MRT68921 HCl

Catalog No.S7949 Batch:S794904

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Technical Data

Formula

C25H34N6O·xHCl
Molecular Weight 434.58 (free base) CAS No. 2070014-87-6
Solubility (25°C)* In vitro DMSO 10 mg/mL
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5% DMSO 95% corn oil
0.5mg/ml Taking the 1 mL working solution as an example, add 50 μL of 10 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
0.5mg/ml Taking the 1 mL working solution as an example, add 50 μL of 10 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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]
In vivo

MRT68921 is a potent and dual autophagy kinase ULK1/2 inhibitor.

Protocol (from reference)

Kinase Assay:

[1]
  • 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 Assay:

[1]
  • 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.
Animal Study:

[2]
  • Animal Models

    Female BALB/c mice

  • Dosages

    20 mg/kg

  • Administration

    s.c.

Customer Product Validation

, , Methods Enzymol. 2017, 587:391-404

Data from [Data independently produced by , , Mol Carcinog, 2018, 57(3):319-332]

Selleck's MRT68921 HCl has been cited by 42 publications

Exposure of the inner mitochondrial membrane triggers apoptotic mitophagy [ Cell Death Differ, 2024, 10.1038/s41418-024-01260-2] PubMed: 38396150
Synthetic lethality of combined ULK1 defection and p53 restoration induce pyroptosis by directly upregulating GSDME transcription and cleavage activation through ROS/NLRP3 signaling [ J Exp Clin Cancer Res, 2024, 43(1):248] PubMed: 39215364
Starvation-induced phosphorylation activates gasdermin A to initiate pyroptosis [ Cell Rep, 2024, 43(9):114728] PubMed: 39264808
Chronic hypoxia stabilizes 3βHSD1 via autophagy suppression [ Cell Rep, 2024, 43(1):113575] PubMed: 38181788
ATG7/GAPLINC/IRF3 axis plays a critical role in regulating pathogenesis of influenza A virus [ PLoS Pathog, 2024, 20(1):e1011958] PubMed: 38227600
ULK2 Is a Key Pro-Autophagy Protein That Contributes to the High Chemoresistance and Disease Relapse in FLT3-Mutated Acute Myeloid Leukemia [ Int J Mol Sci, 2024, 25(1)646] PubMed: 38203816
TECPR1 is activated by damage-induced sphingomyelin exposure to mediate noncanonical autophagy [ EMBO J, 2023, 42(17):e113105] PubMed: 37409525
Phosphorylation of phase-separated p62 bodies by ULK1 activates a redox-independent stress response [ EMBO J, 2023, e113349.] PubMed: 37306101
PROX1 induction by autolysosomal activity stabilizes persister-like state of colon cancer via feedback repression of the NOX1-mTORC1 pathway [ Cell Rep, 2023, S2211-1247(23)00530-2] PubMed: 37224811
Tubeimoside-2 Triggers Methuosis in Hepatocarcinoma Cells through the MKK4-p38α Axis [ Pharmaceutics, 2023, 15(4)1093] PubMed: 37111582

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.