KU-55933

KU-55933 is a potent, selective, and ATP-competitive inhibitor of the ataxia telangiectasia mutated (ATM) kinase, a serine/threonine kinase critically involved in the DNA damage response. It exhibits high specificity for ATM (IC50 = 13 nM, Ki = 2.2 nM) over related kinases such as DNA-PK, mTOR, PI 3-kinase, PI 4-K, and ATR, against which it shows much weaker inhibition. KU-55933 sensitizes cancer cells to ionizing radiation and chemotherapeutic agents by impeding DNA repair, reduces proliferation, induces cell cycle arrest and apoptosis, and has shown promise in preclinical models for enhancing cancer therapy. It also inhibits disturbed flow- and bone morphogenetic protein-induced Smad1/5 activation in endothelial cells, suppressing proliferation, inflammation, and atherosclerotic lesion development in mouse models. KU-55933 has been used to reveal the role of ATM signaling in both cancer and cardiovascular disease pathogenesis, including as a chemosensitizer in combination with drugs such as Olaparib[2][5][6][7][9][1][3].

Other names

ATM Kinase Inhibitor2-(4-Morpholinyl)-6-(1-thianthrenyl)-4H-pyran-4-one2-Morpholin-4-yl-6-thianthren-1-yl-pyran-4-one2-Thianthren-1-yl-6-(morpholin-4-yl)-4H-pyran-4-oneCHEMBL222102CHEMBL-222102CHEMBL 222102O549494L5DO-549494L5DO 549494L5DDTXSID40207516DTXSID-40207516DTXSID 40207516587871-26-9