A 769662

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Cat.No. 3336 - A 769662 | C20H12N2O3S | CAS No. 844499-71-4
Description: Potent AMPK activator
Chemical Name: 6,7-Dihydro-4-hydroxy-3-(2'-hydroxy[1,1'-biphenyl]-4-yl)-6-oxo-thieno[2,3-b]pyridine-5-carbonitrile
Purity: ≥98% (HPLC)
Datasheet
Citations (20)
Reviews
Literature
Pathways

Biological Activity

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.

Compound Libraries

A 769662 is also offered as part of the Tocriscreen Stem Cell Toolbox. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 360.39
Formula C20H12N2O3S
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 844499-71-4
PubChem ID 54708532
InChI Key CTESJDQKVOEUOY-UHFFFAOYSA-N
Smiles OC(C1=C(N3)SC=C1C2=CC=C(C4=CC=CC=C4O)C=C2)=C(C#N)C3=O

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

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 36.04 100
ethanol 3.6 10

Preparing Stock Solutions

The following data is based on the product molecular weight 360.39. Batch specific molecular weights may vary from batch to batch due to solvent 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

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Product Datasheets

Certificate of Analysis / Product Datasheet
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References

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) Metformin 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


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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

20 Citations for A 769662

Citations are publications that use Tocris products. Selected citations for A 769662 include:

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

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

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

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

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

Mo et al (2015) Cellular energy stress induces AMPK-mediated regulation of YAP and the Hippo pathway. Nat Cell Biol 17 500 PMID: 25751140

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

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

Zhang et al (2011) AMP-activated protein kinase suppresses endothelial cell inflammation through phosphorylation of transcriptional coactivator p300. Mol Cells 31 2897 PMID: 21940946

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

Walter et al (2016) Activation of AMPK-induced autophagy ameliorates Huntington disease pathology in vitro. Neuropharmacology 108 24 PMID: 27133377

Saric et al (2016) mTOR controls lysosome tubulation and antigen presentation in macrophages and dendritic cells. Arterioscler Thromb Vasc Biol 27 321 PMID: 26582390

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

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

Melemedjian et al (2014) Bidirectional regulation of P body formation mediated by eIF4F complex formation in sensory neurons. Neurosci Lett 563 169 PMID: 24080374

Mack et al (2012) AMPK-dependent phosphorylation of ULK1 regulates ATG9 localization. Autophagy 8 1197 PMID: 22932492

Lo et al (2012) Lkb1 regulates organogenesis and early oncogenesis along AMPK-dependent and -independent pathways. J Cell Biol 199 1117 PMID: 23266956


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Literature in this Area

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Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases

Pathways for A 769662

AMPK

AMPK Signaling Pathway

AMPK signaling pathway plays an important role in the cellular reponse to low levels of available ATP, often caused by stresses such as heat shock, ischemia or hypoxia.