AKR1Cs-IN-1
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 µM 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[1].
Product Specifications
UNSPSC
12352005
Target
Aldose Reductase
Related Pathways
Metabolic Enzyme/Protease
Field of Research
Cancer
Smiles
O=C1CCCC2=CC(C(CSC3=NC(C4=CC=CC=C4)=CC(N3)=O)=O)=CC=C2N1
Molecular Formula
C22H19N3O3S
Molecular Weight
405.47
References & Citations
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
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