CAS:522629-08-9CGP-57380

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CGP-57380 is a selective Mnk1 inhibitor with IC50 value of 2.2 μM.

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18817579266

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18817579266

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实验数据

技术信息

CAS号

522629-08-9

储存条件

分子式

C11H9FN6

运输

蓝冰

分子量

244.23

别名

溶解度

动物实验配方

4% DMSO+30% PEG 300+water

10 mg/mL

生物活性

靶点 MNK1

IC50:2.2μM
描述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.
动物研究
剂量
Mice: 20 mg/kg, 50 mg/kg^[3] (i.p.)

给药途径
i.p.