AKR1C3 inhibitor KV-37

AKR1C3 inhibitor KV-37 is a potent, isoform selective and metabolically stable inhibitor of Aldo-keto reductase 1C3 (AKR1C3) with IC50 of 66 nM, displays 109-fold selectivity over AKR1C2; shows competitive enzyme inhibition versus AKR1C3 with Ki of 3 uM E.NADPH; inhibits AKR1C3 activity in prostate cancer cell lines by inhibiting the conversion of Δ4-AD to testosterone, exhibits greater reduction of prostate cancer cell viability compared to baccharin; sensitizes CRPC cell lines (22Rv1 and LNCaP1C3) towards the anti-tumor effects of enzalutamide, also reduces androgen receptor (AR) transactivation and prostate specific antigen (PSA) expression levels in CRPC cells lines; reduces cancer cell growth in vivo in 22Rv1 xenograft models.

References 1. Verma K, et al. Mol Cancer Ther. 2018 Jun 11. pii: molcanther.1023.2017. View Related Products by Target Other Targets