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Submit ReviewEeyarestatin I is a potent inhibitor of endoplasmic reticulum associated protein degradation (ERAD). Specifically targets the p97-associated deubiquitinating process (PAD) and inhibits ataxin-3 (atx3)-dependent deubiquitination. Also inhibits Sec61-mediated protein translocation at the ER. Displays cytotoxic activity preferentially against cancer cells; induces cell death via the proapoptotic protein NOXA. Also enhances adeno-associated viral transduction in multiple cells types.
分子量 | 630.44 |
公式 | C27H25Cl2N7O7 |
储存 | Store at +4°C |
纯度 | ≥98% (HPLC) |
CAS Number | 412960-54-4 |
PubChem ID | 23947580 |
InChI Key | JTUXTPWYZXWOIB-LWWHHIEBSA-N |
Smiles | O=C1N(C2=CC=C(Cl)C=C2)C(N(O)C(NC4=CC=C(Cl)C=C4)=O)C(C)(C)N1CC(N/N=C/C=C/C3=CC=C([N+]([O-])=O)O3)=O |
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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 63.04 | 100 |
以下数据基于产品分子量 630.44。 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 | 1.59 mL | 7.93 mL | 15.86 mL |
5 mM | 0.32 mL | 1.59 mL | 3.17 mL |
10 mM | 0.16 mL | 0.79 mL | 1.59 mL |
50 mM | 0.03 mL | 0.16 mL | 0.32 mL |
参考文献是支持产品生物活性的出版物。
Wang et al (2008) Inhibition of p97-dependent protein degradation by eeyarestatin I. J.Biol.Chem. 283 7445 PMID: 18199748
Aletrari et al (2011) Eeyarestatin 1 interferes with both retrograde and anterograde intracellular trafficking pathways. PLoS One 6 e22713 PMID: 21799938
Wang et al (2008) ERAD inhibitors integrate ER stress with an epigenetic mechanism to activate BH3-only protein NOXA in cancer cells. Proc.Natl.Acad.Sci.USA 106 2200
Cross et al (2009) Eeyarestatin I inhibits Sec61-mediated protein translocation at the endoplasmic reticulum. J.Cell Science 122 4393
Berry and Asokan et al (2016) Chemical modulation of endocytic sorting augments adeno-associated viral transduction. J.Biol.Chem. 291 939 PMID: 26527686
If you know of a relevant reference for Eeyarestatin I, please let us know.
关键词: Eeyarestatin I, Eeyarestatin I supplier, endoplasmic, reticulum, ER, associated, protein, degradation, ERAD, translocation, inhibitors, inhibits, ER-stress, viral, transduction, enhancers, enhances, Other, stress/UPR, Translocation, Viral, Transduction, Enhancers, 3922, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 Eeyarestatin I 的部分引用包括:
Manu et al (2020) Protein translocation and retro-translocation across the endoplasmic reticulum are crucial to inflammatory effector CD4+ T cell function. Cytokine 129 154944 PMID: 32146280
Han et al (2015) Combining valosin-containing protein (VCP) inhibition and suberanilohydroxamic acid (SAHA) treatment additively enhances the folding, trafficking, and function of epilepsy-associated γ-aminobutyric acid, type A (GABAA) receptors. Cell Rep 290 325 PMID: 25406314
Davis et al (2015) Comparative Haploid Genetic Screens Reveal Divergent Pathways in the Biogenesis and Trafficking of Glycophosphatidylinositol-Anchored Proteins. Biochem Biophys Res Commun 11 1727 PMID: 26074080
Zhenghong et al (2017) Aggregation of a hepatitis C virus replicase module induced by ablation of p97/VCP. J Gen Virol 98 1667-1678 PMID: 28691899
Yi et al (2016) Affinity Purification of the Hepatitis C Virus Replicase Identifies Valosin-Containing Protein, a Member of the ATPases Associated with Diverse Cellular Activities Family, as an Active Virus Replication Modulator. J Virol 90 9953 PMID: 27558430
Eales et al (2018) Verteporfin selectively kills hypoxic glioma cells through iron-binding and increased production of reactive oxygen species. Sci Rep 8 14358 PMID: 30254296
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