Eeyarestatin I

Name: Eeyarestatin I
Brand: Tocris Bioscience
SKU: 3922

Tocris Bioscience, part of Bio-Techne | Catalog # 3922

Citations (15)

COA / SDS

Potent inhibitor of ER-associated protein degradation and translocation

Key Product Details

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)
Molecular Weight:	630.44

View Full Technical Details for Eeyarestatin I

Technical Data
Citations

Biological Activity for Eeyarestatin I

Eeyarestatin 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-associated viral transduction in multiple cells types.

Technical Data for Eeyarestatin I

M. Wt	630.44
Formula	C₂₇H₂₅Cl₂N₇O₇
Storage	Store 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.

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

Solubility for Eeyarestatin I

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	63.04	100

Preparing Stock Solutions for Eeyarestatin I

The following data is based on the product molecular weight 630.44.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

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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References for Eeyarestatin I

References are publications that support the biological activity of the product.

Berry and Asokan Chemical modulation of endocytic sorting augments adeno-associated viral transduction. J.Biol.Chem. 2016 PMID: 26527686
Cross Eeyarestatin I inhibits Sec61-mediated protein translocation at the endoplasmic reticulum. J.Cell Science
Aletrari Eeyarestatin 1 interferes with both retrograde and anterograde intracellular trafficking pathways. PLoS One 2011 PMID: 21799938
Wang ERAD inhibitors integrate ER stress with an epigenetic mechanism to activate BH3-only protein NOXA in cancer cells. Proc.Natl.Acad.Sci.USA
Wang Inhibition of p97-dependent protein degradation by eeyarestatin I. J.Biol.Chem. 2008 PMID: 18199748