Art. -Nr.: HY-110078

Eeyarestatin I

15 Cited Publications

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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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Reinheit: 99.56%
CAS. Nr.: 412960-54-4
Formel: C₂₇H₂₅Cl₂N₇O₇
Molecular Weight:630.44

Speicherung:

-20°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Eeyarestatin I Chemical Structure

CAS. Nr.: 412960-54-4

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (15)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

Endoplasmic reticulum-associated protein degradation (ERAD)^[1]^[2]

Cellular Effect

Cell Line	Type	Value	Description	References
JeKo-1	IC₅₀	4 μM Compound: Eeyarestatin 1	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	[PMID: 31550150]
MIA PaCa-2	EC₅₀	4.1 μM Compound: 21	Antiproliferative activity against human MIA PaCa-2 cells Antiproliferative activity against human MIA PaCa-2 cells	[PMID: 35033884]

In Vitro

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.

Cell Viability Assay^[1]

Cell Line:

A549 and H358 cells
Concentration:

2.5 μM, 5 μM, 10 μM, 20 μM, 40 μM
Incubation Time:

48 hours
Result:

Caused dose dependent cell death of both A549 and H358 cells.

Western Blot Analysis^[1]

Cell Line:

A549 and H358 cells
Concentration:

2.5 μM, 5 μM, 10 μM, 20 μM, 40 μM
Incubation Time:

48 hours
Result:

Increased ER stress markers including Bip and CHOP.

Chemical Information

CAS. Nr. 412960-54-4
Appearance Solid
Molecular Weight 630.44
Formel C₂₇H₂₅Cl₂N₇O₇
Color Yellow to orange
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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

-20°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Publications (15)

All WBELISACell Imaging/Staining

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Journal Impact Factor

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
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.
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
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
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.
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.
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

Small-molecule modulators of HIPK4 activity and proteostasis. [Abstract]

2026 May 14:2026.05.12.724395. PMID: 42182270
bioRxiv

Cell autonomous inflammation in VEXAS is mediated by cGAS-STING. [Abstract]

2026 May 29:2026.05.26.727520. PMID: 42244578
Heinrich Heine University Dusseldorf

2025.
Res Sq

2024 Sep 22.
SSRN

2024 Apr 19.

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.5862 mL

7.9310 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

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Eeyarestatin I

15 Cited Publications

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Eeyarestatin I

Anti-Infection Compound Library

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Covalent Screening Library

Ubiquitination Compound Library

Endoplasmic Reticulum Stress Compound Library

Heterocyclic Compound Library

Cell Death Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) Eeyarestatin I

Biologische Aktivität

Chemical Information

Publications (15)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Eeyarestatin I

Anti-Infection Compound Library

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Covalent Screening Library

Ubiquitination Compound Library

Endoplasmic Reticulum Stress Compound Library

Heterocyclic Compound Library

Cell Death Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) Eeyarestatin I

Biologische Aktivität

Chemical Information

Publications (15)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Eeyarestatin I Related Classifications

HY-110078 Related Classifications