Eeyarestatin I

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Cat.No. 3922 - Eeyarestatin I | C27H25Cl2N7O7 | CAS No. 412960-54-4
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% (HPLC)
Datasheet
Citations (2)
Literature

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
Storage Desiccate at +4°C
Purity ≥98% (HPLC)
CAS Number 412960-54-4
PubChem ID 23947580
InChI Key JTUXTPWYZXWOIB-LWWHHIEBSA-N
Smiles O=C1N(C2=CC=C(Cl)C=C2)C(N(O)C(NC4=CC=C(Cl)C=C4)=O)C(C)(C)N1CC(N/N=C/C=C/C3=CC=C([N+]([O-])=O)O3)=O

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 63.04 100
ethanol 3.15 5mM with gentle warming

Preparing Stock Solutions

The following data is based on the product molecular weight 630.44. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.59 mL 7.93 mL 15.86 mL
5 mM 0.32 mL 1.59 mL 3.17 mL
10 mM 0.16 mL 0.79 mL 1.59 mL
50 mM 0.03 mL 0.16 mL 0.32 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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

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

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 PMID:

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


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

2 Citations for Eeyarestatin I

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

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

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


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Literature in this Area

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis

Pathways for Eeyarestatin I

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