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生物来源
synthetic (organic)
质量水平
方案
≥98% (HPLC)
表单
powder
储存条件
desiccated
溶解性
DMSO: 5 mg/mL
储存温度
2-8°C
SMILES字符串
Clc1ccc(cc1)N2C(C(N(C2=O)CC(=O)NN=CC=Cc4[o]c(cc4)[N+](=O)[O-])(C)C)N(O)C(=O)Nc3ccc(cc3)Cl
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 key
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。
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。
其他说明
本品为 E/Z 亚胺异构体的混合物
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
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
Gisela Weskamp et al.
The Journal of biological chemistry, 295(13), 4350-4358 (2020-02-16)
The metalloprotease ADAM17 (a disintegrin and metalloprotease 17) is a key regulator of tumor necrosis factor α (TNFα), interleukin 6 receptor (IL-6R), and epidermal growth factor receptor (EGFR) signaling. ADAM17 maturation and function depend on the seven-membrane-spanning inactive rhomboid-like proteins
Garrett E Berry et al.
The Journal of biological chemistry, 291(2), 939-947 (2015-11-04)
Intracellular trafficking of viruses can be influenced by a variety of inter-connected cellular sorting and degradation pathways involving endo-lysosomal vesicles, the ubiquitin-proteasome system, and autophagy-based or endoplasmic reticulum-associated machinery. In the case of recombinant adeno-associated viruses (AAV), proteasome inhibitors are
Jose Lora et al.
The Journal of biological chemistry, 296, 100733-100733 (2021-05-07)
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.
Avantika Gupta et al.
eLife, 9 (2020-06-12)
The transcription factor FoxO has been shown to block proliferation and progression in mTORC1-driven tumorigenesis but the picture of the relevant FoxO target genes remains incomplete. Here, we employed RNA-seq profiling on single clones isolated using laser capture microdissection from
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