Eeyarestatin I 是一种有效的内质网相关蛋白降解 (ERAD) 抑制剂，是一种有效的蛋白易位抑制剂。Eeyarestatin I 抑制Sec61转位子。Eeyarestatin I 靶向与 p97 相关的去泛素化过程 (PAD)，并抑制依赖于 atx3 的去泛素化。Eeyarestatin I 在蛋白酶体降解前一步进行干扰。Eeyarestatin I 可防止 Sec61 蛋白易位。Eeyarestatin I 通过促凋亡蛋白 NOXA 诱导细胞死亡，并具有抗癌作用。
| 生物活性 | Eeyarestatin I, a potentendoplasmic reticulum-associated protein degradation (ERAD)inhibitor, is a potent protein translocation inhibitor. Eeyarestatin I inhibitsSec61translocon. 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] |
体外研究
(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].
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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | -20°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: DMSO : 25 mg/mL(39.65 mM;Need ultrasonic) 配制储备液 | 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 |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: 1.25 mg/mL (1.98 mM); Suspended solution; Need ultrasonic
此方案可获得 1.25 mg/mL (1.98 mM) 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；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 *以上所有助溶剂都可在本网站选购。
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