Catalog Number: 5134
Chemical Name: N-[3-[[5-Cyclopropyl-2-[[3-(4-morpholinylmethyl)phenyl]amino]-4-pyrimidinyl]amino]propyl]cyclobutanecarboxamide dihydrochloride
Biological Activity
Salt inducible kinase (SIK) inhibitor (IC50 values are 67, 250 and 430 nM for SIK2, SIK1 and SIK3 respectively). Also inhibits TBK1, MARK1-4, IKKε and NUAK1 (IC50 values are 19, 27-52, 160 and 230 nM respectively). Has no effect on IKKα or IKKβ. Induces IL-10 secretion and inhibits TNF-α and IL-6 secretion in bacterial LPS-stimulated macrophages. Also enhances IL-1-induced activation of NFκB-dependent gene transcription in mouse embryonic fibroblast (MEF) cells.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 20 mM in water and to 100 mM in DMSO
  • Purity:
  • Storage:
    Desiccate at RT
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. Phosphorylation of CRTC3 by the salt-inducible kinases controls the interconversion of classically activated and regulatory macrophages.
    Clark et al.
    Proc.Natl.Acad.Sci.U.S.A., 2012;109:16986
  2. Novel cross-talk within the IKK family controls innate immunity.
    Clark et al.
    Biochem.J., 2011;434:93
  3. The role of TBK1 and IKKe in the expression and activation of Pellino 1.
    Smith et al.
    Biochem.J., 2011;434:537
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