Catalog No.: PC-35291Not For Human Use, Lab Use Only.
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.
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.
KV-37 shows competitive enzyme inhibition versus AKR1C3 with Ki of 3 uM E.NADPH.
KV-37 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.
KV-37 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.
KV-37 reduces cancer cell growth in vivo in 22Rv1 xenograft models.
