13322  CGP 57380

MNK1 Inhibitor (CAS 522629-08-9)

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  U. Knauf, C. Tschopp and H. Gram. Negative regulation of protein translation by mitogen-activated protein kinase-interacting kinases 1 and 2. Molecular and Cellular Biology 21(16) 5500-5511 (2001).
2  R. M. Rowlett, C. A. Chrestensen, M. Nyce, et al. MNK kinases regulate multiple TLR pathways and innate proinflammatory cytokines in macrophages. American Journal of Physiology and Gastrointestinal Liver Physiology 294 452-459 (2008).

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Size Price Quantity
1 mg €44.00
5 mg €110.00
10 mg €149.00
25 mg €307.00
Pricing updated 2017-01-19.
Prices are subject to change without notice.