Product Image

Contributor Information

  • Name Laurent Rigoreau
  • Institute Cancer Research Technology

Tool Details

  • Tool name: AKR1C3 inhibitor CRT0083914 Small Molecule (Tool Compound)
  • Molecular formula: C16H22N2O3S
  • Tool type: Small molecules
  • Tool sub-type: Inhibitor
  • Purpose: Inhibitor
  • Molecular weight of the target: 322.43
  • 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.
  • Research area: Cell Signaling & Signal Transduction; Neurobiology
  • Selectivity: Displays much weaker inhibitory activity against AKR1C1, AKR1C2 and AKR1C4 (IC50 >30 ÂľM).
  • IUPAC: 1-[4-(2-Methyl-piperidine-1-sulfonyl)-phenyl]-pyrrolidin-2-one
  • IC50: IC50 = 94 nM
  • 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 of the piperidino ring. There was a broad correlation between the enzyme potencies of the compounds and their effectiveness at inhibiting AKR1C3 activity in cells.

  • For Research Use Only

Target Details

  • Target molecular weight: 322.43
  • Primary target: AKR1C3

Application Details


  • Purity: 322.43 g/mol
  • Shipping conditions: Dry Ice



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