Toggle Nav
Close
  • Menu
  • Setting

CGP 57380

Catalog No.
B3570
MNK1 inhibitor, specific and selective
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$60.00
In stock
5mg
$81.00
In stock
10mg
$130.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

CGP 57380 is a specific and selective inhibitor of MNK1 with IC50 value of 2.2 μM [1].

Mitogen-activated protein (MAP) kinase interacting kinases 1 (MNK1) is a serine/threonine kinase and is able to integrate signal from MAP kinase pathway and phosphorylate eIF4E [1].

CGP 57380 is a specific and selective MNK1 inhibitor. In 293 cells, CGP 57380 (10 μM) inhibited eIF4E phosphorylation in response to fetal calf serum (FCS), arsenite, anisomycin, PMA or tumor necrosis factor alpha. Also, CGP 57380 increased the cap-dependent reporter rluc. In cellular assays, CGP 57380 inhibited eIF4E phosphorylation with IC50 value of 3 μM [1]. In rat vascular smooth muscle cells, CGP 57380 inhibited eIF4E phosphorylation, protein synthesis and VSMC hypertrophy induced by angiotensin II in a dose dependent way [2]. In mouse macrophages, CGP 57380 concentration-dependently inhibited TNFα production stimulated by Escherichia coli lipopolysaccharide (LPS) through posttranscriptional regulation. Also, CGP 57380 inhibited eIF4E phosphorylation. These results suggested that adenine/uridine-rich elements (ARE)-containing TNFα mRNA required eIF4E phosphorylation for initiation of translation [3]. In bone marrow-derived macrophages, CGP 57380 significantly inhibited the production of proinflammatory cytokines monocyte chemoattractant protein-1, TNF and IL-6 [4].

References:
[1].  Knauf U, Tschopp C, Gram H. Negative regulation of protein translation by mitogen-activated protein kinase-interacting kinases 1 and 2. Mol Cell Biol, 2001, 21(16): 5500-5511.
[2].  Ishida M, Ishida T, Nakashima H, et al. Mnk1 is required for angiotensin II-induced protein synthesis in vascular smooth muscle cells. Circ Res, 2003, 93(12): 1218-1224.
[3].  Andersson K, Sundler R. Posttranscriptional regulation of TNFalpha expression via eukaryotic initiation factor 4E (eIF4E) phosphorylation in mouse macrophages. Cytokine, 2006, 33(1): 52-57.
[4].  Rowlett RM, Chrestensen CA, Nyce M, et al. MNK kinases regulate multiple TLR pathways and innate proinflammatory cytokines in macrophages. Am J Physiol Gastrointest Liver Physiol, 2008, 294(2): G452-459.

Chemical Properties

Physical AppearanceA solid
StorageDesiccate at -20°C
M.Wt244.23
Cas No.522629-08-9
FormulaC11H9FN6
Solubility≥12.2mg/mL in DMSO
SDFDownload SDF
Canonical SMILESFC1=CC=C(C=C1)NC2=NNC3=C2C(N)=NC=N3
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Biological Activity

Description CGP 57380 is potent inhibitor of MNK1 with IC50 value of 2.2 μM.
Targets MNK1          
IC50 2.2 μM          

Quality Control

Quality Control & MSDS

View current batch:

Chemical structure

CGP 57380