Eeyarestatin I

Catalog # Availability Size / Price Qty
3922/10
Other ER Stress/UPR Inhibitors Small Molecule
1 Image
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%

Product Details
Citations (4)
Reviews

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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

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
  4. Eeyarestatin I inhibits Sec61-mediated protein translocation at the endoplasmic reticulum.
    Cross et al.
    J.Cell Science, 2009;122:4393

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