Eeyarestatin I

Eeyarestatin I is a potent inhibitor of endoplasmic reticulum-associated protein degradation (ERAD) and a potent inhibitor of protein translocation. Eeyarestatin I inhibits the Sec61 translocon. Eeyarestatin I targets the process of p97-associated deubiquitination (PAD) and inhibits atx3-dependent deubiquitination. Eeyarestatin I interferes with a step prior to proteasomal degradation. Eeyarestatin I induces cell death via the pro-apoptotic protein NOXA and has anticancer effects¹²³⁴⁵.Acting in the 2.5-40 μM concentration range for 48 hours, Eeyarestatin I increases endoplasmic reticulum (ER) stress markers, including Bip and CHOP as low as 20 μM, and can lead to cell death in A549 and H358 cells in a dose-dependent manner and ubiquitylation of key proteins, including PERK and IRE1α¹.Eeyarestatin I prevents the transfer of nascent proteins from the membrane-targeting complex to the ER transporter machinery, most likely by inactivating the Sec61 complex².

溶解方案(细胞实验)

DMSO 中的溶解度 : 25 mg/mL (39.65 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

溶解方案(动物实验)

"方案 一": "请依序添加每种溶剂：10% DMSO 40% PEG300 5% Tween-80 45% SalineSolubility: 1.25 mg/mL (1.98 mM); 悬浊液; 超声助溶 此方案可获得 1.25 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。以 1 mL 工作液为例，取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。"