For research use only. Not for therapeutic Use.
GS 143 (CAT: I011264) is a β-TrCP1 ligase inhibitor that blocks the ubiquitination of IκBα, suppressing NF-κB activation. It inhibits IκBα ubiquitination (IC50 = 5.2 μM), reducing inflammatory cytokine expression in human myelomonocytic cells. In OVA-sensitized mice, it suppresses antigen-induced NF-κB expression, inflammation, and mucus production in the airways. GS 143 demonstrates potential as an anti-inflammatory agent by targeting the NF-κB pathway, suggesting its therapeutic utility in conditions associated with excessive inflammation.
Catalog Number | I011264 |
CAS Number | 916232-21-8 |
Synonyms | 4-[4-[[5-(2-Fluorophenyl)-2-furanyl]methylene]-4,5-dihydro-5-oxo-3-(phenylmethyl)-1H-pyrazol-1-yl]benzoic acid |
Molecular Formula | C28H19FN2O4 |
Purity | ≥95% |
Target | Metabolic Enzyme/Protease |
Solubility | Soluble to 100 mM in DMSO |
Storage | Store at +4C |
IUPAC Name | 4-[(4E)-3-benzyl-4-[[5-(2-fluorophenyl)furan-2-yl]methylidene]-5-oxopyrazol-1-yl]benzoic acid |
InChI | 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+ |
InChIKey | IZPMWFSVTDOCDI-HAVVHWLPSA-N |
SMILES | C1=CC=C(C=C1)CC2=NN(C(=O)C2=CC3=CC=C(O3)C4=CC=CC=C4F)C5=CC=C(C=C5)C(=O)O |