2-Morpholin-4-yl-6-thianthren-1-yl-pyran-4-one White solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. A cell-permeable disubstituted pyranone compound that acts as a potent and ATP-competitive inhibitor of ATM kinase (IC50 = 13 nM; Ki = 2.2 nM). Displays excellent selectivity over other PIKK family kinases (IC50 = 2.5 , 9.3 , 16.6 µM for DNA-PK, mTOR, PI 3-K, respectively; IC50 > 100 µM for PI 4-K and ATR) and exhibits little activity towards a panel of 60 other kinases even at concentrations as high as 10 µM. Inhibits ATM-dependent cellular protein phosphorylation following ionizing radiation (IR) and sensitizes cells with wild-type ATM, but not mutant ATM, to the cytotoxic effects of IR and DNA-damaging agents. Purity: ≥98% by HPLC. CAS 587871-26-9. Ref.: Pereg, Y., et al. 2005. Proc. Natl. Acad. Sci. USA 102, 5056. Lau, A., et al. 2005. Nat. Cell Biol. 7, 493. Hickson, I., et al. 2004. Cancer Res. 64, 9152. |
