CGP 57380

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Chemical Structure| 522629-08-9 同义名 : MNK1 Inhibitor
CAS号 : 522629-08-9
货号 : A151588
分子式 : C11H9FN6
纯度 : 99%+
分子量 : 244.228
MDL号 : MFCD03861062
存储条件：

Pure form Keep in dark place,Inert atmosphere,Room temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 5 mg/mL(20.47 mM)，配合低频超声，并水浴加热至45℃助溶，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：

4% DMSO+30% PEG 300+water 10 mg/mL

生物活性
靶点

  • MNK1

    MNK1, IC50:2.2 μM
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
细胞系 浓度 检测类型 检测时间 活性说明 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 25800647
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.09mL

0.82mL

0.41mL

20.47mL

4.09mL

2.05mL

40.95mL

8.19mL

4.09mL
参考文献

[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.