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merck millipore,默克密理博,324521,Eeyarestatin I - CAS 412960-54-4 - Calbiochem
产品名称:Eeyarestatin I - CAS 412960-54-4 - Calbiochem
产品型号:324521
A cell-permeable oxo-imidazolidinyl-hydroxyurea that localizes to ER, where it interacts with AAA ATPase p97 via its nitrofuran-containing moiety, without exhibiting affinity toward Hsp70 / ATPase NSF
merck millipore,默克密理博,324521,Eeyarestatin I - CAS 412960-54-4 - Calbiochem
- 产品介绍
重要规格表
经验配方 CAS号 C₂₇H₂₅Cl₂N₇O₇ 412960-54-4 描述 概述 A cell-permeable oxo-imidazolidinyl-hydroxyurea that preferentially localizes to ER, where it interacts with AAA (ATPase associated with diverse cellular activities) ATPase p97 (Kd = 5 - 10 µM) via its nitrofuran-containing moiety, without exhibiting affinity toward Hsp70 or AAA ATPase NSF (N-methylmaleimide-sensitive factor). Evidence indicates that EerI cellular metabolite, but not EerI itself, is responsible for the inhibition of ER membrane translocon sec61 complex-mediated transfer of newly synthesized polypeptide, resulting in a blockage of ER-mediated posttranslational glycosylation and signal peptide removal (Effective conc. = 8 µM in HepG2 and HeLa cultures). Ether independent or as a consequence of the early effect on sec61 complex, EerI culture treatment also induces a selective dissociation of an 180 kDa protein from the atx3-containing p97/VCP (Valosin-containing protein) complex and a blockage of the complex-associated deubiquitination of ERAD (ER-associated protein degradation) substrates in a reversible manner, resulting in an accumulation of polyubiquitinated proteins (Effective conc. = 10 µM in A9 and 293T cultures). EerI culture treatment (10 µM) is also demonstrated to selectively induce cytotoxicity in lymphoid cell lines, BJAB, HBL-2, JEKO-1, Jurkat, KMS-12, MINO, as well as primary leukemia cells from CLL (chronic lymphocytic leukemia) patients, but not PBMC from healthy donors, by upregulating the BH3-only pro-apoptotic protein NOXA in cancer cells via ATF3/4 activation and a downregulation of H2A ubiquitination. Unlike DBeQ (Cat. No. 506190), EeRI does not inhibit p97 ATPase activity. 产品目录编号 324521 品牌系列 Calbiochem®
同义词 ES1, 1-(4-Chloro-phenyl)-3-(3-(4-chloro-phenyl)-5,5-dimethyl-1-(3-(5-nitro-furan-2-yl)-allyldiene-hydrazinocarbonylmethyl)-2-oxo-imidazolidin-4-yl)-1-hydroxyl-urea, ERAD Inhibitor II, p97 Inhibitor II, EerI, Valosin-containing Protein Inhibitor II, VCP Inhibitor II 参考 参考 Chou, T.F., et al. 2011. Proc. Natl. Acad. Sci. USA 108, 4834.
Wang. Q, et al. 2010. PLoS ONE 5, e15479.
Cross, B.C.S., et al. 2009. J. Cell. Sci. 122, 4393.
Wang, Q., et al. 2009. Proc. Natl. Acad. Sci. USA 106, 2200.
Wang, Q., et al. 2008. J. Biol. Chem. 283, 7445.
Fiebiger, E., et al. 2004. Mol. Biol. Cell 15, 1635.产品信息 CAS号 412960-54-4 形式 Light yellow-orange solid Hill配方 C₂₇H₂₅Cl₂N₇O₇ 化学配方 C₂₇H₂₅Cl₂N₇O₇ Molar Mass 630.4 结构配方图像 生物信息 纯度 ≥90% by HPLC 理化信息 溶解度 DMSO 储存和货运信息 货运代码 Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
毒性 Standard Handling
储存 +2°C to +8°C
避光 Protect from light
无需冷冻 No
特殊指南 Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C. 包装信息 惰性气体下包装 Packaged under inert gas
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