GS 143

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Cat.No. 5636 - GS 143 | C28H19FN2O4 | CAS No. 916232-21-8
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% (HPLC)
Datasheet
Citations
Reviews
Literature

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.

Compound Libraries

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Technical Data

M. Wt 466.46
Formula C28H19FN2O4
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 916232-21-8
PubChem ID 11963988
InChI Key IZPMWFSVTDOCDI-QJOMJCCJSA-N
Smiles FC1=CC=CC=C1C2=CC=C(/C=C3C(CC4=CC=CC=C4)=NN(C5=CC=C(C(O)=O)C=C5)C\3=O)O2

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 46.65 100

Preparing Stock Solutions

The following data is based on the product molecular weight 466.46. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.14 mL 10.72 mL 21.44 mL
5 mM 0.43 mL 2.14 mL 4.29 mL
10 mM 0.21 mL 1.07 mL 2.14 mL
50 mM 0.04 mL 0.21 mL 0.43 mL

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References

References are publications that support the biological activity of the product.

Nakajima et al (2008) A novel small-molecule inhibitor of NF-κB signaling. Biochem.Biophys.Res.Comm. 368 1007 PMID: 18275844

Hirose et al (2008) GS143, an IκB ubiquitination inhibitor, inhibits allergic airway inflammation in mice. Biochem.Biophys.Res.Comm. 374 507 PMID: 18656449


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Keywords: GS 143, GS 143 supplier, GS143, E3, ubiquitin, ligase, ubiquitination, inhibits, inhibitors, NFkappaB, NFκB, NFKB, anti-inflammatory, inflammation, Beta-TrCP1, B-TrCP1, βTrCP1, Ubiquitin, Ligases, 5636, Tocris Bioscience

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Literature in this Area

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