Catalog Number: 5429
Chemical Name: N-[4-[(4-Ethyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-4-methyl-3-(1H-pyrrolo[2,3-b]pyridin-4-yloxy)benzamide
Biological Activity
TGF-β-activated kinase (TAK1) inhibitor (IC50 = 149 nM). Also inhibits LYN, MAP4K2 and Abl kinase activity (IC50 values are 12.9, 21.7 and 75.2 nM, respectively). Suppresses CpG A and CpG B-stimulated secretion of IFN-α and TLR7/8 agonist CL097-stimulated secretion of IFN-β in Gen 2.2 leukemia cells in vitro.
Technical Data
  • M.Wt:
    537.58
  • Formula:
    C29H30F3N5O2
  • Solubility:
    Soluble to 20 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Store at -20°C
  • CAS No:
    1315355-93-1
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.
Additional Information
Licensing Caveats:
Sold under license from Dana-Farber Cancer Institute.
Background References
  1. Discovery of type II inhibitors of TGFβ-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2).
    Tan et al.
    J.Med.Chem., 2015;58:183
  2. Essential role for IKKβ in production of type 1 interferons by plasmacytoid dendritic cells.
    Pauls et al.
    J.Biol.Chem., 2012;287:19216
  3. The IkappaB kinase family phosphorylates the Parkinson's disease kinase LRRK2 at Ser935 and Ser910 during Toll-like receptor signaling.
    Dzamko et al.
    PLoS ONE, 2012;7:e39132

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