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Biological Activity for A 769662
A 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.
Technical Data for A 769662
|Storage||Store at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for A 769662
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for A 769662
The following data is based on the product molecular weight 360.39. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.77 mL||13.87 mL||27.75 mL|
|5 mM||0.55 mL||2.77 mL||5.55 mL|
|10 mM||0.28 mL||1.39 mL||2.77 mL|
|50 mM||0.06 mL||0.28 mL||0.55 mL|
References for A 769662
References are publications that support the biological activity of the product.
Sanders et al (2007) 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. 282 32539 PMID: 17728241
Scott et al (2008) Thienopyridone drugs are selective activators of AMP-activated protein kinase β1-containing complexes. Chem.Biol. 15 1220 PMID: 19022182
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 Met. 3 403
de Meester et al (2014) Role of AMP-activated protein kinase in regulating hypoxic survival and proliferation of mesenchymal stem cells. Cardiovasc.Res. 101 20 PMID: 24104879
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
Duca et al (2015) MetF. activates a duodenal Ampk-dependent pathway to lower hepatic glucose production in rats. Nat.Med. 21 506 PMID: 25849133
Galluzzi et al (2017) Pharmacological modulation of autophagy: therapeutic potential and persisting obstacles. Nat.Rev.Drug.Discov. PMID: 28529316
If you know of a relevant reference for A 769662, please let us know.
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Keywords: A 769662, A 769662 supplier, Potent, AMPK, activators, AMP-Activated, Protein, Kinases, A769662, Enzyme, Substrates, /, Activators, Stem, Cell, Proliferation, Autophagy, 3336, Tocris Bioscience
24 Citations for A 769662
Citations are publications that use Tocris products. Selected citations for A 769662 include:
Ahwazi et al (2021) Investigation of the specificity and mechanism of action of the ULK1/AMPK inhibitor SBI-0206965. Biochem J 478 2977 PMID: 34259310
Wu et al (2013) AMPK-dependent degradation of TXNIP upon energy stress leads to enhanced glucose uptake via GLUT1. Arthritis Rheum 49 1167 PMID: 23453806
Paige et al (2019) AMPK activation regulates P-body dynamics in mouse sensory neurons in vitro and in vivo. Neurobiol Pain 5 PMID: 31080914
Hamann et al (2017) Entosis Is Induced by Glucose Starvation. Cell Rep 20 201 PMID: 28683313
Lo et al (2012) Lkb1 regulates organogenesis and early oncogenesis along AMPK-dependent and -independent pathways. J Cell Biol 199 1117 PMID: 23266956
Mack et al (2012) AMPK-dependent phosphorylation of ULK1 regulates ATG9 localization. Autophagy 8 1197 PMID: 22932492
Walter et al (2016) Activation of AMPK-induced autophagy ameliorates Huntington disease pathology in vitro. Neuropharmacology 108 24 PMID: 27133377
Hwang et al (2015) Enhanced Production of Adenosine Triphosphate by Pharmacological Activation of Adenosine Monophosphate-Activated Protein Kinase Ameliorates Acetaminophen-Induced Liver Injury. J Pharmacol Exp Ther 38 843 PMID: 26434492
López-Cotarelo et al (2015) A novel MEK-ERK-AMPK signaling axis controls chemokine receptor CCR7-dependent survival in human mature dendritic cells. Mol Cell 290 827 PMID: 25425646
Paiva et al (2011) Enhancing AMPK activation during ischemia protects the diabetic heart against reperfusion injury. Am J Physiol Heart Circ Physiol 300 H2123 PMID: 21421816
Lee et al (2018) Peroxisome Proliferator-Activated Receptor α Agonist and Its Target Nanog Cooperate to Induce Pluripotency. J Clin Med 7 PMID: 30486372
Dai et al (2017) Methyl-β-cyclodextrin restores impaired autophagy flux in Niemann-Pick C1-deficient cells through activation of AMPK. Autophagy 13 1435 PMID: 28613987
Saric et al (2016) mTOR controls lysosome tubulation and antigen presentation in macrophages and dendritic cells. Arterioscler Thromb Vasc Biol 27 321 PMID: 26582390
Vlachaki Walker et al (2017) AMP-activated protein kinase activator A-769662 increases intracellular calcium and ATP release from astrocytes in an AMPK-independent manner. Diabetes Obes.Metab. PMID: 28211632
Mo et al (2015) Cellular energy stress induces AMPK-mediated regulation of YAP and the Hippo pathway. Nat Cell Biol 17 500 PMID: 25751140
Kenney et al (2015) Dynamics of elongation factor 2 kinase regulation in cortical neurons in response to synaptic activity. J Neurosci 35 3034 PMID: 25698741
Peart et al (2015) Intact LKB1 activity is required for survival of dormant ovarian cancer spheroids. Oncotarget 6 22424 PMID: 26068970
Weikel et al (2015) Glucose and palmitate uncouple AMPK from autophagy in human aortic endothelial cells. Am J Physiol Cell Physiol 308 C249 PMID: 25354528
Melemedjian et al (2014) Bidirectional regulation of P body formation mediated by eIF4F complex formation in sensory neurons. Neurosci Lett 563 169 PMID: 24080374
Mahapatra et al (2017) Phosphorylation of Cytochrome c Threonine 28 Regulates Electron Transport Chain Activity in Kidney: IMPLICATIONS FOR AMP KINASE. J Biol Chem 292 64 PMID: 27758862
Terkeltaub et al (2011) Chondrocyte AMP-activated protein kinase activity suppresses matrix degradation responses to proinflammatory cytokines interleukin-1β and tumor necrosis factor α. Proc Natl Acad Sci U S A 63 1928 PMID: 21400477
Zhang et al (2011) AMP-activated protein kinase suppresses endothelial cell inflammation through phosphorylation of transcriptional coactivator p300. Mol Cells 31 2897 PMID: 21940946
Müller-Durovic et al (2016) Killer Cell Lectin-like Receptor G1 Inhibits NK Cell Function through Activation of Adenosine 5'-Monophosphate-Activated Protein Kinase. J Immunol 197 2891 PMID: 27566818
Bumpus and Johnson (2011) 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 J Biol Chem 339 886 PMID: 21896918
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Literature in this Area
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