An inhibitor of IκBα ubiquitylation
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GS-143

Item No. 26138

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[4-[[5-(2-fluorophenyl)-2-furanyl]methylene]-4,5-dihydro-5-oxo-3-(phenylmethyl)-1H-pyrazol-1-yl]-benzoic acid
CAS Number
916232-21-8
Molecular Formula
C28H19FN2O4
Formula Weight
466.5
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMF:PBS (pH 7.2) (1:4): 0.20 mg/mlDMSO: 10 mg/ml
λmax
288, 420 nm
SMILES
O=C1N(C2=CC=C(C(O)=O)C=C2)N=C(CC3=CC=CC=C3)/C1=C\C4=CC=C(C5=CC=CC=C5F)O4
InChi Code
InChI=1S/C28H19FN2O4/c29-24-9-5-4-8-22(24)26-15-14-21(35-26)17-23-25(16-18-6-2-1-3-7-18)30-31(27(23)32)20-12-10-19(11-13-20)28(33)34/h1-15,17H,16H2,(H,33,34)/b23-17+
InChi Key
IZPMWFSVTDOCDI-HAVVHWLPSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    GS-143 is an inhibitor of IκBα ubiquitylation.1 It inhibits ubiquitylation of phosphorylated IκBα mediated by the SCFβTrCP1 E3 ubiquitin ligase complex in vitro (IC50 = 5.2 μM) and reduces TNF-α-induced degradation of phosphorylated IκBα, but not β-catenin, another SCFβTrCP1 substrate, in HeLa S3 cells. GS-143 inhibits LPS-induced expression of TNF-α, IL-6, IL-12, ICAM-1, and NF-κB in THP-1 cells in a concentration-dependent manner. Intranasal administration of GS-143 (32 μg/animal) reduces the number of eosinophils, lymphocytes, and total cells in bronchoalveolar lavage fluid (BALF) in an ovalbumin-sensitized mouse model of allergic asthma.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Nakajima, H., Fujiwara, H., Furuichi, Y., et al. A novel small-molecule inhibitor of NF-κB signaling. Biochem. Biophys. Res. Commun. 368(4), 1007-1013 (2008).

    2. Hirose, K., Wakashin, H., Oki, M., et al. GS143, an IκB ubiquitination inhibitor, inhibits allergic airway inflammation in mice. Biochem. Biophys. Res. Commun. 374(3), 507-511 (2008).