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A 769662
- Soluble in DMSO
- MF: C20H12N2O3S
- MW: 360.39
Description
A 769662 is a direct and selective AMP-activated protein kinase activator that preferentially activates AMPK complexes containing the β1 regulatory subunit.
A 769662 activates AMPK allosterically and protects Thr172 from dephosphorylation, mimicking key effects of AMP without altering cellular nucleotide levels. It is a benchmark tool for energy sensing, metabolism, autophagy and cardiovascular signaling.
Key Features
- Direct allosteric AMPK activator
- Selective for β1-containing AMPK complexes
- Inhibits dephosphorylation of AMPK Thr172
- Activates AMPK independently of changes in AMP/ATP ratio
Applications
- AMPK activity and target-engagement assays
- Cellular energy-sensing and metabolic studies
- Autophagy and mTOR pathway research
- Glucose, lipid and cardiovascular signaling models
More Information
| Parent CAS No. | 844499-71-4 |
|---|---|
| Chemical Name | 6,7-Dihydro-4-hydroxy-3-(2'-hydroxy[1,1'-biphenyl]-4-yl )-6-oxo-thieno[2,3-b]pyridine-5-carbonitrile |
| SMILES | C1(C2C3C(O)=C(C#N)C(=O)NC=3SC=2)C=CC(C2C(O)=CC=CC=2)=CC=1 |
| MFCD | MFCD11977269 |
| InChi | InChI=1S/C20H12N2O3S/c21-9-14-18(24)17-15(10-26-20(17)22-19(14)25)12-7-5-11(6-8-12)13-3-1-2-4-16(13)23/h1-8,10,23H,(H2,22,24,25) |
| InChiKey | CTESJDQKVOEUOY-UHFFFAOYSA-N |
| CID | 54708532 |
| Short Description | AMPK activator |
References
- B Cool et al. Identification and characterization of a small molecule AMPK activator that treats key components of type 2 diabetes and the metabolic syndrome. Cell Metabolism. 2006, 3, 403.
- M Sanders 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, 32539.
- O Göransson et al. Mechanism of Action of A-769662, a Valuable Tool for Activation of AMP-activated Protein Kinase. J. Biol. Chem. 2007, 282, 32549-32560.
- JW Scott et al. Thienopyridone drugs are selective activators of AMP-activated protein kinase β1-containing complexes. Chem. Biol. 2008, 15, 1220.
- JT Treebak et al. A-769662 activates AMPK β1-containing complexes but induces glucose uptake through a PI3 kinase-dependent pathway in mouse skeletal muscle. Am. J. Physiol. Cell Physiol. 2009, 297(4), C1041-C1052.
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