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4EGI-1

CAS No. : 315706-13-9

MCE 国际站：4EGI-1

产品活性：4EGI-1 是一种 eIF4E/eIF4G 相互作用抑制剂，抑制 eIF4E 结合，K_d 值为 25 μM。

研究领域：Cell Cycle/DNA Damage  |  Autophagy  |  Apoptosis

作用靶点：Eukaryotic Initiation Factor (eIF)  |  Autophagy  |  Apoptosis

In Vitro: 4EGI-1 is an inhibitor of eIF4E/eIF4G interaction, with a K_d 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 apoptosis in U87 cells, and the apoptosis is via Bax activation. 4EGI-1 causes mitochondrial dysfunction, and induces ER stress via GRP-78 activation, in U87 cells.

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.

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