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Eeyarestatin I

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Chemical Structure| 412960-54-4 同义名 : Eeyarestatin 1
CAS号 : 412960-54-4
货号 : A893133
分子式 : C27H25Cl2N7O7
纯度 : 99%+
分子量 : 630.436
MDL号 : MFCD00319108
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
动物实验配方：
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].
实验方案
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
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.