MRT 67307 dihydrochloride

Name: MRT 67307 dihydrochloride
Brand: Tocris Bioscience
SKU: 5134

Tocris Bioscience, part of Bio-Techne | Catalog # 5134

Citations (2)

COA / SDS

Salt inducible kinase (SIK) inhibitor; also ULK1 and 2 inhibitor

Key Product Details

Description:	Salt inducible kinase (SIK) inhibitor; also ULK1 and 2 inhibitor
Chemical Name:	N-[3-[[5-Cyclopropyl-2-[[3-(4-morpholinylmethyl)phenyl]amino]-4-pyrimidinyl]amino]propyl]cyclobutanecarboxamide dihydrochloride
Purity:	≥98% (HPLC)
Molecular Weight:	537.52

View Full Technical Details for MRT 67307 dihydrochloride

Technical Data
Citations

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

M. Wt	537.52
Formula	C₂₆H₃₆N₆O₂.2HCl
Storage	Desiccate at RT
Purity	≥98% (HPLC)
CAS Number	1781882-89-0
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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for MRT 67307 dihydrochloride

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

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	9.30 mL	18.60 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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References for MRT 67307 dihydrochloride

References are publications that support the biological activity of the product.

Petherick Pharmacological inhibition of ULK1 kinase blocks mammalian target of rapamycin (mTOR)-dependent autophagy. J.Biol.Chem. 2015 PMID: 26614783
Galluzzi Pharmacological modulation of autophagy: therapeutic potential and persisting obstacles. Nat.Rev.Drug.Discov. 2017 PMID: 28529316
Clark Novel cross-talk within the IKK family controls innate immunity. Biochem.J. 2011 PMID: 21138416
Smith The role of TBK1 and IKKe in the expression and activation of Pellino 1. Biochem.J. 2011 PMID: 21204785
Clark Phosphorylation of CRTC3 by the salt-inducible kinases controls the interconversion of classically activated and regulatory macrophages. Proc.Natl.Acad.Sci.U.S.A. 2012 PMID: 23033494