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MRT67307

Catalog No. T0097   CAS 1190378-57-4
Synonyms: MRT67307 HCl

Through its effects on ULK1 and ULK2, MRT67307 blocks autophagy. MRT67307 prevents the phosphorylation of IRF3 and the production of IFN-β and increases toll-like receptor-induced IL-10 and IL-1ra secretion in macrophages. MRT67307 is a kinase inhibitor that has been shown to inhibit TBK1, MARK1-4, IKKε, and NUAK1 (IC50 values are 19, 27-52, 160, and 230 nM, respectively), the salt-inducible kinases (SIKs; IC50s =250, 67, and 430 nM for SIK1, SIK2, and SIK3, respectively) and ULK1 and ULK2 (IC50s = 45 and 38 nM, respectively).

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MRT67307 Chemical Structure
MRT67307, CAS 1190378-57-4
Pack Size Availability Price/USD Quantity
1 mg In stock $ 34.00
5 mg In stock $ 77.00
10 mg In stock $ 127.00
25 mg In stock $ 252.00
50 mg In stock $ 486.00
100 mg In stock $ 692.00
1 mL * 10 mM (in DMSO) In stock $ 80.00
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Purity: 99.79%
Purity: 99.25%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Through its effects on ULK1 and ULK2, MRT67307 blocks autophagy. MRT67307 prevents the phosphorylation of IRF3 and the production of IFN-β and increases toll-like receptor-induced IL-10 and IL-1ra secretion in macrophages. MRT67307 is a kinase inhibitor that has been shown to inhibit TBK1, MARK1-4, IKKε, and NUAK1 (IC50 values are 19, 27-52, 160, and 230 nM, respectively), the salt-inducible kinases (SIKs; IC50s =250, 67, and 430 nM for SIK1, SIK2, and SIK3, respectively) and ULK1 and ULK2 (IC50s = 45 and 38 nM, respectively).
Targets&IC50 TBK1:190 nM, IKKϵ:160 nM
In vitro In macrophages, MRT67307 prevents the phosphorylation of IRF3 and the production of IFNβ. In wild-type MEFs, MRT67307 enhances the IL-1-stimulated phosphorylation of p105 at Ser933 and RelA at both Ser468 and Ser536, and also enhances IL-1-stimulated activation of NF-κB-dependent gene transcription. [1] MRT67307 increases IL-10 production and suppresses proinflammatory cytokine production via a cAMP response element-Binding protein (CREB)-regulated transcriptional coactivator (CRTC) 3 Dependent Mechanism. [2] In addition, MRT67307 inhibit ULK and block autophagy in MEF cells. [3]
Kinase Assay Substrates and kinases are diluted in 50?mM Tris/HCl (pH?7.5), 0.1% 2-mercaptoethanol, 0.1?mM EGTA and 10?mM magnesium acetate. Reactions are initiated with [γ-32P]ATP (2500 c.p.m./pmol) to a final concentration of 0.1?mM and terminated after 15?min at 30°C by the addition of SDS and EDTA (pH?7.0) to final concentrations of 1.0% (w/v) and 20?mM respectively. After heating for 5?min at 100°C and separation by SDS/PAGE, the phosphorylated proteins are detected by autoradiography.
Cell Research Cells are rinsed in ice-cold PBS and extracted in lysis buffer (50 mM Tris·HCl at pH 7.4, 1 mM EDTA, 1 mM EGTA, 50 mM NaF, 5 mM sodium pyrophosphate, 10 mM sodium β-glycerol 1-phosphate, 1 mM DTT, 1 mM sodium orthovanadate, 0.27mol/Lsucrose, 1% (vol/vol) Triton X-100, 1 μg/mL aprotinin, 1 μg/ mL leupeptin, and 1 mM phenylmethylsulphonyl fluoride). Cell extracts are clarified by centrifugation at 14,000 × g for 10 min at 4°C, and protein concentrations are determined by using the Bradford assay. FLAG-CRTC3 is purified on anti-FLAG M2 agarose, whereas endogenous CRTC3 is immunoprecipitated from cell extracts by using anti-CRTC3 raised against the peptide CWKEEKHPGFR (S277D bleed 2) and coupled to Protein GSepharose. To detect proteins in cell lysates, 20 μg of protein extract is separated by SDS/PAGE. After transfer to PVDF membranes, proteins are detected by immunoblotting and visualized by treating the blots with ECL followed by autoradiography. The following antibodies are used for immunoblotting: pSer133 CREB, pSer171 CRTC2, total CRTC2, GAPDH, total STAT3, pTyr705 STAT3, FLAG (M2 clone), CRTC3, HA (3F10), and 14-3-3; and antibodies against pSer329 (S256D bleed 2) and pSer370 (S253D bleed 2) of CRTC3 are raised against the phosphopeptides GLQSSRpSNPSIQ and RLFSLpSNPSLST.
Synonyms MRT67307 HCl
Molecular Weight 464.6
Formula C26H36N6O2
CAS No. 1190378-57-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 83 mg/mL(178.6 mM)

Ethanol: 83 mg/mL(178.6 mM)

TargetMolReferences and Literature

1. Clark K, et al. Biochem J. 2011, 434(1), 93-104. 2. Clark K, et al. Proc Natl Acad Sci U S A. 2012, 109(42), 161986-161991. 3. Petherick KJ, et al. J Biol Chem. 2015, 290(18), 11376-11383.

Related compound libraries

This product is contained In the following compound libraries:
Bioactive Compounds Library Max Autophagy Compound Library Anti-Liver Cancer Compound Library Kinase Inhibitor Library Antidepressant Compound Library Bioactive Compound Library Anti-Breast Cancer Compound Library Inhibitor Library NO PAINS Compound Library Anti-Ovarian Cancer Compound Library

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Keywords

MRT67307 1190378-57-4 Autophagy NF-Κb IκB/IKK MRT 67307 Inhibitor ULK2 ULK IKKε MRT-67307 inhibit IKK MRT67307 HCl ULK1 cancer IκB kinase signal TBK-1 Unc-51 like kinase I kappa B kinase transduction inhibitor

 

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