Date published: 2026-4-24

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AMPKα1 Activators

AMP-activated protein kinase alpha 1 (AMPKα1) serves as a pivotal regulator of cellular energy homeostasis, orchestrating responses to nutrient availability and metabolic demands. The identified activators of AMPKα1, outlined in the table, act through various mechanisms to enhance its activity. A-769662, for instance, allosterically binds to the β1 subunit, promoting phosphorylation and activation. Metformin, a widely used antidiabetic drug, indirectly activates AMPKα1 by inhibiting mitochondrial complex I, leading to increased cellular AMP levels. AICAR, a direct activator, mimics AMP's effects by promoting AMPKα1 phosphorylation.

Resveratrol and berberine, natural compounds found in red grapes and various plants, respectively, activate AMPKα1 by increasing cellular AMP levels. Dorsomorphin, an inhibitor of BMP type I receptors, indirectly activates AMPKα1, influencing cellular processes like autophagy. GW-6471 indirectly activates AMPKα1 by inhibiting PPARα, shedding light on the crosstalk between signaling pathways. Oligomycin A, by inhibiting mitochondrial ATP synthase, increases cellular AMP levels and triggers AMPKα1 phosphorylation. Phenformin, akin to metformin, activates AMPKα1 by inhibiting mitochondrial complex I. PT-1 and ZLN024, direct activators, bind to AMPKα1's α subunit, promoting phosphorylation and activation. These activators collectively provide a nuanced understanding of AMPKα1 regulation, offering valuable insights into cellular responses governing energy balance and metabolic processes. Researchers can leverage these tools to decipher the intricate roles of AMPKα1 in health and disease, shaping future investigations in cellular and molecular physiology.

SEE ALSO...

Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

A-769662

844499-71-4sc-203790
sc-203790A
sc-203790B
sc-203790C
sc-203790D
10 mg
50 mg
100 mg
500 mg
1 g
$184.00
$741.00
$1076.00
$3417.00
$5304.00
23
(2)

A-769662 activates AMPKα1 by allosterically binding to its β1 subunit, promoting phosphorylation and subsequent activation. It enhances AMPKα1's role in energy homeostasis, suppressing hepatic glucose output and promoting fatty acid oxidation through the AMPK signaling pathway.

1,1-Dimethylbiguanide, Hydrochloride

1115-70-4sc-202000F
sc-202000A
sc-202000B
sc-202000C
sc-202000D
sc-202000E
sc-202000
10 mg
5 g
10 g
50 g
100 g
250 g
1 g
$20.00
$43.00
$63.00
$156.00
$260.00
$510.00
$31.00
37
(1)

Metformin, a widely used antidiabetic drug, activates AMPKα1 indirectly by inhibiting mitochondrial complex I. This leads to an increase in cellular AMP levels, triggering AMPKα1 phosphorylation. Metformin's activation of AMPKα1 helps regulate glucose metabolism and improve insulin sensitivity.

AICAR

2627-69-2sc-200659
sc-200659A
sc-200659B
50 mg
250 mg
1 g
$65.00
$280.00
$400.00
48
(2)

AICAR is a direct activator of AMPKα1 that mimics the effects of AMP. It is phosphorylated to ZMP, which activates AMPKα1 by binding to its γ subunit. This activation promotes glucose uptake and fatty acid oxidation, making AICAR a valuable tool in studying AMPKα1-related cellular processes.

Resveratrol

501-36-0sc-200808
sc-200808A
sc-200808B
100 mg
500 mg
5 g
$80.00
$220.00
$460.00
64
(2)

Resveratrol activates AMPKα1 by increasing cellular AMP levels and promoting AMPKα1 phosphorylation. This polyphenol, found in red grapes and berries, contributes to AMPKα1-mediated improvements in metabolic parameters, including glucose homeostasis and insulin sensitivity.

Berberine

2086-83-1sc-507337
250 mg
$92.00
1
(0)

Berberine activates AMPKα1 by increasing cellular AMP levels and promoting AMPKα1 phosphorylation. This natural compound, found in various plants, contributes to AMPKα1-mediated improvements in glucose metabolism, making it a potential therapeutic agent for metabolic disorders.

GW6471

880635-03-0sc-300779
5 mg
$295.00
9
(1)

GW-6471 activates AMPKα1 indirectly by inhibiting PPARα, leading to increased cellular AMP levels and AMPKα1 phosphorylation. This activation contributes to the regulation of lipid metabolism and provides insights into the crosstalk between AMPKα1 and PPARα signaling pathways.

Phenformin Hydrochloride

834-28-6sc-219590
10 g
$119.00
4
(1)

Phenformin, a biguanide similar to metformin, activates AMPKα1 by inhibiting mitochondrial complex I. This leads to increased cellular AMP levels, triggering AMPKα1 phosphorylation. Phenformin's activation of AMPKα1 contributes to its potential therapeutic effects on metabolic disorders.

Oligomycin

1404-19-9sc-203342
sc-203342C
10 mg
1 g
$149.00
$12495.00
18
(2)

Oligomycin A indirectly activates AMPKα1 by inhibiting mitochondrial ATP synthase. This inhibition leads to an increase in cellular AMP levels, triggering AMPKα1 phosphorylation. Oligomycin A provides insights into the regulation of AMPKα1 by mitochondrial ATP production.

PT 1

331002-70-1sc-361299
sc-361299A
10 mg
50 mg
$185.00
$781.00
1
(2)

PT-1 activates AMPKα1 by directly binding to its α subunit and promoting phosphorylation. This activation enhances AMPKα1-mediated cellular responses related to energy homeostasis, making PT-1 a valuable tool in studying the specific activation of AMPKα1 and its downstream effects.