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GS 143

Catalog #: 5636 Datasheet / COA / SDS
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5636/50
5636/10
GS 143 | CAS No. 916232-21-8 | Ubiquitin Ligase (E3) Inhibitors
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Description: β-TrCP1 ligase inhibitor

Chemical Name: 4-[4-[[5-(2-Fluorophenyl)-2-furanyl]methylene]-4,5-dihydro-5-oxo-3-(phenylmethyl)-1H-pyrazol-1-yl]benzoic acid

Purity: ≥98%

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Biological Activity

GS 143 is a 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. GS143, an IκB ubiquitination inhibitor, inhibits allergic airway inflammation in mice.
    Hirose et al.
    Biochem.Biophys.Res.Comm., 2008;374:507
  2. A novel small-molecule inhibitor of NF-κB signaling.
    Nakajima et al.
    Biochem.Biophys.Res.Comm., 2008;368:1007

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