1-(2-Hydroxy-4-morpholin-4-yl-phenyl)ethanone
IC86621 Off-white solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. A cell-permeable aryl-morpholino compound that acts as a potent, selective, ATP-competitive inhibitor of DNA-PK (IC50 = 120 nM) and PI 3-Kinase catalytic subunit p110b (IC50 = 135 nM). It inhibits DNA-PK-mediated cellular DNA DSB (double strand break) repair (EC50 = 68 µM) and enhances DSB-induced antitumor activity both in vitro and in vivo, while exhibiting no cytotoxic effects (up to 50 µM) in the absence of DSBs. It inhibits PI 3K p110a, p110g, and p110d only at much higher concentrations (IC50 = 1.4, 0.88, 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. Purity: ≥95% by HPLC. CAS 404009-40-1. Ref.: Kashishian, A., et al. 2004. Mol. Cancer Ther. 2, 1257. Willmore, E., et al. 2004. Blood,103, 4659. |
