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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. Inhibits autophagy.

Clark et al (2012) Phosphorylation of CRTC3 by the salt-inducible kinases controls the interconversion of classically activated and regulatory macrophages. Proc.Natl.Acad.Sci.U.S.A. 109 16986 PMID:23033494 |Clark et al (2011) Novel cross-talk within the IKK family controls innate immunity. Biochem.J. 434 93 PMID:21138416 |Smith et al (2011) The role of TBK1 and IKKe in the expression and activation of Pellino 1. Biochem.J. 434 537 PMID:21204785 |Galluzzi et al (2017) Pharmacological modulation of autophagy: therapeutic potential and persisting obstacles. Nat.Rev.Drug.Discov. PMID:28529316

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