Eeyarestatin I |
| Katalog-Nr.GC13855 |
Hemmer von Endoplasmatischer-Reticulum-assoziierten Abbau (ERAD) und Proteintranslokation.
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.
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Eeyarestatin I, a potent endoplasmic reticulum-associated protein degradation (ERAD) inhibitor, is a potent protein translocation inhibitor. It disturbs endoplasmic reticulum (ER) homeostasis and has anticancer activities resembling that of Bortezomib. Eeyarestatin I inhibits Sec61 translocon[1].
Eeyarestatin I (8μM; 1h) modulates protein processing at the ER of cultured mammalian cells, when cells were incubated with 8μM Eeyarestatin I, an almost complete loss of secretory glycoproteins in the media was observed[2]. Eeyarestatin I (0.2-5μM; 4h) abolishes both Zika virus and Usutu virus infectivity in a dose-and time-dependent manner, in agreement with an antiviral activity occurring directly upon the viral particles[3]. Eeyarestatin I (10μM; 24h) abrogates TGF-β1-triggered Klotho reduction in cultured HK-2 cells[4].
Eeyarestatin I (2.5mg/kg; ip, 10d) upregulates renal Klotho protein expression, as well as sKlotho levels , without significantly altering Klotho mRNA level[4]. Inhibition of Valosin-containing protein's function by Eeyarestatin I (50µg/each; sc; 2 times) reduces tumor growth in NSCLC-xenograft model[5].
References:
[1] Cross B C S, McKibbin C, Callan A C, et al. Eeyarestatin I inhibits Sec61-mediated protein translocation at the endoplasmic reticulum[J]. Journal of cell science, 2009, 122(23): 4393-4400.
[2]. Cross B C S, McKibbin C, Callan A C, et al. Eeyarestatin I inhibits Sec61-mediated protein translocation at the endoplasmic reticulum[J]. Journal of cell science, 2009, 122(23): 4393-4400.
[3]Rodrigo I, Ballesta C, Nunes E B, et al. Eeyarestatin I, an inhibitor of the valosin-containing protein, exhibits potent virucidal activity against the flaviviruses[J]. Antiviral Research, 2022, 207: 105416.
[4]. Li S S, Kong J W, Yu L X, et al. Abnormally decreased renal Klotho is linked to endoplasmic reticulum-associated degradation in mice[J]. International Journal of Medical Sciences, 2022, 19(2): 321.
[5].Valle C W, Min T, Bodas M, et al. Critical role of VCP/p97 in the pathogenesis and progression of non-small cell lung carcinoma[J]. PloS one, 2011, 6(12): e29073.
| Cell experiment [1]: | |
Cell lines | Normal human epidermal keratinocytes cells |
Preparation Method | Confluent HepG2 cells were treated with Eeyarestatin I for 1 hour in culture before a 30-minute starvation in the presence of the compounds in methionine- and cystine-free medium supplemented with 2mM glutamine. Cells were then metabolically labelled in the presence of the eyarestatin I by incubation in starvation medium containing for 30 minutes. |
Reaction Conditions | 8μM; 1h |
Applications | Eeyarestatin I modulates protein processing at the ER of cultured mammalian cells, when cells were incubated with 8μM Eeyarestatin I , an almost complete loss of secretory glycoproteins in the media was observed. |
| Animal experiment [2]: | |
Animal models | Unilateral ureteral obstruction(UUO) model |
Preparation Method | Male C57BL/6 mice (20-25g, 8 weeks old) were free access to food and water in at light-, temperature- and humidity-controlled environment. All mice were subjected to either a sham or UUO operation and were assigned randomly to 4 groups as follows: sham, UUO, Eeyarestatin I treatment and UUO plus Eeyarestatin I treatment. UUO procedure was performed as previously described. Briefly, experimental animals were anesthetized generally, and the right ureter was double-ligated at two locations following abdominal incision. Consequently, the right ureter was cut between the two locations. Mice in sham group undergone identical UUO procedure but the ureteral was not obstructed or ligated. Eeyarestatin I, an ERAD inhibitor, was injected into abdominal cavity in UUO mice at a dosage of 2.5mg/kg, and repeated on day. All mice were sacrificed at day 10 after UUO operation. Serum and kidney samples were collected and processed properly for further analyses. |
Dosage form | 2.5mg/kg; ip, 10d |
Applications | Eeyarestatin I upregulates renal Klotho protein expression, as well as sKlotho levels , without significantly altering Klotho mRNA level. |
References: | |
| 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 |
| Löslichkeit | 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 | |||
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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)
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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.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 9 reference(s) in Google Scholar.)
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