Eeyarestatin I
Based on 15 publication(s) in Google Scholar
Eeyarestatin I, a potent endoplasmic reticulum-associated protein degradation (ERAD) inhibitor, is a potent protein translocation inhibitor. Eeyarestatin I inhibits Sec61 translocon. Eeyarestatin I targets the p97-associated deubiquitinating process (PAD) and inhibits atx3-dependent deubiquitination. Eeyarestatin I interferes at a step prior to proteasomal degradation. Eeyarestatin I induces cell death via the proapoptotic protein NOXA and has anticancer effects.
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- 純度: 99.56%
- CAS 番号: 412960-54-4
- 分子式: C27H25Cl2N7O7
- 分子量:630.44
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保管条件:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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MedChemExpress（MCE）の使用を引用している文献 Eeyarestatin I
More- Nat Commun. 2025 Dec 10. [Abstract]
- Nat Commun. 2024 Jan 2;15(1):9. [Abstract]
- Neuron. 2026 Mar 11:S0896-6273(26)00086-3. [Abstract]
- Adv Sci (Weinh). 2025 Jul 15:e03486. [Abstract]
- Cell Death Dis. 2026 Apr 3;17(1):452. [Abstract]
- J Hazard Mater. 2024 Jul 5:472:134466. [Abstract]
- Oncogene. 2025 Oct;44(39):3713-3728. [Abstract]
- Int J Biol Macromol. 2024 Oct 25:136922. [Abstract]
- Int Immunopharmacol. 2023 Sep 15;124(Pt A):110905. [Abstract]
- Poult Sci. 2026 Mar 17;105(6):106808. [Abstract]
- bioRxiv. 2026 May 14:2026.05.12.724395. [Abstract]
- bioRxiv. 2026 May 29:2026.05.26.727520. [Abstract]
- Heinrich Heine University Dusseldorf. 2025.
- Res Sq. 2024 Sep 22.
- SSRN. 2024 Apr 19.
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生物活性
Endoplasmic reticulum-associated protein degradation (ERAD)[1][2]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| JeKo-1 | IC50 |
4 μM
Compound: Eeyarestatin 1
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Growth inhibition of human JeKo1 cells assessed as reduction in cell viability by MTT assay
Growth inhibition of human JeKo1 cells assessed as reduction in cell viability by MTT assay
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[PMID: 31550150] |
| MIA PaCa-2 | EC50 |
4.1 μM
Compound: 21
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Antiproliferative activity against human MIA PaCa-2 cells
Antiproliferative activity against human MIA PaCa-2 cells
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[PMID: 35033884] |
Eeyarestatin I (2.5-40 μM; 48 hours; A549 and H358 cells) treatment causes a dose-dependent cell death of both A549 and H358 cells[1].
Eeyarestatin I (2.5-40 μM; 48 hours; A549 and H358 cells) treatment increases endoplasmic reticulum (ER) stress markers including Bip and CHOP as low as 20 μM. Eeyarestatin I treatment shows a dose dependent ubiquitination of key proteins including PERK and IRE1α[1].
Eeyarestatin I (20 μM; 48 hours; A549 and H358 cells) treatment induces cell migration and cell invasion[1].
Eeyarestatin 1 prevents the transfer of nascent proteins from the membrane-targeting complex to the ER translocation machinery, most probably by inactivating the Sec61 complex[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549 and H358 cells
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Concentration:2.5 μM, 5 μM, 10 μM, 20 μM, 40 μM
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Incubation Time:48 hours
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Result:Caused dose dependent cell death of both A549 and H358 cells.
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Cell Line:A549 and H358 cells
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Concentration:2.5 μM, 5 μM, 10 μM, 20 μM, 40 μM
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Incubation Time:48 hours
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Result:Increased ER stress markers including Bip and CHOP.
化学情報
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CAS 番号 412960-54-4
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性状 Solid
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分子量 630.44
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分子式 C27H25Cl2N7O7
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Color Yellow to orange
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SMILES
ON(C(C1(C)C)N(C(C=C2)=CC=C2Cl)C(N1CC(N/N=C/C=C/C(O3)=CC=C3[N+]([O-])=O)=O)=O)C(NC(C=C4)=CC=C4Cl)=O
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別名
イヤレスタチンI
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (15)
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Journal Impact Factor
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Most Recent
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Nat Commun
Ubiquitination by HRD1 is essential for TLR3 trafficking and its innate immune signaling. [Abstract]2025 Dec 10. PMID: 41372171 -
Nat Commun
Pharmaceutical targeting of OTUB2 sensitizes tumors to cytotoxic T cells via degradation of PD-L1. [Abstract]2024 Jan 2;15(1):9. PMID: 38167274 -
Neuron
Targeting PGAM5-driven mitochondrial integrated stress response slows ALS progression across subtypes. [Abstract]2026 Mar 11:S0896-6273(26)00086-3. PMID: 41819100 -
Adv Sci (Weinh)
LncDARS-AS1 Regulates ATP1A1 Stability and Enhances Na+/K+ ATPase Activity to Promote Osteosarcoma Metastasis. [Abstract]2025 Jul 15:e03486. PMID: 40665639 -
Cell Death Dis
PABPC1-induced stabilization of PGK1 mRNA reduces apoptosis and sunitinib sensitivity in renal cell carcinoma by suppressing endoplasmic reticulum stress. [Abstract]2026 Apr 3;17(1):452. PMID: 41932875 -
J Hazard Mater
The involvement of SigmaR1K142 degradation mediated by ERAD in neural senescence linked with CdCl2 exposure. [Abstract]2024 Jul 5:472:134466. PMID: 38718507
Eeyarestatin I purchased from MedChemExpress. Usage Cited in: J Hazard Mater. 2024 Jul 5:472:134466. [Abstract]
Eeyarestatin I (Eer1, 5 μM; 6 h) alleviated CdCl₂-induced SigmaR1 degradation in SH-SY5Y cells treated with CdCl₂ (1 μM; 72 h) by inhibiting ERAD. Eeyarestatin I (Eer1, 5 μM; 6 h) also reversed the activation of the p53/p21/Rb pathway.
