CGP 57380

Cayman Chemical Item Number 13322

MNK1 Inhibitor (CAS 522629-08-9)

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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).

  • 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
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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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Cart Total $0.00

Pricing updated 2015-08-02. Prices are subject to change without notice.

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Warning This product is not for human or veterinary use.

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Cayman Chemical was formed over thirty years ago by demonstrating the value of naturally growing gorgonian corals as a renewable, economically viable source of prostaglandins. Today we operate our business knowing that we owe our start to the renewable resources our environment had provided. As Cayman Chemical continues to grow we consistently evaluate our business processes to ensure we are operating at the highest environmental standards.

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Ann Arbor, Michigan 48108 USA


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