, 9.3, 16.6 µ,M for DNA-PK, mTOR, PI 3-K, respectively, IC50 >100 µ,M for PI 4-K and ATR) and exhibits little activity towards a panel of 60 other kinases even at concentrations as high as 10 µ,M. Inhibits ATM-dependent cellular protein phosphorylation following ionizing radiation (IR) and sensitizes cells with wild-type ATM, but not mutant ATM, to the cytotoxic effects of IR and DNA-damaging agents.