4EGI-1
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
4EGI-1是eIF4E/ eIF4G相互作用的小分子抑制剂,IC50值为125 μM[1]。
eIF4E/eIF4G复合体在基因翻译起始中起关键作用,由4E-BP调节。哺乳动物细胞中eIF4E或eIF4G的过表达可诱发恶变。作为4E-BP的模拟肽,4EGI-1与eIF4G竞争,破环eIF4E/eIF4G的关联。4EGI-1与eIF4E结合的KD值为25 μM。4EGI-1不影响4E-BP与eIF4E的结合,反而引起其结合水平的增加。此外,4EGI-1抑制Cap依赖性的翻译,而增强起始因子不依赖的翻译。在Jurkat白血病T细胞中,4EGI-1也引起eIF4G从eIF4E的位移[1]。
参考文献:
[1] Moerke N J, Aktas H, Chen H, et al. Small-molecule inhibition of the interaction between the translation initiation factors eIF4E and eIF4G. Cell, 2007, 128(2): 257-267.
- 1.Haimov O, Sehrawat U, et al. "Dynamic interactions of eIF4G1 with eIF4E and eIF1 underlie scanning dependent and independent translation." Mol Cell Biol. 2018 Jul 9. pii: MCB.00139-18. PMID:29987188
- 2.Lee YC, Wang LJ, et al. "ABT-263-induced MCL1 upregulation depends on autophagy-mediated 4EBP1 downregulation in human leukemia cells." Cancer Lett. 2018 Jun 15;432:191-204. PMID:29913235
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 451.28 |
Cas No. | 315706-13-9 |
Formula | C18H12Cl2N4O4S |
Solubility | ≥22.56 mg/mL in DMSO |
Chemical Name | (E)-2-(2-(4-(3,4-dichlorophenyl)thiazol-2-yl)hydrazono)-3-(2-nitrophenyl)propanoic acid |
SDF | Download SDF |
Canonical SMILES | O=C(O)/C(CC1=CC=CC=C1[N+]([O-])=O)=N/NC2=NC(C3=CC=C(Cl)C(Cl)=C3)=CS2 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验 [1]: | |
细胞系 |
Jurkat细胞 |
制备方法 |
在DMSO中的溶解度大于22.6 mg/mL。若配制更高浓度的溶液,一般步骤如下:请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。 |
反应条件 |
0 ~ 200 μM;24小时 |
实验结果 |
在Jurkat细胞中,给予4EGI-1 (> 50 μM),于24小时后,能诱导细胞死亡。此外,4EGI-1显著增加subG1 DNA含量。同时给予caspase抑制剂zVAD-FMK抑制4EGI-1诱导的subG1 DNA含量增加。 |
References: [1]. Moerke N J, Aktas H, Chen H, et al. Small-molecule inhibition of the interaction between the translation initiation factors eIF4E and eIF4G. Cell, 2007, 128(2): 257-267. |
描述 | 4EGI-1是一种竞争性的eIF4E/eIF4G相互作用抑制剂,与 eIF4E结合,KD值为25 μM。 | |||||
靶点 | eIF4E/eIF4G | |||||
IC50 | 25 μM (KD) |
质量控制和MSDS
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