DNA-PK抑制剂III是一种细胞可渗透的芳基吗啉类化合物，是一种有效的、选择性的DNA-PK (IC|50|= 120 nM)和PI 3-激酶催化亚单位p110β (IC|50|= 135 nM)的ATP竞争性抑制剂。抑制DNA-PK介导的细胞DNA DSB(双链断裂)修复(EC|50|= 68μM)并增强DSB诱导的抗肿瘤活性|体外|，同时在不存在DSB的情况下不显示细胞毒性作用(高达50μM)。也仅在高得多的浓度下抑制PI 3K p110α、p110γ和p110δ(IC50分别为1.4 μM, 880 nM, and 1.0 μM),并且对包括Cdk2、Src、PKA、PKC、Chk1、CK1、ATM和FKBP12在内的其他几种激酶没有作用，甚至在高达100 μM的浓度下也是如此。 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.