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Submit ReviewEeyarestatin I
Description: Potent inhibitor of ER-associated protein degradation and translocation
Chemical Name: 3-(4-Chlorophenyl)-4-[[[(4-chlorophenyl)amino]carbonyl]hydroxyamino]-5,5-dimethyl-2-oxo-1-imidazolidineacetic acid 2-[3-(5-nitro-2-furanyl)-2-propen-1-ylidene]hydrazide
Purity: ≥98% (HPLC)
Biological Activity for Eeyarestatin I
Eeyarestatin 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.
Technical Data for Eeyarestatin I
| M. Wt | 630.44 |
| Formula | C27H25Cl2N7O7 |
| Storage | Store at +4°C |
| Purity | ≥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 |
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 Eeyarestatin I
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 63.04 | 100 |
Preparing Stock Solutions for Eeyarestatin I
The following data is based on the product molecular weight 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.
| Concentration / Solvent Volume / Mass | 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 |
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Product Datasheets for Eeyarestatin I
References for Eeyarestatin I
References are publications that support the biological activity of the product.
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.
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Keywords: 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
6 Citations for Eeyarestatin I
Citations are publications that use Tocris products. Selected citations for Eeyarestatin I include:
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
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
Do you know of a great paper that uses Eeyarestatin I from Tocris? Please let us know.
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