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DNA-dependent protein kinase (DNA-PK) catalyzes nonhomologous end-joining, which is required to repair lethal DNA double-strand breaks. Because cells that are defective in DNA double-strand break repair are highly sensitive to ionizing radiation and topoisomerase II poisons, modulating DNA-PK is one strategy to defer cancer cell resistance to radiation or chemotherapeutic treatments. NU 7441 is a selective DNA-PK inhibitor with an IC50 value of 14 nM. It inhibits other members of the PI3K-related kinase family, including mTOR, PI3K, ataxia telangiectasia mutated (ATM), and ataxia telangiectasia and Rad3 related (ATR) with IC50 values of 1.7, 5, >100, and >100 µM, respectively. NU 7441 has been shown to increase the cytotoxicity of ionizing radiation and etoposide (Cay-12092) in human colon cancer cell lines in vitro and to potentiate the effects of etoposide in mice bearing human colon cancer xenograft tumors in vivo.Formal Name: 8-(4-dibenzothienyl)-2-(4-morpholinyl)-4H-1-benzopyran-4-one. CAS Number: 503468-95-9. Synonyms: Ku-57788. Molecular Formula: C25H19NO3S. Formula Weight: 413.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 1 mg/ml, DMF:PBS (pH 7.2) (1:4): 0.2 mg/ml, DMSO: 0.12 mg/ml. lambdamax: 234, 288 nm. SMILES: O=C(C=C(N1CCOCC1)O2)C3=C2C(C4=CC=CC5=C4SC6=C5C=CC=C6)=CC=C3. InChi Code: InChI=1S/C25H19NO3S/c27-21-15-23(26-11-13-28-14-12-26)29-24-17(6-3-9-20(21)24)19-8-4-7-18-16-5-1-2-10-22(16)30-25(18)19/h1-10,15H,11-14H2. InChi Key: JAMULYFATHSZJM-UHFFFAOYSA-N.
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