AKR1Cs-IN-1

Description

AKR1Cs-IN-1 Compound 29 is a potent and broad-spectrum inhibitor targeting members of the Aldo-Keto Reductase 1C family AKR1C1-1C4 . By simultaneously occupying the SP2 and SP3 pockets, it effectively inhibits multiple isoforms and disrupts metabolic pathways associated with drug resistance. In enzymatic activity assays, AKR1Cs-IN-1 exhibited significant inhibitory potency, with IC50 values of 0.09, 0.28, 0.05, and 0.51 AAasAasAAmuM against AKR1C1, AKR1C2, AKR1C3, and AKR1C4, respectively. In the doxorubicin DOX -resistant breast cancer cell line MCF-7/ADR, AKR1Cs-IN-1 showed remarkable resensitization effects and significantly enhanced the cytotoxicity of DOX. AKR1Cs-IN-1 holds promise for research on overcoming drug resistance in breast cancer.