KV-37

KV-37 is a potent, isoform-selective, and hydrolytically stable small molecule inhibitor of aldo-keto reductase 1C3 (AKR1C3), also known as type 5 17β-hydroxysteroid dehydrogenase. AKR1C3 is a key enzyme responsible for intratumoral androgen biosynthesis, converting adrenal precursors into testosterone and dihydrotestosterone (DHT), which facilitates the progression of castration-resistant prostate cancer (CRPC). KV-37 reduces androgen receptor (AR) transactivation and prostate-specific antigen (PSA) expression in CRPC cell lines. Preclinical studies demonstrate that KV-37 inhibits prostate cancer cell growth in vitro and in vivo and significantly sensitizes resistant cells to the antitumor effects of enzalutamide, showing a high degree of synergistic drug interaction that can result in a >200-fold potentiation of enzalutamide action.

Other names

(E)-3-(4-(3-methylbut-2-en-1-yl)-3-(3-phenylpropanamido)phenyl)acrylic acid