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MRT68921 HCl

Catalog No. T5356   CAS 2070014-87-6

MRT68921 hydrochloride is a potent inhibitor of both ULK1 and ULK2 (IC50s: 2.9 and 1.1 nM, respectively).

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MRT68921 HCl Chemical Structure
MRT68921 HCl, CAS 2070014-87-6
Pack Size Availability Price/USD Quantity
1 mg In stock $ 37.00
5 mg In stock $ 60.00
10 mg In stock $ 95.00
25 mg In stock $ 198.00
50 mg In stock $ 358.00
100 mg In stock $ 446.00
1 mL * 10 mM (in DMSO) In stock $ 61.00
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Purity: 99.86%
Purity: 99.15%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description MRT68921 hydrochloride is a potent inhibitor of both ULK1 and ULK2 (IC50s: 2.9 and 1.1 nM, respectively).
Targets&IC50 ULK2:1.1 nM, ULK1:2.9 nM
In vitro MRT68921 is the most potent inhibitor of both ULK1 and ULK2, with greater than a 15-fold reduction in the IC50 for ULK1 (2.9 nM) and greater than a 30-fold reduction for ULK2 (1.1 nM). MRT68921 (1 μM) was sufficient to reduce phospho-ATG13 to control levels, and in line with the in vitro IC50 values [1]. Pre-incubating the cells for 30 min with the ULK1 inhibitor MRT68921 at the optimal concentration of 100 nM prevented the forskolin-induced CYTO-ID staining. The same effect was observed with siRNA against ULK1 [2].
Kinase Assay Initial ULK1 kinase assays were performed with GST-ULK1, produced in Sf9 cells. For other experiments, recombinant GST-ULK1 (wild type, kinase-dead (K46I), and M92T and M92Q) was expressed in 293T cells, purified, and eluted from a glutathione-Sepharose column. Kinase assays were 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 were prewarmed to 25 °C for 5 min. Reactions were stopped by the addition of sample buffer, followed by SDS-PAGE, transfer to nitrocellulose, and analysis by autoradiography and immunoblot. For IC50 curve measurements, kinase assays were performed, using myelin basic protein as a substrate [1].
Cell Research Immortalized wild-type mouse embryonic fibroblasts (MEFs) have been described previously. 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) unless indicated. MRT67307 (10 μM), MRT68921 (1 μM), AZD8055 (1 μM), or bafilomycin A1 (50 nM) was included where indicated. Transfection and transduction were as described [1].
Molecular Weight 471.04
Formula C25H34N6O·HCl
CAS No. 2070014-87-6

Storage

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

Solubility Information

DMSO: 4.71 mg/mL (10 mM), Sonification is recommended

H2O: 10 mg/mL

TargetMolReferences and Literature

1. Petherick KJ, et al. Pharmacological inhibition of ULK1 kinase blocks mammalian target of rapamycin (mTOR)-dependent autophagy. J Biol Chem. 2015 May 1;290(18):11376-83. 2. Skah S, et al. cAMP-mediated autophagy inhibits DNA damage-induced death of leukemia cells independent of p53. Oncotarget. 2018 Jul 13;9(54):30434-30449.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Bioactive Compound Library Anti-COVID-19 Compound Library Kinase Inhibitor Library Bioactive Compounds Library Max Target-Focused Phenotypic Screening Library Autophagy Compound Library

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Keywords

MRT68921 HCl 2070014-87-6 Autophagy MRT-68921 HCl inhibitor inhibit

 

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