AKR1C3 inhibitor CRT0036521 Small Molecule (Tool Compound)

CRT0036521 is a highly potent and selective inhibitor of the Type 5 17-?-Hydroxysteroid.

Contributors

Inventor Institute
Laurent Rigoreau Cancer Research Technology
Cat. #: 151843
Tool sub type: Inhibitor
Research Fields: Cell signaling and signal transduction;Metabolism;Neurobiology
Application: The compounds showed good cellular potency, as measured by inhibition of AKR1C3 metabolism of a known dinitrobenzamide substrate, with a broad rank order between enzymic and cellular activity, but amide analogues were more effective than predicted by the cellular assay. displays potency in a cellular assay, blocking the ability of AKR1C3 to metabolize a proven substrate.
Purpose: Inhibitor
Product description: CRT0036521 is a highly potent and selective inhibitor of the Type 5 17-?-Hydroxysteroid. A high-throughput screen identified 3-(3,4-dihydroisoquinolin-2(1H)-ylsulfonyl)benzoic acid as a novel, highly potent (low nM), and isoform-selective (1500-fold) inhibitor of aldo-keto reductase AKR1C3: a target of interest in both breast and prostate cancer. Crystal structure studies showed that the carboxylate group occupies the oxyanion hole in the enzyme, while the sulfonamide provides the correct tw…
Molecular weight: 317.37
Selectivity: Isoform-selective (1500-fold) inhibitor of aldo-keto reductase AKR1C3. Does not display any COX (cyclooxygenase) inhibition at 10 ÂľM in whole blood assay.
Primary target: AKR1C3
Shipping conditions: Dry Ice
References:

Janieson et al. 2012. J Med.Chem. PMID: 22877157

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