Determine the necessary mass, volume, or concentration for preparing a solution.
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SKU | Size | Availability | Price | Qty |
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A127825-5mg | 5mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $64.90 | |
A127825-10mg | 10mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $90.90 | |
A127825-50mg | 50mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $325.90 |
AMP-activated protein kinase activator
Synonyms | 844499-71-4 | A-769662 | 4-Hydroxy-3-(2'-hydroxy-[1,1'-biphenyl]-4-yl)-6-oxo-6,7-dihydrothieno[2,3-b]pyridine-5-carbonitrile | A 769662 | A769662 | 6,7-DIHYDRO-4-HYDROXY-3-(2'-HYDROXY[1,1'-BIPHENYL]-4-YL)-6-OXO-THIENO[2,3-B]PYRIDINE-5-CARBONITRILE | 4-hydroxy-3-[4-(2 |
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Specifications & Purity | Moligand™, ≥98% |
Biochemical and Physiological Mechanisms | A-769662 is a potent, reversible AMP-activated protein kinase (AMPK) activator (EC50 = 0.8 μM) that displays selectivity towards β1 subunit-containing heterotrimers. A-769662 inhibits fatty acid synthesis (IC50 = 3.2 μM) and decreases plasma gl |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Note | Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details. |
Product Description | A-769662 is a potent, reversible AMPK activator with EC50 of 0.8 μM, little effect on GPPase/FBPase activity. |
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IUPAC Name | 4-hydroxy-3-[4-(2-hydroxyphenyl)phenyl]-6-oxo-7H-thieno[2,3-b]pyridine-5-carbonitrile |
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INCHI | InChI=1S/C20H12N2O3S/c21-9-14-18(24)17-15(10-26-20(17)22-19(14)25)12-7-5-11(6-8-12)13-3-1-2-4-16(13)23/h1-8,10,23H,(H2,22,24,25) |
InChi Key | CTESJDQKVOEUOY-UHFFFAOYSA-N |
Canonical SMILES | C1=CC=C(C(=C1)C2=CC=C(C=C2)C3=CSC4=C3C(=C(C(=O)N4)C#N)O)O |
Isomeric SMILES | C1=CC=C(C(=C1)C2=CC=C(C=C2)C3=CSC4=C3C(=C(C(=O)N4)C#N)O)O |
PubChem CID | 54708532 |
Molecular Weight | 360.39 |
PubChem CID | 54708532 |
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CAS Registry No. | 844499-71-4 |
ChEMBL Ligand | CHEMBL512504 |
RCSB PDB Ligand | C1V |
BindingDB Ligand | 50242401 |
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Solubility | DMSO ≥70mg/mL Water <1.2mg/mL Ethanol <1.2mg/mL |
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Refractive Index | 1.78 |
Boil Point(°C) | 630.08° C at 760 mmHg |
Melt Point(°C) | 268.39°C |
1. Cool B, Zinker B, Chiou W, Kifle L, Cao N, Perham M, Dickinson R, Adler A, Gagne G, Iyengar R 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 Metab, 3 (6): (403-16). [PMID:16753576] |
2. Sanders MJ, Ali ZS, Hegarty BD, Heath R, Snowden MA, Carling D. (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 (45): (32539-48). [PMID:17728241] |
3. Göransson O, McBride A, Hawley SA, Ross FA, Shpiro N, Foretz M, Viollet B, Hardie DG, Sakamoto K. (2007) Mechanism of action of A-769662, a valuable tool for activation of AMP-activated protein kinase.. J Biol Chem, 282 (45): (32549-60). [PMID:17855357] |
4. Walter C, Clemens LE, Müller AJ, Fallier-Becker P, Proikas-Cezanne T, Riess O, Metzger S, Nguyen HP. (2016) Activation of AMPK-induced autophagy ameliorates Huntington disease pathology in vitro.. Neuropharmacology, 108 (3): (24-38). [PMID:27133377] |
5. Webb TJ et al.. (2016) Alterations in cellular metabolism modulate CD1d-mediated NKT-cell responses.. Pathog Dis, 74 (6): [PMID:27297969] |
