Catalog Number: 5636
Chemical Name: 4-[4-[[5-(2-Fluorophenyl)-2-furanyl]methylene]-4,5-dihydro-5-oxo-3-(phenylmethyl)-1H-pyrazol-1-yl]benzoic acid
Biological Activity
β-TrCP1 ligase inhibitor. Inhibits IκBα ubiquitination (IC50 = 5.2 μM) without affecting proteasome activity. Blocks LPS-induced expression of inflammatory cytokines in human myelomonocytic cells. Suppresses antigen-induced NFκB expression, inflammation and mucus production in airways of OVA-sensitized mice.
Technical Data
  • M.Wt:
    466.46
  • Formula:
    C28H19FN2O4
  • Solubility:
    Soluble to 100 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Store at +4°C
  • CAS No:
    916232-21-8
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. A novel small-molecule inhibitor of NF-κB signaling.
    Nakajima et al.
    Biochem.Biophys.Res.Comm., 2008;368:1007
  2. GS143, an IκB ubiquitination inhibitor, inhibits allergic airway inflammation in mice.
    Hirose et al.
    Biochem.Biophys.Res.Comm., 2008;374:507

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