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Submit ReviewA 769662
说明： Potent AMPK activator
化学名： 6,7-Dihydro-4-hydroxy-3-(2'-hydroxy[1,1'-biphenyl]-4-yl)-6-oxo-thieno[2,3-b]pyridine-5-carbonitrile
纯度： ≥98% (HPLC)
生物活性 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.
技术数据 for A 769662
| 分子量 | 360.39 |
| 公式 | C20H12N2O3S |
| 储存 | Store at +4°C |
| 纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for A 769662
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 36.04 | 100 |
制备储备液 for A 769662
以下数据基于产品分子量 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.
| 浓度/溶剂体积/质量 | 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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产品说明书 for A 769662
参考文献 for A 769662
参考文献是支持产品生物活性的出版物。
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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关键词: A 769662, A 769662 supplier, Potent, AMPK, activators, AMP-Activated, Protein, Kinases, A769662, Enzyme, Substrates, /, Activators, Stem, Cell, Proliferation, Autophagy, 3336, Tocris Bioscience
24 篇 A 769662 的引用文献
引用文献是使用了 Tocris 产品的出版物。 A 769662 的部分引用包括：
Paige et al (2019) AMPK activation regulates P-body dynamics in mouse sensory neurons in vitro and in vivo. Neurobiol Pain 5 PMID: 31080914
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
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
Saric et al (2016) mTOR controls lysosome tubulation and antigen presentation in macrophages and dendritic cells. Arterioscler Thromb Vasc Biol 27 321 PMID: 26582390
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
Walter et al (2016) Activation of AMPK-induced autophagy ameliorates Huntington disease pathology in vitro. Neuropharmacology 108 24 PMID: 27133377
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
Lee et al (2018) Peroxisome Proliferator-Activated Receptor α Agonist and Its Target Nanog Cooperate to Induce Pluripotency. J Clin Med 7 PMID: 30486372
Hamann et al (2017) Entosis Is Induced by Glucose Starvation. Cell Rep 20 201 PMID: 28683313
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
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
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
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
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