LX1 is an anti-prostate cancer compound that targets androgen receptor ( AR ), AR variants and steroidogenic enzyme AKR1C3. LX1 inhibits the enzymatic activity of AKR1C3 , reduces the conversion of androstenedione to testosterone and reduces the expression of AR and AR-V7 and downregulates their target genes. LX1 overcomes the resistance of tumor cells to Enzalutamide , and the combination with Enzalutamide further inhibits tumor growth.