Catalog No.: PC-22814Not For Human Use, Lab Use Only.
EPI-7386 (Masofaniten) is a next-generation androgen receptor N-terminal domain (AR NTD) inhibitor, inhibits AR activity by binding the N-terminal domain (NTD) and blocking transcription, irrespective of ligand-binding domain resistance mechanisms.
EPI-7386 (Masofaniten) is a next-generation androgen receptor N-terminal domain (AR NTD) inhibitor, inhibits AR activity by binding the N-terminal domain (NTD) and blocking transcription, irrespective of ligand-binding domain resistance mechanisms. EPI-7386 exhibited potent activity in inhibiting full-length AR (AR-FL) driven transcriptional activity and also strongly impaired the transcriptional activity and the viability of cellular models driven exclusively by truncated AR protein. EPI-7386 inhibits androgen-activated AR binding to target gene loci such as KLK3. EPI-7386 suppresses AR-regulated target gene expression in a comparable manner as lutamides in three human prostate cancer cell lines, LNCaP, 22Rv1, and VCaP. The combination of EPI-7386 with lutamides resulted in broader and deeper inhibition of AR-associated transcriptional activity in both LNCaP and VCaP cells.
