MRT68921 HCl

Catalog No.S7949

MRT68921 HCl Chemical Structure

Molecular Weight(MW): 434.58 (free base)

MRT68921 is a potent and dual autophagy kinase ULK1/2 inhibitor with IC50 of 2.9 nM and 1.1 nM, respectively.

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  • Methods Enzymol. 2017, 587:391-404. MRT68921 HCl purchased from Selleck.

Purity & Quality Control

Choose Selective Autophagy Inhibitors

Biological Activity

Description MRT68921 is a potent and dual autophagy kinase ULK1/2 inhibitor with IC50 of 2.9 nM and 1.1 nM, respectively.
Targets
ULK2 [1]
(Cell-free assay)
ULK1 [1]
(Cell-free assay)
1.1 nM 2.9 nM
In vitro

MRT68921 specifically disrupts autophagosome maturation and thus blocks autophagic flux through ULK1 inhibition. [1]

Protocol

Kinase Assay:

[1]

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Kinase Assays:

Initial ULK1 kinase assays are performed with GST-ULK1, produced in Sf9 cells, which is described on the MRC-PPU Reagents website. For other experiments, recombinant GST-ULK1 (wild type, kinase-dead (K46I), and M92T and M92Q) is expressed in 293T cells, purified, and eluted from a glutathione-Sepharose column. Kinase assays are carried out in 50 mM Tris-HCl, pH 7.4, 10 mM magnesium acetate, 0.1 mM EGTA, and 0.1% β-mercaptoethanol, containing 30 μM cold ATP, and 0.5 μCi of [γ-32P]ATP for 5 min at 25 °C. Prior to ATP addition, reaction mixes are prewarmed to 25 °C for 5 min. Reactions are stopped by the addition of sample buffer, followed by SDS-PAGE, transfer to nitrocellulose, and analysis by autoradiography and immunoblot.
Cell Research:

[1]

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  • Cell lines: MEFs and 293T cells
  • Concentrations: 1 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 Insoluble warmed
Water Insoluble
Ethanol Insoluble

* 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 434.58 (free base)
Formula

C25H34N6O·xHCl

CAS No. 1190379-70-4 (free base)
Storage powder
in solvent
Synonyms N/A

Bio Calculators

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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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Autophagy Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID