货号:A734706
同义名:
eIF4E/eIF4G Interaction Inhibitor
4EGI-1 是一种 eIF4E/eIF4G 相互作用的破坏剂,对 eIF4E 的结合解离常数 (Kd) 为 25 μM。
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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]. |
体内研究 | In vivo, 4EGI-1 administered at 75 mg/kg intraperitoneally is effective in diminishing the growth and angiogenesis of breast cancer stem cell tumors[2]. Additionally, the same dosage (75 mg/kg, i.p.) demonstrates a significant reduction in tumor volume and weight in mice implanted with U87 cells[3]. |
体外研究 | 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]. |
计算器 | ||||
存储液制备 | ![]() |
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 |
CAS号 | 315706-13-9 |
分子式 | C18H12Cl2N4O4S |
分子量 | 451.283 |
别名 | eIF4E/eIF4G Interaction Inhibitor |
运输 | 蓝冰 |
存储条件 |
粉末 Sealed in dry,Store in freezer, under -20°C 液体 -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 |