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Products
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A 769662
Cat. No. KS-290
Structure:
4-Hydroxy-3-(2′-hydroxy-[1,1′-biphenyl]-4-yl)-6-oxo-6,7-dihydrothieno[2,3-b]pyridine-5-carbonitrile
Activity:
AMPK activator
A 769662 is a potent and reversible AMP-activated protein kinase (AMPK) allosteric activator with an EC50 of 0.8 μM, that displays selectivity towards β1 subunit-containing heterotrimers, activating AMPK by binding to the β and γ subunits and not the AMP binding site. AMPK is a key cellular energy sensor and regulator of metabolic homeostasis and activation of AMPK provides beneficial outcomes in fighting against metabolic disorders such as insulin resistance and type 2 diabetes. In vivo, A 769662 inhibits fatty acid biosynthesis in rat hepatocytes and decreases plasma glucose and triglyceride levels. In ob/ob mice, A-769662 inhibits the rate of whole-body fatty acid oxidation, decreases body weight gain, reduces triglycerides and lowers glucose levels. A 769662 also inhibits proliferation of mesenchymal stem cells and impedes reprogramming of mouse embryonic fibroblasts to induced pluripotent stem cells (iPSCs).
Cool et al (2006) Identification and characterization of a small molecule AMPK activator that treats key components of type 2 diabetes and the metabolic syndrome. Cell Metab. 3(6) 403 PMID: 16753576
Scott et al (2008) Thienopyridone drugs are selective activators of AMP-activated protein kinase beta1-containing complexes. Chem Biol. 15(11) 1220 PMID: 19022182
Vazquez-Martin et al (2012) Activation of AMP-activated protein kinase (AMPK) provides a metabolic barrier to reprogramming somatic cells into stem cells. Cell Cycle 5 974 PMID: 2233578
Ducommun et al (2014) Enhanced activation of cellular AMPK by dual-small molecule treatment: AICAR and A769662. Am J Physiol Endocrinol Metab. 306(6) E688 PMID: 24425763
Abdallah and Alzahrani (2021) A-769662 stimulates the differentiation of bone marrow-derived mesenchymal stem cells into osteoblasts via AMP-activated protein kinase-dependent mechanism. J Appl Biomed. 19(3) 159 PMID: 34907759
Related areas
All small molecules >
All kinase modulators >
All diabetes research categories >
All stem cell research categories >
Technical Data
| Structure | 4-Hydroxy-3-(2′-hydroxy-[1,1′-biphenyl]-4-yl)-6-oxo-6,7-dihydrothieno[2,3-b]pyridine-5-carbonitrile |
| CAS Number | 844499-71-4 |
| Molecular Weight | 360.39 |
| Formula | C20H12N2O3S |
Solubility and Storage
| Solubility | Soluble in DMSO up to 30 mg/ml or in ethanol up to 5 mg/ml |
| Appearance | White solid |
| Storage | Store dry, frozen and in the dark |
Batch Specific Data
| Purity | 98% by HPLC, NMR conforms |
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Recent citations
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