AKR1C3 inhibitor CRT0083914 Small Molecule (Tool Compound)

CRT0083914 is a novel non-carboxylate inhibitors of the aldo-ketoreductase enzyme AKR1C3, which is a target of interest in breast and prostate cancer and also some leukaemias.

Contributors

Inventor Institute
Laurent Rigoreau Cancer Research Technology
Cat. #: 151879
Tool sub type: Inhibitor
Research Fields: Cell signaling and signal transduction;Neurobiology
Purpose: Inhibitor
Product description: CRT0083914 is a novel non-carboxylate inhibitors of the aldo-ketoreductase enzyme AKR1C3, which is a target of interest in breast and prostate cancer and also some leukaemias.
Additional notes: CRT0083914: a series of (piperidinosulfonamidophenyl)pyrrolidin-2-ones as potent (<100 nM) and isoform-selective non-carboxylate inhibitors of AKR1C3. Structure–activity relationships identified the sulfonamide was critical, and a crystal structure showed the 2-pyrrolidinone does not interact directly with residues in the oxyanion hole. Variations in the position, co-planarity or electronic nature of the pyrrolidinone ring severely diminished activity, as did altering the size or polarity o…
Molecular weight: 322.43
Selectivity: Displays much weaker inhibitory activity against AKR1C1, AKR1C2 and AKR1C4 (IC50 >30 ÂľM).
Primary target: AKR1C3
Shipping conditions: Dry Ice
References:

CRT0083914- Heinrich et al. 2013. Eur J Med. Chem. PMID: 23454516

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