IC-87361

IC-87361 is a DNA-dependent protein kinase (DNA-PKcs) inhibitor and radiosensitiser. IC-87361 inhibits catalytic activity of DNA-PKcs, blocks non-homologous end joining (NHEJ) DNA double-strand break repair. IC-87361 induces apoptosis, radiosensitises wild-type endothelial cells, increases ionising radiation-induced apoptosis in lung cancer and melanoma cells, enhances ionising radiation-induced tumour growth delay of lung cancer xenografts via effects on tumour vasculature. IC-87361 can be used for the research of lung cancer, melanoma^[1]. In Vitro:IC-87361 (35 nM), a DNA-PK inhibitor with an enzyme IC₅₀ of 35 nM, selectively radiosensitises DNA-PK-competent wild-type endothelial cells, lung cancer cells, and melanoma cells, and enhances radiation-induced apoptosis in lung cancer and melanoma cells^[1]. In Vivo:IC-87361 acts as a radiosensitizer to enhance ionizing radiation-induced tumour growth delay in human lung cancer xenografts, with a partial effect on tumour vasculature^[1].