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CAS No.: 522629-08-9

CGP 57380 Catalog No. CSN16827

Synonyms: MNK1 Inhibitor

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

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靶点选择性

生物活性

实验方案

技术信息

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.
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
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	25800647

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

给药途径
i.p.
参考文献

动物研究
剂量	Mice: 20 mg/kg, 50 mg/kg^[3] (i.p.)
给药途径	i.p.

[1] Chrestensen CA, Eschenroeder A,et al. Loss of MNK function sensitizes fibroblasts to serum-withdrawal induced apoptosis. Genes Cells. 2007 Oct;12(10):1133-40.
[2] Ishida M, Ishida T, et al. Mnk1 is required for angiotensin II-induced protein synthesis in vascular smooth muscle cells. Circ Res. 2003 Dec 12;93(12):1218-24.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 4.0945 mL
- 20.4727 mL
- 40.9454 mL
- 5 mM
- 0.8189 mL
- 4.0945 mL
- 8.1891 mL
- 10 mM
- 0.4095 mL
- 2.0473 mL
- 4.0945 mL

技术信息

CAS号

522629-08-9

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C11H9FN6

运输

蓝冰

分子量

244.23

别名

MNK1 Inhibitor

溶解度

DMSO	47.0 mg/mL (192.4 mM) warming
Water	Insoluble
Ethanol	Insoluble

动物实验配方

4% DMSO+30% PEG 300+water

10 mg/mL

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