VPC-13566 is Binding Function 3 (BF3)-specific inhibitor of the androgen receptor. VPC-13566 potently inhibits AR transcriptional activity by displacement of the BAG1L peptide from the BF3 pocket. VPC-13566 inhibits the growth of various prostate cancer cell lines including an enzalutamide-resistant cell line and inhibits the growth of AR-dependent prostate cancer xenograft in mice.