Home / Pharmacology / Enzymes / Ligases / Ubiquitin E3 Ligases / Ubiquitin E3 Ligase Inhibitors / GS 143

GS 143

Cat. No. 5636 2 Citations Submit a Review Datasheet / COA / SDS
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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% (HPLC)
Datasheet
Citations (2)
Reviews
Literature (3)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for GS 143

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.

Compound Libraries for GS 143

GS 143 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.

Technical Data for GS 143

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for GS 143

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

Preparing Stock Solutions for GS 143

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

Select a batch to recalculate based on the batch molecular weight:
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 for GS 143

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

If you know of a relevant reference for GS 143, please let us know.

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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

2 Citations for GS 143

Citations are publications that use Tocris products. Selected citations for GS 143 include:

Robert R et al (2021) SKI activates the Hippo pathway via LIMD1 to inhibit cardiac fibroblast activation. Basic Res Cardiol 116 25 PMID: 33847835

Smadar et al (2018) Periostin in cardiovascular disease and development: a tale of two distinct roles. Basic Res Cardiol 113 1 PMID: 29101484

Do you know of a great paper that uses GS 143 from Tocris? Please let us know.

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

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TPD and Induced Proximity Research Product Guide

TPD and Induced Proximity Research Product Guide

This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:

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