1. Cell Cycle/DNA Damage
    Apoptosis
  2. p97
    Apoptosis
  3. Eeyarestatin I

Eeyarestatin I 

Cat. No.: HY-110078 Purity: 98.96%
COA Handling Instructions

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.

For research use only. We do not sell to patients.

Eeyarestatin I Chemical Structure

Eeyarestatin I Chemical Structure

CAS No. : 412960-54-4

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Based on 1 publication(s) in Google Scholar

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Description

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[1][2][3][4][5].

IC50 & Target

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

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].

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.
Molecular Weight

630.44

Formula

C27H25Cl2N7O7

CAS No.
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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture

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

Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (39.65 mM; Need ultrasonic)

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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 98.96%

References
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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.

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Product Name:
Eeyarestatin I
Cat. No.:
HY-110078
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