CGP 57380

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. It blocks the phosphorylation of eIF4E in response to TNF-alpha, arsenite, anisomycin, PMA, or fetal calf serum in 293 cells (IC50 = 3 µM). CGP 57380 also dose-dependently inhibits TNF-alpha 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.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: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml, Ethanol: 0.25 mg/ml. lambdamax: 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.