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NU7441 is a potent, selective, ATP-competitive small molecule inhibitor of DNA-dependent protein kinase catalytic subunit (DNA-PKcs), a key regulator of DNA double-strand break repair via the non-homologous end-joining (NHEJ) pathway. By inhibiting DNA-PKcs, NU7441 impairs DNA damage repair, enhances sensitivity to radiation and chemotherapeutic agents such as topoisomerase inhibitors, and induces apoptosis in cancer cell lines. NU7441 has been explored in preclinical models for sensitization of tumors to radiotherapy and chemotherapy in multiple cancer types, including non-small cell lung carcinoma, liver cancer, breast cancer, leukemia, prostate cancer, and melanoma. There is also preclinical evidence of neuroprotective effects in models of intracerebral hemorrhage and suggested utility in genome engineering by modulating NHEJ and homology-directed repair pathways[1][3][4][5][6][8].
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