Bozepinib

Enzyme inhibitor

This potent antitumor agent (FW = 521.33 g/mol), sysyematically known as (RS)-2,6-dichloro-9-[1-(p-nitrobenzenesulfonyl)-1,2,3,5-tetrahydro-4,1- benzoxazepin-3-yl]-9H-purine, induces apoptosis in breast and colon cancer cells via inhibition (IC50 = 0.3–2 μM) of the the double-stranded RNAdependent protein kinase, PKR, but not p53. Moreover, interferon enhances cytotoxicity of bozepinib in colon and breast cancer cells by increasing apoptotic cell death.