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Eeyarestatin I {[allProObj[0].p_purity_real_show]}

货号:A893133 同义名: Eeyarestatin 1 Ambeed 开学季,买赠积分,赢豪礼

Eeyarestatin I 是一种有效的内质网相关蛋白降解 (ERAD) 抑制剂和蛋白质转运抑制剂。Eeyarestatin I 通过诱导 NOXA 蛋白介导的凋亡来防止蛋白质转运,并表现出抗癌活性。

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There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Eeyarestatin I 化学结构 CAS号:412960-54-4
Eeyarestatin I 化学结构
CAS号:412960-54-4
Eeyarestatin I 3D分子结构
CAS号:412960-54-4
Eeyarestatin I 化学结构 CAS号:412960-54-4
Eeyarestatin I 3D分子结构 CAS号:412960-54-4
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Eeyarestatin I 纯度/质量文件 产品仅供科研

货号:A893133 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 p97 其他靶点 纯度
DBeQ +++

p97, IC50: 1.5 μM

{[allProObj[0].p_purity_real_show]}
MNS ++

p97, IC50: 1.7 μM

Syk,Src {[allProObj[0].p_purity_real_show]}
NMS-873 ++++

p97, IC50: 30 nM

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1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Eeyarestatin I 生物活性

描述 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 effects[1][2][3][4][5].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 IRE1α[1].Eeyarestatin I prevents the transfer of nascent proteins from the membrane-targeting complex to the ER transporter machinery, most likely by inactivating the Sec61 complex[2].

Eeyarestatin I 参考文献

[1]Parag P Shah, et al. Regulation of VCP/p97 demonstrates the critical balance between cell death and epithelial-mesenchymal transition (EMT) downstream of ER stress. Oncotarget. 2015 Jul 10;6(19):17725-37.

[2]Benedict C S Cross, et al. Eeyarestatin I inhibits Sec61-mediated protein translocation at the endoplasmic reticulum. J Cell Sci. 2009 Dec 1;122(Pt 23):4393-400.

[3]Qiuyan Wang, et al. Inhibition of p97-dependent protein degradation by Eeyarestatin I. J Biol Chem. 2008 Mar 21;283(12):7445-54.

[4]Qiuyan Wang, et al. ERAD inhibitors integrate ER stress with an epigenetic mechanism to activate BH3-only protein NOXA in cancer cells. Proc Natl Acad Sci U S A. 2009 Feb 17;106(7):2200-5.

[5]Pauwels E, et al. Inhibitors of the Sec61 Complex and Novel High Throughput Screening Strategies to Target the Protein Translocation Pathway. Int J Mol Sci. 2021 Nov 5;22(21):12007.

Eeyarestatin I 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.59mL

0.32mL

0.16mL

7.93mL

1.59mL

0.79mL

15.86mL

3.17mL

1.59mL

Eeyarestatin I 技术信息

CAS号412960-54-4
分子式C27H25Cl2N7O7
分子量 630.436
别名 Eeyarestatin 1
运输蓝冰
存储条件

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 25 mg/mL(39.66 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

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