A-769662

A-769662 is a AMP-activated protein kinase (AMPK) activator. A-769662 inhibits the function of the 26S proteasome by an AMPK-independent mechanism and leads to cell cycle arrest. A-769662 directly stimulates partially purified rat liver AMPK (EC50 = 0.8 μM) and inhibits fatty acid synthesis in primary rat hepatocytes (IC50 = 3.2 μM) . A-769662 can alleviate the symptoms of metabolic diseases such as type 2 diabetes[1][2][3][4].

Product Specifications

CAS Number

[844499-71-4]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

AMPK

Type

Reference compound

Related Pathways

Epigenetics; PI3K/Akt/mTOR

Applications

Cancer-Kinase/protease

Field of Research

Metabolic Disease

Assay Protocol

https://www.medchemexpress.com/A-769662.html

Purity

99.33

Solubility

DMSO : 50 mg/mL (ultrasonic; warming; heat to 80°C)

Smiles

N#CC1C(C2=C(NC1=O)SC=C2C3=CC=C(C4=CC=CC=C4O)C=C3)=O

Molecular Formula

C20H12N2O3S

Molecular Weight

360.39

Precautions

H302, H315, H319, H335

References & Citations

[1]Cool B, et al. Identification and characterization of a small molecule AMPK activator that treats key components of type 2 diabetes and the metabolic syndrome. Cell Metab, 2006, 3 (6), 403-416.|[2]Sanders MJ, et al. Defining the mechanism of activation of AMP-activated protein kinase by the small molecule A-769662, a member of the thienopyridone family. J Biol Chem, 2007, 282 (45), 32539-32548.|[3]Moreno D, et al, A769662, a novel activator of AMP-activated protein kinase, inhibits non-proteolytic components of the 26S proteasome by an AMPK-independent mechanism. FEBS Lett, 2008, 583 (17), 2650-2654.|[4]Yerra VG, et al. Adenosine Monophosphate-Activated Protein Kinase Abates Hyperglycaemia-Induced Neuronal Injury in Experimental Models of Diabetic Neuropathy: Effects on Mitochondrial Biogenesis, Autophagy and Neuroinflammation. Mol Neurobiol. 2017 Apr;54 (3) :2301-2312.