Catalog Number: 5240
Chemical Name: 4-[(3-Chloro-4-fluorophenyl)amino]-6-[(3-pyridinylmethyl)amino]-1,7-naphthyridine-3-carbonitrile
Biological Activity
Potent and selective Tpl2 (Cot; MAP3K8) inhibitor (IC50 = 50 nM). Selective for Tpl2 over MEK, p38, Src, MK2, PKC and EGFR. Inhibits LPS-induced TNF-α secretion from monocytes and attenuates acute myeloid leukemia (AML) cell proliferation in vitro. Also reduces cytolytic activity of human CD8+ cytotoxic T lymphocytes. Cell permeable.
Technical Data
  • M.Wt:
    404.83
  • Formula:
    C21H14ClFN6
  • Solubility:
    Soluble to 100 mM in DMSO
  • Purity:
    >99%
  • Storage:
    Store at -20°C
  • CAS No:
    871307-18-5
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Pharmacological inhibition of TPL2/MAP3K8 blocks human cytotoxic T lymphocyte effector functions.
    Chowdhury et al.
    PLoS ONE, 2014;9:e92187
  2. Inhibition of Cot1/Tlp2 oncogene in AML cells reduces ERK5 activation and up-regulates p27Kip1 concomitant with enhancement of differentiation and cell cycle arrest induced by silibinin and 1,25-dihydroxyvitamin D3.
    Wang et al.
    Cell Cycle, 2010;9:4542
  3. Inhibition of Tpl2 kinase and TNF-α production with 1,7-naphthyridine-3-carbonitriles: synthesis and structure-activity relationships.
    Gavrin et al.
    Bioorg.Med.Chem.Lett., 2005;15:5288

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