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MRT 67307 dihydrochloride
Biological Activity for MRT 67307 dihydrochloride
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 for MRT 67307 dihydrochloride
|Storage||Desiccate at RT|
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.
Solubility Data for MRT 67307 dihydrochloride
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for MRT 67307 dihydrochloride
The following data is based on the product molecular weight 537.52. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.86 mL||9.3 mL||18.6 mL|
|5 mM||0.37 mL||1.86 mL||3.72 mL|
|10 mM||0.19 mL||0.93 mL||1.86 mL|
|50 mM||0.04 mL||0.19 mL||0.37 mL|
Product Datasheets for MRT 67307 dihydrochloride
References for MRT 67307 dihydrochloride
References are publications that support the biological activity of the product.
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. 16 487 PMID: 28529316
Petherick et al (2015) Pharmacological inhibition of ULK1 kinase blocks mammalian target of rapamycin (mTOR)-dependent autophagy. J.Biol.Chem. 290 28726 PMID: 26614783
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1 Citation for MRT 67307 dihydrochloride
Citations are publications that use Tocris products. Selected citations for MRT 67307 dihydrochloride include:
Alison et al (2020) LAP-like non-canonical autophagy and evolution of endocytic vacuoles in pancreatic acinar cells. Autophagy 16 1314-1331 PMID: 31651224
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Literature in this Area
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