MRT68921 (dihydrochloride)

MRT68921 dihydrochloride is a potent NUAK1/ULK1 dual inhibitor. MRT68921 dihydrochloride inhibits ULK1 and ULK2 with IC50 values of 2.9 nM and 1.1 nM, respectively. MRT68921 dihydrochloride can block cells autophagy and kill tumor cells by breaking the balance of oxidative stress signals. MRT68921 dihydrochloride can inhibit cell proliferation and induce ROS production and apoptosis. MRT68921 dihydrochloride can be used for the research of cancer, such as breast cancer[1][2].

Product Specifications

CAS Number

[2080306-21-2]

UNSPSC

12352005

Hazard Statement

H315, H319, H335

Target

Apoptosis; Bcl-2 Family; GSK-3; Reactive Oxygen Species (ROS) ; ULK

Type

Reference compound

Related Pathways

Apoptosis; Autophagy; Immunology/Inflammation; Metabolic Enzyme/Protease; NF-κB; PI3K/Akt/mTOR; Stem Cell/Wnt

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/MRT68921-hydrochloride.html

Concentration

10mM

Purity

99.67

Solubility

DMSO : 8.33 mg/mL (ultrasonic; warming; heat to 60°C) |H2O : 20.83 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

[H]Cl.O=C(C1CCC1)NCCCNC2=NC(NC3=CC4=C(CN(C)CC4)C=C3)=NC=C2C5CC5.[H]Cl

Molecular Formula

C25H36Cl2N6O

Molecular Weight

507.50

Precautions

H315, H319, H335

References & Citations

[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]Chen Y, et al. Dual targeting of NUAK1 and ULK1 using the multitargeted inhibitor MRT68921 exerts potent antitumor activities. Cell Death Dis. 2020 Sep 1;11 (8) :712.