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 ActivityEeyarestatin 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-acssociated viral transduction in multiple cells types.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Inhibition of p97-dependent protein degradation by eeyarestatin I.
Wang et al.
Eeyarestatin 1 interferes with both retrograde and anterograde intracellular trafficking pathways.
Aletrari et al.
PLoS One, 2011;6:e22713
ERAD inhibitors integrate ER stress with an epigenetic mechanism to activate BH3-only protein NOXA in cancer cells.
Wang et al.
Eeyarestatin I inhibits Sec61-mediated protein translocation at the endoplasmic reticulum.
Cross et al.
J.Cell Science, 2009;122:4393
Chemical modulation of endocytic sorting augments adeno-associated viral transduction.
Berry and Asokan et al.
Citations for Eeyarestatin I
The citations listed below are publications that use Tocris products. Selected citations for Eeyarestatin I include:
4 Citations: Showing 1 - 4
Verteporfin selectively kills hypoxic glioma cells through iron-binding and increased production of reactive oxygen species.
Authors: Eales Et al.
Sci Rep 2018;8(1):14358
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.
Authors: Yi Et al.
J Virol 2016;90:9953
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
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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