MNK1 is important for its regulation of phosphorylation of eIF4E mediated via the activation of MAP kinase pathways. CGP57380 is a MNK1 inhibitor with IC50 values of 2.2μM and 3μM for inhibition of MNK1 kinase activity in vitro and phosphorylation of eIF4E in cellular assays, respectively. Pretreatment with CGP57380 at concentration of 10μM for 60min could block phosphorylation of eIF4E induced by TNF-α, arsenite, anisomycin, PMA or FCS in 293 cells. Meanwhile, inhibition of MNK1 by CGP-57380 resulted in a dose-dependent increase in the activity of cap-dependent translation in a reporter gene assay with reduced eIF4E phosphorylation in 293 cells. CGP57380 at concentration ranging in 1-10μM resulted in dose-dependent decreases in Ang II–stimulated phosphorylation of eIF4E, protein synthesis, and VSMC hypertrophy of VSMCs. CGP-57380 prevented eIF4E phosphorylation, β-catenin activation, and BC LSC function in vitro at concentration of 10μM and in vivo at dose of 40mg/kg, intraperitoneally, daily, for 3 weeks.
CGP 57380 细胞研究
细胞系
浓度
检测类型
检测时间
活动说明
数据源
MV4-11 cells
Growth inhibition assay
72 h
Growth inhibition of human MV4-11 cells after 72 hrs by resazurin assay, GI50=4.88 μM
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