Cas No.: | 1954693-22-1 |
Chemical Name: | (E)-3-(4-(3-methylbut-2-en-1-yl)-3-(3-phenylpropanamido)phenyl)acrylic acid |
Synonyms: | KV-37 |
SMILES: | C(O)(=O)/C=C/C1=CC=C(C/C=C(/C)\C)C(NC(=O)CCC2=CC=CC=C2)=C1 |
Formula: | C23H25NO3 |
M.Wt: | 363.457 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
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. |