4EGI-1
目录号: PL14822 纯度: ≥99%
CAS No. :315706-13-9
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中文名称
4EGI-1
中文别名
4EGI-1 抑制剂;ALPHA-[2-[4-(3,4-二氯苯基)-2-噻唑基]亚肼基]-2-硝基苯丙酸
英文名称
4EGI-1
英文别名
4EGI-1;2-[[4-(3,4-dichlorophenyl)-4,5-dihydro-1,3-thiazol-2-yl]hydrazinylidene]-3-[2-(dihydroxyamino)phenyl]propanoic acid
Cas No.
315706-13-9
分子式
C18H12N4O4Scl2
分子量
451.28
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
4EGI-1 是一种 eIF4E/eIF4G 相互作用抑制剂,抑制 eIF4E 结合,Kd 值为 25 μM。
生物活性
4EGI-1 is an inhibitor of eIF4E/eIF4G interaction, with a K d of 25 μM against eIF4E binding.
性状
Solid
IC50 & Target[1][2]
Kd: 25 μM (eIF4E/eIF4G)
体外研究(In Vitro)
4EGI-1 is an inhibitor of eIF4E/eIF4G interaction, with a Kd of 25 μM against eIF4E binding. 4EGI-1 disrupts the eIF4F complex and inhibits expression of oncogenic proteins in mammalian cells. 4EGI-1 (0-40 μM) also exhibits proapoptotic activity and inhibits the growth of multiple cancer cell lines. 4EGI-1 is cytotoxic to breast cancer cells, such as SKBR-3, MCF-7 and MDA-MB-231 cells, with the IC50 of appr 30 μM, and to the non-CSCs (Cancer stem cells), the IC50 is about 22 μM. 4EGI-1 enhances breast CSC differentiation (40 μM), and suppresses breast CSC induced HUVEC tube-like structure formation (8 μM). Moreover, 4EGI-1 selectively inhibits translation that persists in CSC maintenance and dissemination. 4EGI-1 (50 μM) impairs the formation of eIF4F complex in U87 cells. 4EGI-1 (10, 50 and 100 μM) inhibits cell proliferation via inducing apop
体内研究(In Vivo)
4EGI-1 (75 mg/kg, i.p.) inhibits breast cancer stem cells (CSC) tumor growth and tumorangiogenesis in vivo. 4EGI-1 (75 mg/kg, i.p.) shows inhibitory effect on the tumor volume and weight in mice bearing U87 cells. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
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.
溶解度数据
In Vitro: DMSO : ≥ 35 mg/mL (77.56 mM)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。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。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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