Chemical Name: 6,7-Dihydro-4-hydroxy-3-(2'-hydroxy[1,1'-biphenyl]-4-yl)-6-oxo-thieno[2,3-b]pyridine-5-carbonitrile
Biological ActivityA 769662 is a potent, reversible AMP-activated protein kinase (AMPK) activator (EC50 = 0.8 μM) that displays selectivity towards β1 subunit-containing heterotrimers. Inhibits fatty acid synthesis (IC50 = 3.2 μM) and decreases plasma glucose and triglyceride levels in vivo. Also inhibits proliferation of mesenchymal stem cells, and impedes reprogramming of mouse embryonic fibroblasts to iPSCs. Activates autophagy.
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Role of AMP-activated protein kinase in regulating hypoxic survival and proliferation of mesenchymal stem cells.
de Meester et al.
Pharmacological modulation of autophagy: therapeutic potential and persisting obstacles.
Galluzzi et al.
Activation of AMP-activated protein kinase (AMPK) provides a metabolic barrier to reprogramming somatic cells into stem cells.
Vazquez-Martin et al.
Cell Cycle, 2012;5:974
MetF. activates a duodenal Ampk-dependent pathway to lower hepatic glucose production in rats.
Duca et al.
Defining the mechanism of activation of AMP-activated protein kinase by the small molecule A-769662, a member of the thienopyridone family.
Sanders et al.
Thienopyridone drugs are selective activators of AMP-activated protein kinase β1-containing complexes.
Scott et al.
Identification and characterization of a small molecule AMPK activator that treats key components of type 2 diabetes and the metabolic syndrome.
Cool et al.
Cell Met., 2006;3:403
Citations for A 769662
The citations listed below are publications that use Tocris products. Selected citations for A 769662 include:
24 Citations: Showing 1 - 10
Investigation of the specificity and mechanism of action of the ULK1/AMPK inhibitor SBI-0206965.
Authors: Ahwazi Et al.
Biochem J 2021;478:2977
AMPK activation regulates P-body dynamics in mouse sensory neurons in vitro and in vivo.
Authors: Paige Et al.
Neurobiol Pain 2019;5
Peroxisome Proliferator-Activated Receptor α Agonist and Its Target Nanog Cooperate to Induce Pluripotency.
Authors: Lee Et al.
J Clin Med 2018;7
Phosphorylation of Cytochrome c Threonine 28 Regulates Electron Transport Chain Activity in Kidney: IMPLICATIONS FOR AMP KINASE.
Authors: Mahapatra Et al.
J Biol Chem 2017;292:64
Entosis Is Induced by Glucose Starvation.
Authors: Hamann Et al.
Cell Rep 2017;20:201
Methyl-β-cyclodextrin restores impaired autophagy flux in Niemann-Pick C1-deficient cells through activation of AMPK.
Authors: Dai Et al.
AMP-activated protein kinase activator A-769662 increases intracellular calcium and ATP release from astrocytes in an AMPK-independent manner.
Authors: Vlachaki Walker Et al.
Diabetes Obes.Metab. 2017;
mTOR controls lysosome tubulation and antigen presentation in macrophages and dendritic cells.
Authors: Saric Et al.
Arterioscler Thromb Vasc Biol 2016;27:321
Killer Cell Lectin-like Receptor G1 Inhibits NK Cell Function through Activation of Adenosine 5'-Monophosphate-Activated Protein Kinase.
Authors: M?ller-Durovic Et al.
J Immunol 2016;197:2891
Activation of AMPK-induced autophagy ameliorates Huntington disease pathology in vitro.
Authors: Walter Et al.
Intact LKB1 activity is required for survival of dormant ovarian cancer spheroids.
Authors: Peart Et al.
Enhanced Production of Adenosine Triphosphate by Pharmacological Activation of Adenosine Monophosphate-Activated Protein Kinase Ameliorates Acetaminophen-Induced Liver Injury.
Authors: Hwang Et al.
J Pharmacol Exp Ther 2015;38:843
Dynamics of elongation factor 2 kinase regulation in cortical neurons in response to synaptic activity.
Authors: Kenney Et al.
J Neurosci 2015;35:3034
Glucose and palmitate uncouple AMPK from autophagy in human aortic endothelial cells.
Authors: Weikel Et al.
Am J Physiol Cell Physiol 2015;308:C249
A novel MEK-ERK-AMPK signaling axis controls chemokine receptor CCR7-dependent survival in human mature dendritic cells.
Authors: López-Cotarelo Et al.
Mol Cell 2015;290:827
Cellular energy stress induces AMPK-mediated regulation of YAP and the Hippo pathway.
Authors: Mo Et al.
Nat Cell Biol 2015;17:500
Bidirectional regulation of P body formation mediated by eIF4F complex formation in sensory neurons.
Authors: Melemedjian Et al.
Neurosci Lett 2014;563:169
AMPK-dependent degradation of TXNIP upon energy stress leads to enhanced glucose uptake via GLUT1.
Authors: Wu Et al.
Arthritis Rheum 2013;49:1167
AMPK-dependent phosphorylation of ULK1 regulates ATG9 localization.
Authors: Mack Et al.
Lkb1 regulates organogenesis and early oncogenesis along AMPK-dependent and -independent pathways.
Authors: Lo Et al.
J Cell Biol 2012;199:1117
Chondrocyte AMP-activated protein kinase activity suppresses matrix degradation responses to proinflammatory cytokines interleukin-1β and tumor necrosis factor α.
Authors: Terkeltaub Et al.
Proc Natl Acad Sci U S A 2011;63:1928
5-Aminoimidazole-4-carboxyamide-ribonucleoside (AICAR)-stimulated hepatic expression of Cyp4a10, Cyp4a14, Cyp4a31, and other peroxisome proliferator-activated receptor α-responsive mouse genes is AICAR 5'-monophosphate-dependent and AMP-activated
Authors: Bumpus and Johnson
J Biol Chem 2011;339:886
AMP-activated protein kinase suppresses endothelial cell inflammation through phosphorylation of transcriptional coactivator p300.
Authors: Zhang Et al.
Mol Cells 2011;31:2897
Enhancing AMPK activation during ischemia protects the diabetic heart against reperfusion injury.
Authors: Paiva Et al.
Am J Physiol Heart Circ Physiol 2011;300:H2123
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