Eeyarestatin I

Cat. No. 3922

Eeyarestatin I C27H25Cl2N7O7 [412960-54-4]

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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

Biological Activity

Potent inhibitor of endoplasmic reticulum associated protein degradation (ERAD). Specifically targets the p97-associated deubiquinating 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.

Technical Data

M.Wt:
630.44
Formula:
C27H25Cl2N7O7
Solubility:
Soluble to 100 mM in DMSO
Purity:
>98 %
Storage:
Desiccate at +4°C
CAS No:
412960-54-4

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Aletrari et al (2011) Eeyarestatin 1 interferes with both retrograde and anterograde intracellular trafficking pathways. PLoS One 6 e22713. PMID: 21799938.

Cross et al (2009) Eeyarestatin I inhibits Sec61-mediated protein translocation at the endoplasmic reticulum. J.Cell Science 122 4393.

Wang et al (2008) Inhibition of p97-dependent protein degradation by eeyarestatin I. J.Biol.Chem. 283 7445. PMID: 18199748.

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.

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Citations are publications that use Tocris products. Selected citations for Eeyarestatin I include:

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.

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.

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Keywords: Eeyarestatin I, supplier, endoplasmic, reticulum, ER, associated, protein, degradation, ERAD, translocation, inhibitors, inhibits, ER-stress, Tocris Bioscience, Translocation, Exocytosis & Endocytosis products

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