MRT 67307 dihydrochloride

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Cat.No. 5134 - MRT 67307 dihydrochloride | C26H36N6O2.2HCl
Description: Salt inducible kinase (SIK) inhibitor
Chemical Name: N-[3-[[5-Cyclopropyl-2-[[3-(4-morpholinylmethyl)phenyl]amino]-4-pyrimidinyl]amino]propyl]cyclobutanecarboxamide dihydrochloride
Purity: ≥98% (HPLC)
Datasheet
Citations
Literature

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. Inhibits autophagy.

Technical Data

M. Wt 537.52
Formula C26H36N6O2.2HCl
Storage Desiccate at RT
Purity ≥98% (HPLC)
PubChem ID 90489013
InChI Key ZIKXPHATVRPOQG-UHFFFAOYSA-N
Smiles O=C(C5CCC5)NCCCNC1=C(C4CC4)C=NC(NC2=CC(CN3CCOCC3)=CC=C2)=N1.Cl.Cl

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 53.75 100
water 10.75 20

Preparing Stock Solutions

The following data is based on the product molecular weight 537.52. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
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

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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: 8529316


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Keywords: MRT67307 dihydrochloride salt inducible kinase SIK inhibitors inhibits TBK1 IKKε IKKepsilon IKKe MARK NUAK Other Kinases

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Cancer

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