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A-769662 AMPK activator,potent and reversible

Catalog No.A3963
Size Price Stock Qty
10mM (in 1mL DMSO)
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Sample solution is provided at 25 µL, 10mM.

Product Citations

1. Wen Z, Jin K, et al. "N-myristoyltransferase deficiency impairs activation of kinase AMPK and promotes synovial tissue inflammation." Nat Immunol. 2019 Mar;20(3):313-325. PMID:30718913
2. Hubbard JA, Xiao B, et al. "Production and Crystallization of Full-Length Human AMP-Activated Protein Kinase (α1β1γ1)." Methods Mol Biol. 2018;1732:1-14. PMID:29480465
3. Oladimeji PO, Lin W, et al. "Glucose-dependent regulation of pregnane X receptor is modulated by AMP-activated protein kinase." Sci Rep. 2017 Apr 24;7:46751. PMID:28436464

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Chemical structure


Related Biological Data


Related Biological Data


Related Biological Data


Biological Activity

Description A-769662 is a small-molecule activator of AMPK with EC50 value of 116 nM.
Targets AMPK          
IC50 116 nM (EC50)          


Cell experiment [1]:

Cell lines

Primary rat hepatocytes.

Preparation method

Soluble in DMSO > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reaction Conditions

4 h.


A-769662 dose-dependently increases ACC phosphorylation, which is phosphorylated by AMPK. A-769662 inhibits fatty acid synthesis with IC50 value of 3.2 μM. Treatment of rat hepatocytes with A-769662 at concentrations up to 100 μM shows no measurable cytotoxicity.

Animal experiment [1]:

Animal models

Sprague Dawley (SD) rats.

Dosage form

30 mg/kg; gavaged.


A-769662 significantly reduces the respiratory exchange ratio (RER) throughout the first 3 h, which is followed by a small but significant increase in RER over the subsequent 3 h. A-769662 reduces malonyl CoA levels in rat livers by 33%.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.


[1]. Cool B, Zinker B, Chiou W, et al. Identification and characterization of a small molecule AMPK activator that treats key components of type 2 diabetes and the metabolic syndrome. Cell Metab, 2006, 3(6): 403-416.

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Chemical Properties

Cas No. 844499-71-4 SDF Download SDF
Synonyms A-769662;A769662
Chemical Name 4-hydroxy-3-[4-(2-hydroxyphenyl)phenyl]-6-oxo-7H-thieno[2,3-b]pyridine-5-carbonitrile
Canonical SMILES C1=CC=C(C(=C1)C2=CC=C(C=C2)C3=CSC4=C3C(=C(C(=O)N4)C#N)O)O
Formula C20H12N2O3S M.Wt 360.39
Solubility ≥18.0195 mg/mL in DMSO, <2.35 mg/mL in EtOH, <2.39 mg/mL in H2O Storage Store at -20°C
Physical Appearance A solid Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.


A-769662 is a potent activator of AMPK with EC50 value of 0.8 μM in vitro[1].

AMPK(AMP-activated protein kinase) is a serine/threonine protein kinase which is formed by three proteins: α,β and γ subunits. They play important roles in both the activity and stabilities of AMPK. AMPK functions as sensors of cellular energy by detecting and reacting to the change of AMP: ATP ratio. AMPK plays an important role in regulating intracellular energy metabolism. AMPK inhibits ATP-consuming pathways containing cholesterol synthesis, fatty acid synthesisand gluconeogenesis. AMPK stimulates fatty acid oxidation and glycolysis which are ATP-generating processes. AMPK inhibits gluconeogenesis by suppressing the expression of glucose-6-phosphatase and PEPCK wich are two key gluconeogenic enzymes.[1]

A-769662 belongs to the thienopyridone family. It activates the activity of purified AMPK from diffrent tissues with a dose-dependent manner. A-769662 activated the activity of AMPK extracted from human embryonic kidney cells (HEKs), rat muscle, or rat heart with EC50 values of 1.1 mM, 1.9 mM, or 2.2mM, respectively. A-769662 inhibited the synthesis of fatty acid with IC50 value of 3.2mM in primary rat hepatocytes.[1] A769662 also has inhibition effect on the 26S proteasome with an AMPK-independent mechanism. A769662 does not inhibit the proteolytic activities of the 20S core subunit which is a novel mechanism. A769662 can cause the arrest of cell cycle by inhibiting the 26S proteasome[2]. A-769662 activates AMPK in an allosterically manner. It also inhibits Thr-172 dephosphorylation of AMPK.[3]

In mice treated with dose of 30mg/kg, A-769662 decreased the expression of FAS, G6Pase, and PEPCK in liver of. It also lowered plasma glucose by 40% and reduced body weight gain.[1]

[1].  Cool B, Zinker B, Chiou W, Kifle L, Cao N, Perham M, Dickinson R, Adler A, Gagne G, Iyengar R et al: Identification and characterization of a small molecule AMPK activator that treats key components of type 2 diabetes and the metabolic syndrome. Cell Metab 2006, 3(6):403-416.
[2].  Moreno D, Knecht E, Viollet B, Sanz P: A769662, a novel activator of AMP-activated protein kinase, inhibits non-proteolytic components of the 26S proteasome by an AMPK-independent mechanism. FEBS Lett 2008, 582(17):2650-2654.
[3].  Sanders MJ, Ali ZS, Hegarty BD, Heath R, Snowden MA, Carling D: 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 2007, 282(45):32539-32548.