In cell line models of castration-resistant prostate cancer, CCS1477 inhibited AR signaling by reducing the expression of AR-regulated genes (KLK2, KLK, and TMPRSS2), whereas in a mouse xenograft model it managed to inhibit tumor growth and AR signaling by reducing AR-FL and AR-V7 protein expression in all the dosing groups, as it did with C-MYC. Here, TMPRSS2 is linked to prostate carcinoma.