6. Choudhury Y et al.. (2014) AMP-activated protein kinase (AMPK) as a potential therapeutic target independent of PI3K/Akt signaling in prostate cancer.. Oncoscience, 1 (6): (446-56). [PMID:25594043] |
7. Qin Y et al.. (2019) AMPK activation induced in pemetrexed-treated cells is associated with development of drug resistance independently of target enzyme expression.. Mol Oncol, 13 (6): (1419-1432). [PMID:31033201] |
8. Shrikanth CB et al.. (2021) AMPK differentially alters sulphated glycosaminoglycans under normal and high glucose milieu in proximal tubular cells.. J Biochem, 169 (75-86). [PMID:32785657] |
9. Watterson KR et al.. (2013) Anorexigenic and orexigenic hormone modulation of mammalian target of rapamycin complex 1 activity and the regulation of hypothalamic agouti-related protein mRNA expression.. Neurosignals, 21 (1-2): (28-41). [PMID:22456226] |
10. Head SA et al.. (2015) Antifungal drug itraconazole targets VDAC1 to modulate the AMPK/mTOR signaling axis in endothelial cells.. Proc Natl Acad Sci U S A, 112 (52): (E7276-85). [PMID:26655341] |
11. Henry WS et al.. (2017) Aspirin Suppresses Growth in PI3K-Mutant Breast Cancer by Activating AMPK and Inhibiting mTORC1 Signaling.. Cancer Res, 77 (3): (790-801). [PMID:27940576] |
12. Mancini SJ et al.. (2018) Canagliflozin inhibits interleukin-1ß-stimulated cytokine and chemokine secretion in vascular endothelial cells by AMP-activated protein kinase-dependent and -independent mechanisms.. Sci Rep, 8 (5276). [PMID:29588466] |
13. Bizjak M et al.. (2017) Combined treatment with Metformin and 2-deoxy glucose induces detachment of viable MDA-MB-231 breast cancer cells in vitro.. Sci Rep, 7 (1761). [PMID:28496098] |
14. Schiavon CR et al.. (2018) Compositional complexity of rods and rings.. Mol Biol Cell, 29 (19): (2303-2316). [PMID:30024290] |
15. Vincent EE et al.. (2014) Differential effects of AMPK agonists on cell growth and metabolism.. Oncogene, [PMID:25241895] |
16. Zibrova D et al.. (2017) GFAT1 phosphorylation by AMPK promotes VEGF-induced angiogenesis.. Biochem J, 474 (6): (983-1001). [PMID:28008135] |
17. Galic S et al.. (2011) Hematopoietic AMPK ß1 reduces mouse adipose tissue macrophage inflammation and insulin resistance in obesity.. J Clin Invest, 121 (12): (4903-15). [PMID:22080866] |
18. Gao Y et al.. (2020) LKB1 Represses ATOH1 via PDK4 and Energy Metabolism and Regulates Intestinal Stem Cell Fate.. Gastroenterology, 158 (5): (1389-1401.e10). [PMID:31930988] |
19. Ren Y et al.. (2021) Oxidative stress-mediated AMPK inactivation determines the high susceptibility of LKB1-mutant NSCLC cells to glucose starvation.. Free Radic Biol Med, 166 (128-139). [PMID:33636336] |
20. Chen Z et al.. (2012) Promotion of adiponectin multimerization by emodin, a novel AMPK activator with PPAR?-agonist activity.. J Cell Biochem, [PMID:22730200] |
21. Langendorf CG et al.. (2016) Structural basis of allosteric and synergistic activation of AMPK by furan-2-phosphonic derivative C2 binding.. Nat Commun, 7 (10912). [PMID:26952388] |
22. Ngoei KRW et al.. (2018) Structural Determinants for Small-Molecule Activation of Skeletal Muscle AMPK a2ß2?1 by the Glucose Importagog SC4.. Cell Chem Biol, 25 (6): (728-737.e9). [PMID:29657085] |
23. Yan Y et al.. (2015) SUMOylation of AMPKa1 by PIAS4 specifically regulates mTORC1 signalling.. Nat Commun, 6 (8979). [PMID:26616021] |
24. Dite TA et al.. (2017) The autophagy initiator ULK1 sensitizes AMPK to allosteric drugs.. Nat Commun, 8 (571). [PMID:28924239] |