| Bioactivity | 4EGI-1 is an inhibitor of eIF4E/eIF4G interaction, with a Kd of 25 μM against eIF4E binding. | ||||||||||||
| Invitro | 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[1]. 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[2]. 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[3]. | ||||||||||||
| Name | 4EGI-1 | ||||||||||||
| CAS | 315706-13-9 | ||||||||||||
| Formula | C18H12Cl2N4O4S | ||||||||||||
| Molar Mass | 451.28 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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