AKR1C3 inhibitor KV-37 |CAS:1954693-22-1 Probechem Biochemicals

Chemical Structure : AKR1C3 inhibitor KV-37

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AKR1C3 inhibitor KV-37 (KV-37)

货号: 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.

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生物&药学活性

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.

物理化学性质&存储条件

分子量	363.457
分子式	C23H25NO3
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(E)-3-(4-(3-methylbut-2-en-1-yl)-3-(3-phenylpropanamido)phenyl)acrylic acid

参考文献

1. Verma K, et al. Mol Cancer Ther. 2018 Jun 11. pii: molcanther.1023.2017.

AKR1C3 inhibitor KV-37 (KV-37)

生物&药学活性

物理化学性质&存储条件

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AKR1C3 inhibitor KV-37 (KV-37)

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物理化学性质&存储条件

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