Inhibitor of MAPK-interacting kinase1
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CGP 57380

Item No. 13322

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N3-(4-fluorophenyl)-1H-pyrazolo[3,4-d]pyrimidine-3,4-diamine
CAS Number
522629-08-9
Synonyms
  • MNK1 Inhibitor
Molecular Formula
C11H9FN6
Formula Weight
244.2
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/mlEthanol: 0.25 mg/ml
λmax
204, 235, 260, 303 nm
SMILES
Fc1ccc(cc1)Nc1n[nH]c2ncnc(N)c12
InChi Code
InChI=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
UQPMANVRZYYQMD-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    CGP 57380 is a selective inhibitor of MAP kinase-interacting kinase 1 (MNK1) in vitro (IC50 = 2.2 μM), with no inhibitory activity against p38, JNK1, ERK1/2, PKC, or Src-like kinases.1 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

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    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(2), 452-459 (2008).