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Eeyarestatin I

Catalog No.GC13855

inhibitor of endoplasmic reticulum-associated degradation (ERAD) and protein translocation

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Eeyarestatin I Chemical Structure

Cas No.: 412960-54-4

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5mg
$78.00
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10mg
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25mg
$284.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

Terminally misfolded proteins, recognized by chaperones on the endoplasmic reticulum (ER), are transported to depots for ubiquitination and proteasomal degradation by the ER-associated protein degradation (ERAD) pathway. Eeyarestatin 1 is an inhibitor of the ERAD pathway, blocking the degradation of misfolded proteins at a dose of 8 µM.[1] It associates with the p97-associated deubiquitinating complex in cells, preventing deubiquitination of substrates by ataxin-3.[2],[3] Eeyarestatin 1, at 4 µM, interferes with both retrograde and anterograde trafficking of proteins, including certain toxins, and potentially, viruses.[4]

Reference:
[1]. Fiebiger, E., Hirsch, C., Vyas, J.M., et al. Dissection of the dislocation pathway for type I membrane proteins with a new small molecule inhibitor, eeyarestatin. Molecular Biology of the Cell 15, 1635-1646 (2004).
[2]. Wang, Q., Li, L., and Ye, Y. Inhibition of p97-dependent protein degradation by Eeyarestatin I. The Journal of Biological Chemisty 283(12), 7445-7454 (2008).
[3]. Wang, Q., Shinkre, B.A., Lee, J.G., et al. The ERAD inhibitor Eeyarestatin I is a bifunctional compound with a membrane-binding domain and a p97/VCP inhibitory group. PLoS One 5(11), 1-12 (2010).
[4]. Aletrari, M.O., McKibbin, C., Williams, H., et al. Eeyarestatin 1 interferes with both retrograde and anterograde intracellular trafficking pathways. PLoS One 6(7), 1-11 (2011).

Chemical Properties

Cas No. 412960-54-4 SDF
Chemical Name 3-(4-chlorophenyl)-1-((R)-3-(4-chlorophenyl)-5,5-dimethyl-1-(2-((E)-2-((Z)-3-(5-nitrofuran-2-yl)allylidene)hydrazinyl)-2-oxoethyl)-2-oxoimidazolidin-4-yl)-1-hydroxyurea
Canonical SMILES ClC1=CC=C(C=C1)N2[C@@H](C(C)(C)N(CC(N/N=C/C=C\C3=CC=C([N+]([O-])=O)O3)=O)C2=O)N(C(NC(C=C4)=CC=C4Cl)=O)O
Formula C27H25Cl2N7O7 M.Wt 630.44
Solubility 30mg/mL in DMSO or DMF Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 1.5862 mL 7.931 mL 15.8619 mL
5 mM 0.3172 mL 1.5862 mL 3.1724 mL
10 mM 0.1586 mL 0.7931 mL 1.5862 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 9 reference(s) in Google Scholar.)

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