MRT 67307 dihydrochloride
Tocris Bioscience, part of Bio-Techne | Catalog # 5134
Salt inducible kinase (SIK) inhibitor; also ULK1 and 2 inhibitor
Key Product Details
Description
Salt inducible kinase (SIK) inhibitor; also ULK1 and 2 inhibitor
Product Description
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.Product Specifications
Molecular Weight
537.52
Formula
C26H36N6O2.2HCl
Storage
Desiccate at RT
Purity
≥98% (HPLC)
Chemical Name
N-[3-[[5-Cyclopropyl-2-[[3-(4-morpholinylmethyl)phenyl]amino]-4-pyrimidinyl]amino]propyl]cyclobutanecarboxamide dihydrochloride
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.
Solubility
| 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 all 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 |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
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
Product Specific Notices for MRT 67307 dihydrochloride
For research use only
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