AKR1C3 inhibitor KV-37

Modify Date: 2025-08-25 12:22:19

AKR1C3 inhibitor KV-37 Structure
AKR1C3 inhibitor KV-37 structure
Common Name AKR1C3 inhibitor KV-37
CAS Number 1954693-22-1 Molecular Weight 363.457
Density N/A Boiling Point N/A
Molecular Formula C23H25NO3 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of 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.

 Names

Name AKR1C3 inhibitor KV-37

 AKR1C3 inhibitor KV-37 Biological Activity

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

 Chemical & Physical Properties

Molecular Formula C23H25NO3
Molecular Weight 363.457
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