Eeyarestatin I purchased from MedChemExpress. Usage Cited in: J Hazard Mater. 2024 Jul 5:472:134466. [Abstract]
Eeyarestatin I (Eer1, 5 μM; 6 h) reduced IL‑6 levels in CdCl₂‑treated SH‑SYY5Y cells.
Eeyarestatin I purchased from MedChemExpress. Usage Cited in: J Hazard Mater. 2024 Jul 5:472:134466. [Abstract]
Eeyarestatin I (Eer1, 5 μM; 6 h) reduced the number of senescent cells in CdCl₂‑treated SH‑SY5Y cells.
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Oncogene
EMC2 promotes triple negative breast cancer growth by protecting FDFT1 from endoplasmic reticulum associated degradation to impair ferroptosis susceptibility. [Abstract]2025 Oct;44(39):3713-3728. PMID: 40931051
Eeyarestatin I purchased from MedChemExpress. Usage Cited in: Oncogene. 2025 Oct;44(39):3713-3728. [Abstract]
The shEMC2 MDA-MB-231 and BT-20 cells were treated with the ERAD pathway inhibitor Eeyarestatin I (Eer I) (10 μM) for the indicated time (8-16 h) for the western blot detection of FDFT1 and EMC2 expression, n = 3. The results showed that Eeyarestatin I (Eer I) significantly reversed the downregulation of FDFT1 induced by EMC2.
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Int J Biol Macromol
Identification of c.146G > A mutation in a Fabry patient and its correction by customized Cas9 base editors in vitro. [Abstract]2024 Oct 25:136922. PMID: 39490876 -
Int Immunopharmacol
Boningmycin induces AMPK-mediated endoplasmic reticulum-associated degradation of PD-L1 protein in human cancer cells. [Abstract]2023 Sep 15;124(Pt A):110905. PMID: 37717372
Eeyarestatin I purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2023 Sep 15;124(Pt A):110905. [Abstract]
After pretreatment with Eeyarestatin I (Eer I, 2 μM) for 2 h, cells were exposed to BON (2 μM) for 8 h, and the protein levels were measured. The results showed that Eeyarestatin I (Eer I) markedly suppressed the reduction in PD-L1 protein levels following BON or MET exposure.
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Poult Sci
ERAD inhibitor Eeyarestatin I (EerI) suppresses duck plague virus by restoring STING-mediated antiviral immunity. [Abstract]2026 Mar 17;105(6):106808. PMID: 41865653 -
bioRxiv
2026 May 14:2026.05.12.724395. PMID: 42182270 -
bioRxiv
2026 May 29:2026.05.26.727520. PMID: 42244578 -
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溶剤 & 溶解度
DMSO : 25 mg/mL (39.65 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 1.25 mg/mL (1.98 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 1.25 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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参考文献
[1]. Parag P Shah, et al. Regulation of VCP/p97 demonstrates the critical balance between cell death and epithelial-mesenchymal transition (EMT) downstream of ER stress. Oncotarget. 2015 Jul 10;6(19):17725-37. [Content Brief]
[2]. Benedict C S Cross, et al. Eeyarestatin I inhibits Sec61-mediated protein translocation at the endoplasmic reticulum. J Cell Sci. 2009 Dec 1;122(Pt 23):4393-400. [Content Brief]
[3]. Qiuyan Wang, et al. Inhibition of p97-dependent protein degradation by Eeyarestatin I. J Biol Chem. 2008 Mar 21;283(12):7445-54. [Content Brief]
[4]. Qiuyan 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 U S A. 2009 Feb 17;106(7):2200-5. [Content Brief]
[5]. Pauwels E, et al. Inhibitors of the Sec61 Complex and Novel High Throughput Screening Strategies to Target the Protein Translocation Pathway. Int J Mol Sci. 2021 Nov 5;22(21):12007. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.5862 mL | 7.9310 mL | 15.8619 mL | 39.6548 mL |
| 5 mM | 0.3172 mL | 1.5862 mL | 3.1724 mL | 7.9310 mL | |
| 10 mM | 0.1586 mL | 0.7931 mL | 1.5862 mL | 3.9655 mL | |
| 15 mM | 0.1057 mL | 0.5287 mL | 1.0575 mL | 2.6437 mL | |
| 20 mM | 0.0793 mL | 0.3965 mL | 0.7931 mL | 1.9827 mL | |
| 25 mM | 0.0634 mL | 0.3172 mL | 0.6345 mL | 1.5862 mL | |
| 30 mM | 0.0529 mL | 0.2644 mL | 0.5287 mL | 1.3218 mL |
Eeyarestatin I 関連分類
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