CGP 57380

Cayman Chemical Item Number 13322

MNK1 Inhibitor (CAS 522629-08-9)

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Description

CGP 57380 is a selective inhibitor of MAP kinase-interacting kinase 1 (MNK1) in vitro (IC50 = 2.2 μM),1 with no inhibitory activity against p38, JNK1, ERK1/2, PKC, or Src-like kinases. It blocks the phosphorylation of eIF4E in response to TNF-α, arsenite, anisomycin, PMA, or fetal calf serum in 293 cells (IC50 = 3 μM).1 CGP 57380 also dose-dependently inhibits TNF-α production in RAW 264.7 cells that have been co-treated with agonists for Toll-like receptor (TLR)2 (HKLM), TLR4 (LPS), TLR6/2 (FSL), TLR7 (imiquimod), or TLR9 (CpG DNA), presumably by inhibiting MNK1.2

1. Knauf, U., Tschopp, C., and Gram, H. Negative regulation of protein translation by mitogen-activated protein kinase-interacting kinases 1 and 2. Mol Cell Biol 21(16) 5500-5511 (2001).

2. Rowlett, R.M., Chrestensen, C.A., Nyce, M., et al. MNK kinases regulate multiple TLR pathways and innate proinflammatory cytokines in macrophages. Am J Physiol Gastrointest Liver Physiol 294 452-459 (2008).

Synonyms
  • MNK1 Inhibitor
Formal Name N3-​(4-​fluorophenyl)-​1H-​pyrazolo[3,​4-​d]pyrimidine-​3,​4-​diamine
CAS Number 522629-08-9
Molecular Formula C11H9FN6
Formula Weight 244.2
Formulation A crystalline solid
Purity ≥95%
Stability 2 years
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
SMILES
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Fc1ccc(cc1)​Nc1n[nH]​c2ncnc(N)​c12
InCHI Code
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​1S/C11H9FN6/c12-6-1-3-7(4-2-6)​16-11-8-9(13)​14-5-15-10(8)​17-18-11/h1-5H,(H4,13,14,15,16,17,18)​
InCHI Key
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UQPMANVRZYYQMD-UHFFFAOYSA-N

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CGP 57380 is available in the following screening library:

Size Price Quantity Subtotal
1 mg $35.00 $0.00
5 mg $88.00 $0.00
10 mg $119.00 $0.00
25 mg $245.00 $0.00
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Pricing updated 2015-05-22. Prices are subject to change without notice.

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