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Description

A potent, selective, reversible, and ATP-competitive inhibitor of DNA-PK (IC50 = 0.27 µ,M). Inhibits the PI 3-K catalytic subunit p110-isozymes at higher concentrations (IC50 = 32 µ,M, 3.7 µ,M, 22 µ,M and ~100 µ,M for alpha, beta, delta and gamma, respectively). Only weakly inhibits a panel of several other kinases, including, ATM, ATR, CK2, GRK2, mTOR, PI-3KC2alpha, PI-3KC2beta, PI-3KC2gamma and PI-4Kbeta, even at concentrations as high as 50 µ,M., A morpholino-benzophenone compound that acts as a potent, selective, reversible, and ATP-competitive inhibitor of DNA-PK (IC50 = 270 nM). Inhibits PI 3-K catalytic subunit p110-isozymes at higher concentrations (IC50 = 32 µ,M, 3.7 µ,M, 22 µ,M and ~ 100 µ,M for alpha, beta, delta and gamma, respectively) and weakly inhibits a panel of several other kinases, including, ATM, ATR, CK2, GRK2, mTOR, PI 3KC2alpha, PI 3KC2beta, PI 3KC2gamma and PI 4Kbeta, even at concentrations as high as 50 µ,M.