Description
DNA-PK Inhibitor III is a cell-permeable aryl-morpholino compound that is potent, selective, and an ATP-competitive inhibitor of DNA-PK (IC:50:= 120 nM) and PI 3-Kinase catalytic subunit p110β (IC:50:= 135 nM). Inhibits DNA-PK-mediated cellular DNA DSB (double strand break) repair (EC:50:= 68 µM) and enhances DSB-induced antitumor activity:in vitro:, while exhibiting no cytotoxic effects (up to 50 µM) in the absence of DSBs. Also inhibits PI 3K p110α, p110γ, and p110δ only at much higher concentrations (IC50= 1.4 µM, 880 nM, and 1.0 µM, respectively) and exhibits no effect against a panel of several other kinases, including, Cdk2, Src, PKA, PKC, Chk1, CK1, ATM, and FKBP12, even at concentrations as high as 100 µM