MRT 67307 dihydrochloride

Biological Activity

MRT 67307 dihydrochloride is a salt inducible kinase (SIK) inhibitor (IC₅₀ values are 67, 250 and 430 nM for SIK2, SIK1 and SIK3 respectively) and a potent inhibitor of ULK1 and 2 (IC₅₀ values of 45 and 38 nM, respectively). MRT 67307 dihydrochloride 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.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. Pharmacological modulation of autophagy: therapeutic potential and persisting obstacles.
   Galluzzi et al.
   Nat.Rev.Drug.Discov., 2017;
2. 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
3. Novel cross-talk within the IKK family controls innate immunity.
   Clark et al.
   Biochem.J., 2011;434:93
4. 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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