2-(Morpholin-1-yl)pyrimido[2,1-a]isoquinolin-4-one Beige solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. A cell-permeable pyrimido-isoquinolinone compound that acts as a potent, reversible, and ATP-competitive inhibitor of DNA-PK (IC50 = 280 nM) with ~19-fold selectivity over mTOR (IC50 = 5.3 µM). Exhibits much reduced or no activity against 43 other commonly studied kinases, including PI 3-K, ATM, and ATR. Shown to induce apoptosis and inhibit mTOR-dependent growth in TSC1-/- murine embryo fibroblasts. Purity: ≥95% by HPLC. CAS 168425-64-7. Ref.: Ballou, L.M., et al. 2007. J. Biol. Chem. 282, 24463. Griffin, R.J., et al. 2005. J. Med. Chem. 48, 569. |
