N-[4-Cyano-3-(trifluoromethyl)phenyl]-N′-[2-(2-thienyl)ethenyl]urea

Uses

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[1].

in vivo

References

[1] Qianhui Yi , et al. Discovery of a Small-Molecule Inhibitor Targeting the Androgen Receptor N-Terminal Domain for Castration-Resistant Prostate Cancer. 2023 May 4;22(5):570-582. DOI:10.1158/1535-7163.MCT-22-0237