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Merck
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Key Documents

E1286

Sigma-Aldrich

Eeyarestatin I

≥98% (HPLC)

别名:

3-(4-氯苯基)-4-[[[(4-氯苯基)氨基] 羰基] 羟基氨基]-5,5-二甲基-2-氧代-1-咪唑烷乙酸 2-[3-(5-硝基-2-呋喃基)-2-丙烯-1-亚基] 酰肼

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About This Item

经验公式(希尔记法):
C27H25Cl2N7O7
分子量:
630.44
分類程式碼代碼:
12352204
NACRES:
NA.77

生物源

synthetic (organic)

品質等級

化驗

≥98% (HPLC)

形狀

powder

儲存條件

desiccated

溶解度

DMSO: 5 mg/mL

儲存溫度

2-8°C

InChI

1S/C27H25Cl2N7O7/c1-27(2)24(35(40)25(38)31-19-9-5-17(28)6-10-19)34(20-11-7-18(29)8-12-20)26(39)33(27)16-22(37)32-30-15-3-4-21-13-14-23(43-21)36(41)42/h3-15,24,40H,16H2,1-2H3,(H,31,38)(H,32,37)

InChI 密鑰

JTUXTPWYZXWOIB-UHFFFAOYSA-N

生化/生理作用

Eeyarestatin I 或 Eer1 通过诱导 NOXA 转录因子 ATF3 和 ATF4 的激活,并通过阻断其泛素化来抑制组蛋白 H2A 的降解,从而促进促凋亡蛋白 NOXA 的转录激活。
Eeyarestatin I 是内质网相关蛋白降解 (ERAD) 的强效抑制剂。特异性靶向 p97 相关去泛素化过程 (PAD) 并抑制 ataxin-3 (atx3) 依赖性去泛素化。也抑制 Sec61 介导的内质网蛋白转位。优先显示对癌细胞的细胞毒活性;通过促凋亡蛋白 NOXA 诱导细胞死亡。

其他說明

本品为 E/Z 亚胺异构体的混合物

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


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Qiuyan Wang et al.
Proceedings of the National Academy of Sciences of the United States of America, 106(7), 2200-2205 (2009-01-24)
The ubiquitin-proteasome system has recently emerged as a major target for drug development in cancer therapy. The proteasome inhibitor bortezomib has clinical activity in multiple myeloma and mantle cell lymphoma. Here we report that Eeyarestatin I (EerI), a chemical inhibitor
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A disintegrin and metalloprotease 17 (ADAM17) is a cell-surface metalloprotease that serves as the principle sheddase for tumor necrosis factor α (TNFα), interleukin-6 receptor (IL-6R), and several ligands of the epidermal growth factor receptor (EGFR), regulating these crucial signaling pathways.
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Journal of cell science, 129(19), 3635-3647 (2016-08-24)
Limited detoxification capacity often directs aggregation-prone, potentially hazardous, misfolded proteins to be deposited in designated cytosolic compartments known as 'aggresomes'. The roles of aggresomes as cellular quality control centers, and the cellular origin of the deposits contained within these structures

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