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MRT 67307 dihydrochloride

Cat. No. 5134 1 Citation Submit a Review Datasheet / COA / SDS
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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)
Datasheet
Citations (1)
Reviews
Biological Activity Technical Data Solubility Calculators Datasheets References

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 Data 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.

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 for MRT 67307 dihydrochloride

Certificate of Analysis / Product Datasheet
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Safety Datasheet

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

If you know of a relevant reference for MRT 67307 dihydrochloride, please let us know.

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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

Do you know of a great paper that uses MRT 67307 dihydrochloride from Tocris? Please let us know.

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