Eeyarestatin I
目录号 : GC13855An ERAD inhibitor
Cas No.:412960-54-4
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Terminally misfolded proteins, recognized by chaperones on the endoplasmic reticulum (ER), are transported to depots for ubiquitination and proteasomal degradation by the ER-associated protein degradation (ERAD) pathway. Eeyarestatin 1 is an inhibitor of the ERAD pathway, blocking the degradation of misfolded proteins at a dose of 8 µM.[1] It associates with the p97-associated deubiquitinating complex in cells, preventing deubiquitination of substrates by ataxin-3.[2],[3] Eeyarestatin 1, at 4 µM, interferes with both retrograde and anterograde trafficking of proteins, including certain toxins, and potentially, viruses.[4]
终端错折蛋白质被内质网上分子伴侣识别后,通过内质网相关蛋白质降解途径(ERAD)被转运到质体进行泛素化和蛋白酶体降解。Eeyarestatin 1是一种ERAD通路的抑制剂,能够以8µM的剂量阻止错折蛋白的降解[1]。它与p97相关联的去泛素化复合物结合于细胞中,阻止ataxin-3对底物的去泛素化[2],[3]。在4µM的剂量下,Eeyarestatin 1干扰蛋白质的逆行和顺行运输,包括某些毒素和可能的病毒[4]。
Reference:
[1]. Fiebiger, E., Hirsch, C., Vyas, J.M., et al. Dissection of the dislocation pathway for type I membrane proteins with a new small molecule inhibitor, eeyarestatin. Molecular Biology of the Cell 15, 1635-1646 (2004).
[2]. Wang, Q., Li, L., and Ye, Y. Inhibition of p97-dependent protein degradation by Eeyarestatin I. The Journal of Biological Chemisty 283(12), 7445-7454 (2008).
[3]. Wang, Q., Shinkre, B.A., Lee, J.G., et al. The ERAD inhibitor Eeyarestatin I is a bifunctional compound with a membrane-binding domain and a p97/VCP inhibitory group. PLoS One 5(11), 1-12 (2010).
[4]. Aletrari, M.O., McKibbin, C., Williams, H., et al. Eeyarestatin 1 interferes with both retrograde and anterograde intracellular trafficking pathways. PLoS One 6(7), 1-11 (2011).
Cas No. | 412960-54-4 | SDF | |
化学名 | 3-(4-chlorophenyl)-1-((R)-3-(4-chlorophenyl)-5,5-dimethyl-1-(2-((E)-2-((Z)-3-(5-nitrofuran-2-yl)allylidene)hydrazinyl)-2-oxoethyl)-2-oxoimidazolidin-4-yl)-1-hydroxyurea | ||
Canonical SMILES | ClC1=CC=C(C=C1)N2[C@@H](C(C)(C)N(CC(N/N=C/C=C\C3=CC=C([N+]([O-])=O)O3)=O)C2=O)N(C(NC(C=C4)=CC=C4Cl)=O)O | ||
分子式 | C27H25Cl2N7O7 | 分子量 | 630.44 |
溶解度 | 30mg/mL in DMSO or DMF | 储存条件 | Store at -20°C |
General tips | 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°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
||
Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 1.5862 mL | 7.931 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 |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。