| Bioactivity | 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]. |
| Invitro | 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]. Cell Viability Assay[1] Cell Line: |
| Name | Eeyarestatin I |
| CAS | 412960-54-4 |
| Formula | C27H25Cl2N7O7 |
| Molar Mass | 630.44 |
| Transport | 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) |