4EGI1 是一种竞争性 eIF4E/eIF4 g 相互作用抑制剂,与 eIF4E 结合,Kd值为 25 μM。
产品描述
4EGI-1, a competitive eIF4E/eIF4 g interaction inhibitor, binds to eIF4E(KD=25 μM).
体内活性
在Jurkat细胞中,4EGI-1能够促进细胞凋亡。在A549肺癌细胞中(IC50=6 μM),4EGI-1能够有效抑制细胞生长。在人类肺癌细胞中,4EGI-1通过诱导DR5和下调c-FLIP,cap依赖性蛋白质翻译的抑制而增加TRAIL诱导的细胞凋亡。
细胞实验
Cell viability is measured by treatment of Jurkat cells with compound for 24 h and by determination of intracellular ATP using the CellTiterGlo assay. For measurement of apoptotic DNA fragmentation, cells are treated for 24 h with 60 μM EGI-1 or 6.65 μM camptothecin in the presence or absence of 100 mM zVAD-FMK, a broad-spectrum caspase inhibitor. After fixation and staining with PI, cellular DNA content is determined by FACS analysis in a FACS Calibur machine. Nuclear morphology after 24 h EG1-1 treatment is visualized by staining of cells with Hoechst dye and ?uorescence microscopy. For the A549 lung cancer cells, cell growth in the presence of 4EGI-1 is determined using the SRB staining method.(Only for Reference)
Cas No.
315706-13-9
分子式
C18H12Cl2N4O4S
分子量
451.28
别名
4EGI 1
储存和溶解度
DMSO:45.1 mg/mL (100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years