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PI3K&mTOR

A-769662 (844499-71-4)

A-769662 is a potent, reversible AMP-activated protein kinase (AMPK) activator with an EC50 of 0.8 μM.A-769662 displays selectivity towards β1 subunit-containing heterotrimers.

Not Intended for Therapeutic Use. For research use only.

SKU 844499-71-4 Category

A-769662 (844499-71-4) Description

A-769662 (844499-71-4) is a potent and reversible AMP-activated protein kinase (AMPK) allosteric activator.  Activates AMPK by binding to the β and γ subunits and not the AMP binding site. The activation of AMPK inhibits mTOR (mammalian target of rapamycin) signaling, which is a positive effector of cell growth, proliferation and survival. A769662 has been shown to inhibit the Na⁺K⁺-ATPase at higher concentrations. It also inhibits the differentiation of adipocytes.

 

A-769662 (844499-71-4) Specifications

Product Name A-769662
Synonyms A769662; A 769662; A-769662
Chemical Names UNII-P68477CD2C; 4-Hydroxy-3-(2′-hydroxy-[1,1′-biphenyl]-4-yl)-6-oxo-6,7-dihydrothieno[2,3-b]pyridine-5-carbonitrile; P68477CD2C; cc-24; KS-00000IAY; EX-A380; AJ-75502; 6-hydroxy-3-[4-(2-hydroxyphenyl)phenyl]-4-oxo-7H-thieno[2,3-b]pyridine-5-carbonitrile
Purity ≥98% (HPLC)
CAS Number 844499-71-4
Molecular Formula C20H12N2O3S
Molecular Weight 360.38588
Monoisotopic Mass 360.057 g/mol
MDL number MFCD11977269
InChIKey CTESJDQKVOEUOY-UHFFFAOYSA-N
InChi Code 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)
SMILES C1=CC=C(C(=C1)C2=CC=C(C=C2)C3=CSC4=C3C(=C(C(=O)N4)C#N)O)O
Form Powder
Color White
Solubility  DMSO(30 mg/ml) or Ethanol (5 mg/ml)
Storage Temp.  Store at +4°C
Shelf life >2 years if stored properly
Handling Protect from air and light
Application An AMPK activator which induces PI3-kinase-dependent glucose uptake

 


Details

RIDADR NONH for all modes of transport

References:

[1]. Kopietz F, Berggreen C, Larsson S, Säll J, Ekelund M, Sakamoto K, Degerman E, Holm C, Göransson O. AMPK activation by A-769662 and 991 does not affect catecholamine-induced lipolysis in human adipocytes. Am J Physiol Endocrinol Metab. 2018 Nov 1;315(5):E1075-E1085. doi: 10.1152/ajpendo.00110.2018. Epub 2018 Sep 25. PMID: 30253109

[2]. Huang Y, Smith CA, Chen G, Sharma B, Miner AS, Barbee RW, Ratz PH. The AMP-Dependent Protein Kinase (AMPK) Activator A-769662 Causes Arterial Relaxation by Reducing Cytosolic Free Calcium Independently of an Increase in AMPK Phosphorylation. Front Pharmacol. 2017 Oct 18;8:756. doi: 10.3389/fphar.2017.00756. eCollection 2017. PMID: 29093683

[3]. Strembitska A, Mancini SJ, Gamwell JM, Palmer TM, Baillie GS, Salt IP. A769662 Inhibits Insulin-Stimulated Akt Activation in Human Macrovascular Endothelial Cells Independent of AMP-Activated Protein Kinase. Int J Mol Sci. 2018 Dec 5;19(12). pii: E3886. doi: 10.3390/ijms19123886. PMID: 30563079

[4]. Kitzmiller L, Ledford JR, Hake PW, O’Connor M, Piraino G, Zingarelli B. Activation of AMP-Activated Protein Kinase by A769662 Ameliorates Sepsis-Induced Acute Lung Injury in Adult Mice. Shock. 2018 Dec 13. doi: 10.1097/SHK.0000000000001303. PMID: 30562237

[5]. Calle-Guisado V et al. Andrology. Human sperm motility is downregulated by the AMPK activator A769662.DOI: 10.1111/andr.12423 PMID: 28980456