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Submit ReviewGS 143
说明： β-TrCP1 ligase inhibitor
化学名： 4-[4-[[5-(2-Fluorophenyl)-2-furanyl]methylene]-4,5-dihydro-5-oxo-3-(phenylmethyl)-1H-pyrazol-1-yl]benzoic acid
纯度： ≥98% (HPLC)
生物活性 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.
化合物库 for GS 143
GS 143 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. 了解 Tocris 化合物库的更多信息。
技术数据 for GS 143
| 分子量 | 466.46 |
| 公式 | C28H19FN2O4 |
| 储存 | Store at +4°C |
| 纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for GS 143
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 46.65 | 100 |
制备储备液 for GS 143
以下数据基于产品分子量 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.
| 浓度/溶剂体积/质量 | 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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产品说明书 for GS 143
参考文献 for GS 143
参考文献是支持产品生物活性的出版物。
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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关键词: 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 篇 GS 143 的引用文献
引用文献是使用了 Tocris 产品的出版物。 GS 143 的部分引用包括：
Smadar et al (2018) Periostin in cardiovascular disease and development: a tale of two distinct roles. Basic Res Cardiol 113 1 PMID: 29101484
Robert R et al (2021) SKI activates the Hippo pathway via LIMD1 to inhibit cardiac fibroblast activation. Basic Res Cardiol 116 25 PMID: 33847835
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
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Programmed Cell Death Poster
There are two currently recognized forms of programmed cell death: apoptosis and necroptosis. This poster summarizes the signaling pathways involved in apoptosis, necroptosis and cell survival following death receptor activation, and highlights the influence of the molecular switch, cFLIP, on cell fate.
Targeted Protein Degradation Poster
Degraders (e.g. PROTACs) are bifunctional small molecules, that harness the Ubiquitin Proteasome System (UPS) to selectively degrade target proteins within cells. They consist of three covalently linked components: an E3 ubiquitin ligase ligand, a linker and a ligand for the target protein of interest. Authored in-house, this poster outlines the generation of a toolbox of building blocks for the development of Degraders. The characteristics and selection of each of these components are discussed. Presented at EFMC 2018, Ljubljana, Slovenia