eeyarestatin-1

Eeyarestatin-1 (EerI) is a small molecule inhibitor of endoplasmic reticulum-associated degradation (ERAD) and protein translocation. It acts by targeting the AAA+ ATPase p97 (also known as valosin-containing protein, VCP) and the Sec61 translocon complex. By inhibiting p97-associated deubiquitinating enzymes (such as ataxin-3) and blocking Sec61-mediated protein translocation across the ER membrane, Eeyarestatin-1 disrupts ER proteostasis, induces severe endoplasmic reticulum stress, and activates the unfolded protein response (UPR). This leads to the upregulation of pro-apoptotic factors like NOXA and ATF4, preferentially inducing cell death in cancer cells. Eeyarestatin-1 is widely utilized as a chemical biology tool to study ER homeostasis, protein retrotranslocation, and intracellular trafficking pathways.

Other names

EerIEeyarestatin 1Eeyarestatin1Eeyarestatin-1Eeyarestatin IES1ES-1ES 1p97 Inhibitor IIp-97 Inhibitor IIp 97 Inhibitor IIValosin-containing Protein Inhibitor IIVCP Inhibitor II