MRT67307 HCl

Catalog No.S7948

MRT67307 HCl Chemical Structure

Molecular Weight(MW): 464.6 (free-base)

MRT67307 is a potent and dual IKKϵ and TBK1 inhibitor with IC50 of 160 and 19 nM, respectively.

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Cited by 4 Publications

2 Customer Reviews

  • Methods Enzymol. 2017, 587:391-404. MRT67307 HCl purchased from Selleck.

    (C) MRT67307 treatment and (D) inhibited the effect of BAI on p-TBK1.

    Mol Med Rep, 2018, 17(2):3085-3091. MRT67307 HCl purchased from Selleck.

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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.
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]

Protocol

Kinase Assay:

[1]

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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]

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  • 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.


    (Only for Reference)

Solubility (25°C)

In vitro DMSO 92 mg/mL warmed
Water 92 mg/mL
Ethanol 92 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 464.6 (free-base)
Formula

C26H36N6O2· xHCl

CAS No. 1190378-57-4 (free-base)
Storage powder
in solvent
Synonyms N/A

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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

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID