Home NF-κB IκB/IKK inhibitor - TBK1 inhibitor - ULK inhibitor - Autophagy inhibitor MRT67307 HCl

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MRT67307 HCl IκB/IKK inhibitor

Cat.No.S7948

MRT67307 is a potent and dual IKKϵ and TBK1 inhibitor with IC50 of 160 and 19 nM, respectively. MRT67307 potently inhibits ULK1 and ULK2 and blocks autophagy.
MRT67307 HCl IκB/IKK inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 464.6 (free-base)

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Quality Control

Chemical Information, Storage & Stability

Molecular Weight 464.6 (free-base) Formula

C26H36N6O2· xHCl

 Storage (From the date of receipt)
CAS No. 1781882-89-0 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles C1CC(C1)C(=O)NCCCNC2=NC(=NC=C2C3CC3)NC4=CC=CC(=C4)CN5CCOCC5

Solubility

In vitro
Batch:

DMSO : 92 mg/mL
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 92 mg/mL

Ethanol : 92 mg/mL

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Mechanism of Action

Targets/IC50/Ki
TBK1 [1]
(Cell-free assay)
19 nM
IKKϵ [1]
(Cell-free assay)
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
Protein kinase assays
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.
References

Applications

Methods Biomarkers Images PMID
Western blot pSTAT3 / STAT3 p-IRF3 / IRF3 / pTBK1 / TBK1 / IKKε S7948-WB2 24444711

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