NU7026

NU7026 is a potent and selective small-molecule inhibitor of the DNA-dependent protein kinase catalytic subunit (DNA-PKcs). It functions by competitively inhibiting the ATP-binding site of DNA-PKcs, which is a critical component of the non-homologous end joining (NHEJ) pathway for repairing DNA double-strand breaks (DSBs). By blocking this repair mechanism, NU7026 acts as a potent radiosensitizer and chemosensitizer, enhancing the cytotoxic effects of ionizing radiation and various DNA-damaging agents such as topoisomerase II inhibitors (e.g., etoposide) and alkylating agents (e.g., melphalan). While NU7026 is extensively used as a research tool to investigate DNA damage response and repair biology, it has also been explored in preclinical models for various cancers, including prostate, lung, and ovarian cancers, as well as non-oncological conditions like hypoxic pulmonary hypertension and atherosclerosis.

Other names

2-(morpholin-4-yl)benzo[h]chromen-4-one2-(4-morpholinyl)-4H-naphtho[1,2-b]pyran-4-one