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4EGI-1

现货
Catalog No.
B3696
竞争性的eIF4E/eIF4G相互作用抑制剂。
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 1,300.00
Ship with 10-15 days
10mg
¥ 1,370.00
Ship with 10-15 days
25mg
¥ 2,350.00
Ship with 10-15 days

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Background

4EGI-1 is a small-molecule inhibitor of eIF4E/eIF4G interaction with IC50 value of 125μM [1].

The eIF4E/eIF4G complex plays a key role in gene translation initiation and is regulated by 4E-BP. Overexpression of eIF4E or eIF4G can induce malignant transformation in mammalian cells. As a mimic peptide of 4E-BP, 4EGI-1 competes with eIF4G and disrupts the association of eIF4E/eIF4G. The KD value for 4EGI-1 binding to eIF4E is 25μM. 4EGI-1 can not affect the binding of 4E-BP to eIF4E and instead causes increase of this binding level. In addition, 4EGI-1 is found to inhibit the Cap-dependent translation while enhances the initiation factor-independent translation. In Jurkat leukemia T cells, 4EGI-1 also causes eIF4G to be displaced from eIF4E [1].

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.

文献引用

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

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt451.28
Cas No.315706-13-9
FormulaC18H12Cl2N4O4S
Solubility≥22.56mg/mL in DMSO
SDFDownload SDF
Canonical SMILESC1=CC=C(C(=C1)CC(=NNC2=NC(=CS2)C3=CC(=C(C=C3)Cl)Cl)C(=O)O)[N+](=O)[O-]
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。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。

试验操作

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.

生物活性

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

化学结构

4EGI-1

相关生物数据

4EGI-1

相关生物数据

4EGI-1