4EGI-1

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Chemical Structure| 315706-13-9 同义名 : eIF4E/eIF4G Interaction Inhibitor
CAS号 : 315706-13-9
货号 : A734706
分子式 : C18H12Cl2N4O4S
纯度 : 98%
分子量 : 451.283
MDL号 : MFCD28142689
存储条件：

Pure form Sealed in dry,Store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(77.56 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 4EGI-1 is a disruptor of the eIF4E/eIF4G interaction, with a binding dissociation constant (Kd) of 25 μM against eIF4E. It interferes with the eIF4F complex formation and reduces oncogenic protein expression in mammalian cells. Additionally, 4EGI-1, in concentrations up to 40 μM, displays proapoptotic activities and curtails the proliferation of various cancer cell lines[1]. 4EGI-1 shows cytotoxicity toward breast cancer cell lines like SKBR-3, MCF-7, and MDA-MB-231, achieving an approximate IC50 value of 30 μM. It is more potent against non-Cancer stem cells (CSCs) with an IC50 around 22 μM. At 40 μM, 4EGI-1 facilitates the differentiation of breast CSCs and at 8 μM, it prevents the formation of tube-like structures in HUVEC cells induced by breast CSCs. 4EGI-1 is also noted for selectively targeting translation processes important for CSC maintenance and spread[2]. In U87 cells, 4EGI-1 at 50 μM inhibits the assembly of the eIF4F complex. It suppresses cell proliferation and promotes apoptosis at concentrations of 10, 50, and 100 μM through Bax activation. Furthermore, 4EGI-1 induces mitochondrial dysfunction and triggers endoplasmic reticulum stress by activating GRP-78 in U87 cells[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.22mL

0.44mL

0.22mL

11.08mL

2.22mL

1.11mL

22.16mL

4.43mL

2.22mL
参考文献

[1]Moerke NJ, et al. Small-molecule inhibition of the interaction between the translation initiation factors eIF4E and eIF4G. Cell. 2007 Jan 26;128(2):257-67.

[2]Yi T, et al. 4EGI-1 targets breast cancer stem cells by selective inhibition of translation that persists in CSC maintenance, proliferation and metastasis. Oncotarget. 2014 Aug 15;5(15):6028-37.

[3]Wu M, et al. Anti-Cancer Effect of Cap-Translation Inhibitor 4EGI-1 in Human Glioma U87 Cells: Involvement of Mitochondrial Dysfunction and ER Stress. Cell Physiol Biochem. 2016;40(5):1013-1028. Epub 2016 Dec 12.