Eeyarestatin I (Synonyms: イヤレスタチンI)

Name: Eeyarestatin I
Brand: MedChemExpress
SKU: HY-110078
Rating: 5.0 (11 reviews)

製品番号: HY-110078 純度: 99.56%: Data Sheet SDS COA 取扱説明書
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Technical Support

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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号 : 412960-54-4

容量	価格（税別）	在庫状況	数量

>無料サンプル (0.1 - 0.2 mg)		今すぐ申し込む
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 250	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 250	在庫あり	Estimated Time of Arrival: December 31
Solid
5 mg	$180	在庫あり	Estimated Time of Arrival: December 31
10 mg	$300	在庫あり	Estimated Time of Arrival: December 31
50 mg		お問い合わせ
100 mg		お問い合わせ

or バルクお問い合わせ

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

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Based on 11 publication(s) in Google Scholar

顧客検証

ELISA

Cell Imaging/Staining

: 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.

: 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.

: 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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製品説明

IC₅₀ & Target

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

Cellular Effect

Cell Line	Type	Value	Description	References
JeKo-1	IC₅₀	4 3 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]
JeKo-1	IC₅₀	4 3 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 3 Compound: 21	Antiproliferative activity against human MIA PaCa-2 cells Antiproliferative activity against human MIA PaCa-2 cells	[PMID: 35033884]
MIA PaCa-2	EC₅₀	4.1 3 Compound: 21	Antiproliferative activity against human MIA PaCa-2 cells Antiproliferative activity against human MIA PaCa-2 cells	[PMID: 35033884]

体外実験

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.

分子量

630.44

分子式

C₂₇H₂₅Cl₂N₇O₇

CAS 番号

412960-54-4

Appearance

Solid

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

輸送条件

Room temperature in continental US; may vary elsewhere.

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)

溶剤 & 溶解度

体外:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the 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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

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.

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

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

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).

Calculation results:

Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

純度とドキュメンテーション

純度: 99.56%

Select Batch:

データシート (277 KB) SDS (252 KB)

COA (251 KB) HNMR (207 KB) LCMS (95 KB)

取扱説明書 (2659 KB)

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

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 Related Classifications

Molarity Calculator
Dilution Calculator

The molarity calculator equation

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

質量		濃度		体積		分子量 *
	=		×		×

The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）	×	体積 _（開始）	=	濃度 _（終了）	×	体積 _（終了）
	×		=		×
C1		V1		C2		V2

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Eeyarestatin I412960-54-4p97ApoptosisVCPCdc48ERADEMTNOXAdeubiquitinationatx3Sec61anticancerendoplasmicreticulumInhibitorinhibitorinhibit

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Eeyarestatin I (Synonyms: イヤレスタチンI)

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Eeyarestatin I 関連抗体

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おすすめ

•関連スクリーニングライブラリ:

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•関連タンパク質:

生物活性

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参考文献

カスタマーレビュー

Eeyarestatin I 関連抗体

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Eeyarestatin I Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

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