Cat. No. 3336
Chemical Name: 6,7-Dihydro-4-hydroxy-3-(2'-hydroxy[
Biological ActivityPotent, 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.
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All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Data Sheet
Duca et al (2015) Metformin activates a duodenal Ampk-dependent pathway to lower hepatic glucose production in rats. Nat.Med. 21 506. PMID: 25849133 .
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.
Scott et al (2008) Thienopyridone drugs are selective activators of AMP-activated protein kinase β1-containing complexes. Chem.Biol. 15 1220. PMID: 19022182.
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.
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.
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Citations are publications that use Tocris products. Selected citations for A 769662 include:
Saric et al (2016) mTOR controls lysosome tubulation and antigen presentation in macrophages and dendritic cells. Arterioscler Thromb Vasc Biol 27 321. PMID: 26582390.
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.
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.
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.
Mo et al (2015) Cellular energy stress induces AMPK-mediated regulation of YAP and the Hippo pathway. Nat Cell Biol 17 500. PMID: 25751140.
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.
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.
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.
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 protein kinase-independent. J Biol Chem 339 886. PMID: 21896918.
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.
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Keywords: A 769662, supplier, Potent, AMPK, activators, AMP-Activated, Protein, Kinases, A769662, Tocris Bioscience, AMPK Activator products
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