Catalog Number: 3922
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.
Background References
  1. Inhibition of p97-dependent protein degradation by eeyarestatin I.
    Wang et al.
    J.Biol.Chem., 2008;283:7445
  2. Eeyarestatin 1 interferes with both retrograde and anterograde intracellular trafficking pathways.
    Aletrari et al.
    PLoS One, 2011;6:e22713
  3. ERAD inhibitors integrate ER stress with an epigenetic mechanism to activate BH3-only protein NOXA in cancer cells.
    Wang et al.
    Proc.Natl.Acad.Sci.USA, 2008;106:2200
Citations:

The citations listed below are publications that use Tocris products. Selected citations for Eeyarestatin I include:

2 Citations: Showing 1 - 2
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  1. 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.
    Authors: Han Et al.
    Cell Rep 2015;290:325
  2. Comparative Haploid Genetic Screens Reveal Divergent Pathways in the Biogenesis and Trafficking of Glycophosphatidylinositol-Anchored Proteins.
    Authors: Davis Et al.
    Biochem Biophys Res Commun 2015;11:1727

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