Catalog Number: 4630
Chemical Name: 2-(4-Amino-1,2,5-oxadiazol-3-yl)-1-ethyl-N-4-piperidinyl-1H-imidazo[4,5-c]pyridine-7-methanamine dihydrochloride
Biological Activity
Potent, ATP-competitive mitogen- and stress-activated kinase 1 (MSK1) inhibitor (IC50 = 11 nM in an in vitro kinase assay); targets the N-terminal kinase domain. Inhibits MSK1, MSK2, PKA, PKB, RSK and p70S6K activity in cells. Blocks IL-10 production in macrophages.
Technical Data
  • M.Wt:
    415.32
  • Formula:
    C16H22N8O.2HCl
  • Solubility:
    Soluble to 50 mM in water and to 50 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Desiccate at RT
  • CAS No:
    1781882-72-1
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 with the permission of GlaxoSmithKline.
Background References
  1. (1H-imidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: a novel class of potent MSK-1-inhibitors.
    Bamford et al.
    Bioorg.Med.Chem.Lett., 2005;15:3402
  2. (1H-imidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: further optimisation as highly potent and selective MSK-1-inhibitors.
    Bamford et al.
    Bioorg.Med.Chem.Lett., 2005;15:3407
  3. Characterization of the cellular action of the MSK inhibitor SB-747651A.
    Naqvi et al.
    Biochem.J., 2012;441:347

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