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

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%
Molecular Weight:	630.44 kDa

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 kDa
Formula	C₂₇H₂₅Cl₂N₇O₇
Storage	Store at +4°C
Purity	≥98%
CAS Number	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.

Solubility for Eeyarestatin I

Solubility

Soluble Soluble to 100 mM in DMSO

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References for Eeyarestatin I

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

XJ Di, YJ Wang, DY Han, YL Fu, AS Duerfeldt, BS Blagg, TW Mu Grp94 Protein Delivers ?-Aminobutyric Acid Type A (GABAA) Receptors to Hrd1 Protein-mediated Endoplasmic Reticulum-associated Degradation J. Biol. Chem., 2016;291(18):9526-39. 2016 PMID: 26945068
Han D, Di X, Fu Y, Mu T Combining valosin-containing protein (VCP) inhibition and suberanilohydroxamic acid (SAHA) treatment additively enhances the folding, trafficking, and function of epilepsy-associated gamma-aminobutyric acid, type A (GABAA) receptors. J Biol Chem, 2015;290(1):325-37. 2015 PMID: 25406314
Zhong S, Xu J, Li P, Tsukamoto H Caveosomal oxidative stress causes Src-p21ras activation and lysine 63 TRAF6 protein polyubiquitination in iron-induced M1 hepatic macrophage activation. J Biol Chem, 2102;287(38):32078-84. 2102 PMID: 22829592
Wang, Hongxia, Yu, Xiaofei, Guo, Chunqing, Zuo, Daming, Fisher, Paul B, Subjeck, John R, Wang, Xiang-Ya Enhanced endoplasmic reticulum entry of tumor antigen is crucial for cross-presentation induced by dendritic cell-targeted vaccination. J Immunol, 2013;191(12):6010-21. 2013 PMID: 24218449
Wang et al. Inhibition of p97-dependent protein degradation by eeyarestatin I. J.Biol.Chem., 2008;283:7445 PMID: 18199748
Aletrari et al. Eeyarestatin 1 interferes with both retrograde and anterograde intracellular trafficking pathways. PLoS One, 2011;6:e22713 PMID: 21799938
Wang et al. ERAD inhibitors integrate ER stress with an epigenetic mechanism to activate BH3-only protein NOXA in cancer cells. Proc.Natl.Acad.Sci.USA, 2008;106:2200
Cross et al. Eeyarestatin I inhibits Sec61-mediated protein translocation at the endoplasmic reticulum. J.Cell Science, 2009;122:4393
Berry and Asokan et al. Chemical modulation of endocytic sorting augments adeno-associated viral transduction. J.Biol.Chem., 2016;291:939 PMID: 26527686