SC428 is an androgen receptor ( AR ) inhibitor that targets the N-terminal domain. SC428 potently decrease the transactivation of ( AR )-V7, ( AR )v567es, as well as full-length ( AR ) (AR-FL) and its LBD mutants, substantially. SC428 inhibits androgen-stimulated ( AR )-FL nuclear translocation, chromatin binding, and ( AR ) -regulated gene transcription. SC428 inhibits the proliferation of tumor cells in vitro. SC428 inhibits tumor cell growth by inducing apoptosis in mice transplanted with 22RV1.