#151879

AKR1C3 inhibitor CRT0083914 Small Molecule (Tool Compound)

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Cat. #151879

AKR1C3 inhibitor CRT0083914 Small Molecule (Tool Compound)

Cat. #: 151879

Sub-type: Inhibitor

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Contributor

Inventor: Laurent Rigoreau

Institute: Cancer Research Technology

Tool Details
Handling
Target Details
Related Tools
References

Tool Details

*FOR RESEARCH USE ONLY

  • Tool name: AKR1C3 inhibitor CRT0083914 Small Molecule (Tool Compound)
  • Research fields: Cell signaling and signal transduction;Neurobiology
  • Molecular formula: C16H22N2O3S
  • Tool sub type: Inhibitor
  • Primary target: AKR1C3
  • 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.
  • Purpose: Inhibitor
  • 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
  • Molecular weight: 322.43
  • 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...

Handling

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

Target Details

  • Primary target: AKR1C3
  • Ic50: IC50 = 94 nM

Related Tools

  • Related tools: AKR1C3 inhibitor CRT0036521 Small Molecule (Tool Compound) ; AKR1C3 inhibitor CRT0093964 Small Molecule (Tool Compound)

References

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