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Biological Activity:
Potent, selective and ATP-competitive inhibitor of DNA-dependent protein kinase (DNA-PK), with IC50 value to be 13 nM for in vitro DNA-PK inhibition; selectivity >100 fold for DNA-PK over related kinases.
References:
E Willmore et al. DNA-Dependent Protein Kinase Is a Therapeutic Target and an Indicator of Poor Prognosis in B-Cell Chronic Lymphocytic Leukemia. Clin. Cancer Res. 2008, 14(12), 3984. [abstract]
Y Zhao et al. Preclinical Evaluation of a Potent Novel DNA-Dependent Protein Kinase Inhibitor NU7441. Cancer Research 2006, 66, 5354-5362. [abstract]
M Ljungman. Targeting the DNA damage response in cancer. Chem. Rev. 2009, 109(7), 2929-50.
Chemical Name: 8-Dibenzothiophen-4-yl-2-morpholin-4-yl-chromen-4-one
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