Eeyarestatin I |
Catalog No.GC13855 |
inhibitor of endoplasmic reticulum-associated degradation (ERAD) and protein translocation
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 412960-54-4
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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).
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. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Average Rating: 5
(Based on Reviews and 9 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
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