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说明： Inhibitor of 20S proteasome; immunosuppressant
别名： Aspergillin
化学名： (3R,5aS,6S,10aR)-2,3,5a,6-Tetrahydro-6-hydroxy-3-(hydroxymethyl)-2-methyl-10H-3,10a-epidithiopyrazino[1,2-a]indole-1,4-dione
生物活性 for Gliotoxin
Gliotoxin is an immunosuppressive agent; blocks phagocytosis, cytokine production and proliferation of T and B cells. Non-competitively inhibits chymotrypsin-like activity of 20S proteasome; prevents degradation of IκBα, an endogenous blocker of NF-κB. Inhibits leukotriene B4 (LTB4) biosynthesis via inhibition of LTA4 hydrolase. Also inhibits farnesyltransferase and geranylgeranyltransferase I (IC50 values are 80 and 17 μM respectively) and displays antitumor activity against breast cancer in vivo.
技术数据 for Gliotoxin
| 分子量 | 326.38 |
| 公式 | C13H14N2O4S2 |
| 储存 | Desiccate at -20°C |
| CAS Number | 67-99-2 |
| PubChem ID | 6223 |
| InChI Key | FIVPIPIDMRVLAY-RBJBARPLSA-N |
| Smiles | O=C([C@@]2(SS4)N(C([C@@]43CO)=O)[C@@H]1[C@@H](O)C=CC=C1C2)N3C |
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.
产品说明书 for Gliotoxin
参考文献 for Gliotoxin
参考文献是支持产品生物活性的出版物。
Waring and Beaver (1996) Gliotoxin and related epipolythiodioxopiperazines. Gen.Pharmacol. 27 1311 PMID: 9304400
Fitzpatrick et al (2000) In vitro and in vivo effects of gliotoxin, a fungal metabolite: efficacy against dextran sodium sulfate-induced colitis in rats. Dig.Dis.Sci. 45 2327 PMID: 11258552
Vigushin et al (2004) Gliotoxin is a dual inhibitor of farnesyltransferase and geranylgeranyltransferase I with antitumour activity against breast cancer in vivo. Med.Oncol. 21 21 PMID: 15034210
König et al (2019) Gliotoxin from Aspergillus fumigatus abrogates leukotriene B4 formation through inhibition of leukotriene A4 hydrolase. Cell Chem.Biol. 26 524 PMID: 30745237
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关键词: Gliotoxin, Gliotoxin supplier, inhibitors, 20S, proteasome, immunosuppressant, inhibits, NF-κB, NF-kappaB, NF-kB, cytokine, production, Farnesyltransferase, geranylgeranyltransferase, I, Proteinases, Proteases, Nuclear, Factor, Kappa, B, Cytokine, Signaling, Signalling, Post-translational, Modification, Aspergillin, Protein, Prenyltransferases, NF-kB/IkB, Proteasome, Modifications, Immunosuppressants, LTA4, Hydrolase, 2637, Tocris Bioscience
1 篇 Gliotoxin 的引用文献
引用文献是使用了 Tocris 产品的出版物。 Gliotoxin 的部分引用包括：
Park et al (2019) Gliotoxin Enhances Autophagic Cell Death via the DAPK1-TAp63 Signaling Pathway in PTX-Resistant Ovarian Cancer Cells. Mar Drugs 17 PMID: 31336860
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该领域的文献
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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:
- Active Degraders
- TAG Degradation Platform
- Degrader Building Blocks
- Assays for Protein Degradation
- Induced Proximity Tools
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