MRT67307 HCl

Catalog No.S7948

For research use only.

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 Chemical Structure

CAS No. 1781882-89-0

Selleck's MRT67307 HCl has been cited by 14 publications

Purity & Quality Control

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Biological Activity

Description 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.
Targets
IKKϵ [1]
(Cell-free assay)
TBK1 [1]
(Cell-free assay)
160 nM 190 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]

Assay
Methods Test Index PMID
Western blot p-IRF3 / IRF3 / pTBK1 / TBK1 / IKKε ; pSTAT3 / STAT3 24444711

Protocol (from reference)

Kinase Assay:

[1]

  • 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.

Cell Research:

[3]

  • Cell lines: MEFs and 293T cells
  • Concentrations: 10 μM
  • Incubation Time: 1 h
  • Method:

    MEFs and 293T cells were grown in DMEM, supplemented with 10% fetal bovine serum and penicillin/streptomycin, and cultured at 37 °C, 5% CO2. For induction of autophagy, cells were typically grown to 75% confluency, washed twice, and incubated in Earle's balanced salt solution (EBSS) for 1 h (or complete medium as a control) in the presence or absence of 10 μM MRT67307, 1 μM MRT68921, or 50 nM bafilomycin A1 and followed by lysis and immunoblotting with the indicated antibodies.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 464.6 (free-base)
Formula

C26H36N6O2· xHCl

CAS No. 1781882-89-0
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CC(C1)C(=O)NCCCNC2=NC(=NC=C2C3CC3)NC4=CC=CC(=C4)CN5CCOCC5

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

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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