In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Eeyarestatin I (EerI ) is an inhibitor of endoplasmic reticulum-associated degradation (ERAD). It disturbs endoplasmic reticulum (ER) homeostasis and has anticancer activities resembling that of Bortezomib. ESI induced cell death in JEKO-1 cells with an IC50 of 4±1.2 µM . ESI is also a potent inhibitor of protein translocation. The IC50 of ESI to ER translocation and N-glycosylation in vitro is ~70 µM .
ERAD pathway can eliminate misfolded ER proteins. Timely removing misfolded proteins from ER is involved in maintaining ER homeostasis . N-Glycosylation is the most common and versatile protein modification, it occurs at the β-amide of the aspargine of the Asn-Xaa-Ser/Thr sequon . ER mannosidase I could trigger the targeting of improperly folded glycoproteins to degradation .
In A9 cells, compared with Me2SO, treatment with EerI made polyubiquitinated MHC class I heavy chain (HC) accumulate in the cytosol. Compared with MG132, treatment with EerI resulted in very few deubiquitinated deglycosylated HC molecules, although a similar amount of accumulated polyubiquitinated HC . In H1299 cells, treatment with EerI for 24 hrs significantly (p< 0.01) reduced cell proliferation (24.0%) as compared to the vehicle-treated control .
On the 2nd day and the 6th day after the subcutaneous injection of H1299 cells (8×106) complexed with Matrigel, athymic nude mice were treated with EerI (10 µM). EerI treatment significantly reduced tumor growth as compared to the DMSO vehicle control .
. Benedict C. S. Cross, Craig McKibbin, Anna C. Callan, et al. Eeyarestatin I inhibits Sec61-mediated protein translocation at the endoplasmic reticulum. Journal of Cell Science, 2009, 122:4393-4400.
. Qiuyan Wang, Bidhan A. Shinkre, Jin-gu Lee, et al. The ERAD Inhibitor Eeyarestatin I Is a Bifunctional Compound with a Membrane-Binding Domain and a
p97/VCP Inhibitory Group. PLoS ONE, 2010, 5(11):e15479.
. Shifra Ben-Dor, Nir Esterman, Eitan Rubin, et al. Biases and complex patterns in the residues flanking protein N-glycosylation sites. Glycobiology, 2004, 14(2):95-101.
. Myriam Ermonval, Claudia Kitzmüller, Anne Marie Mir, et al. N-glycan structure of a short-lived variant of ribophorin I expressed in the MadIA214 glycosylation-defective cell line reveals the role of a mannosidase that is not ER mannosidase I in the process of glycoprotein degradation. Glycobiology, 2001, 11(7):565-576.
. Qiuyan Wang, Lianyun Li and Yihong Ye. Inhibition of p97-dependent Protein Degradation by Eeyarestatin I. Journal of Biological Chemistry, 2008, 283(12):7445-7454.
. Christopher W. Valle, Taehong Min, Manish Bodas, et al. Critical Role of VCP/p97 in the Pathogenesis and Progression of Non-Small Cell Lung Carcinoma. PLoS ONE, 2011, 6(12): e29073.
|Physical Appearance||A crystalline solid|
|Storage||Store at -20°C|
|Solubility||Soluble in DMSO|
|Canonical SMILES||ClC1=CC=C(C=C1)N2[[email protected]@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|
|Shipping Condition||Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.|