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

Eeyarestatin I 

Cat. No.: HY-110078
Handling Instructions

Eeyarestatin I, a potent endoplasmic reticulum-associated protein degradation (ERAD) inhibitor, is a potent protein translocation inhibitor. Eeyarestatin I targets the p97-associated deubiquitinating process (PAD) and inhibits atx3-dependent deubiquitination. 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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Description

Eeyarestatin I, a potent endoplasmic reticulum-associated protein degradation (ERAD) inhibitor, is a potent protein translocation inhibitor. Eeyarestatin I targets the p97-associated deubiquitinating process (PAD) and inhibits atx3-dependent deubiquitination. Eeyarestatin I induces cell death via the proapoptotic protein NOXA and has anticancer effects[1][2][3][4].

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.

412960-54-4

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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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

Eeyarestatin Ip97ApoptosisVCPCdc48ERADEMTNOXAdeubiquitinationatx3Sec61anticancerendoplasmicreticulumInhibitorinhibitorinhibit

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