AMPK

AMPK activators and inhibitors act on adenosine monophosphate-activated protein kinase (AMPK), an energy sensor. The enzyme is a heterotrimer of a catalytic α subunit with regulatory β and γ subunits. When cellular energy falls, AMPK switches off anabolic pathways such as fatty acid synthesis and switches on catabolic processes. A 2001 study linked AMPK activation to the actions of metformin and introduced compound C, also known as dorsomorphin, as an inhibitor. A-769662, reported in 2006, was among the first direct small-molecule AMPK activators. MK8722 and ex229 also activate the kinase directly, whereas acadesine acts through a cellular metabolite that mimics adenosine monophosphate.

Items 1-25 of 71

  • A-769662
    Cat. No.
    A11071

    A-769662

    A-769662 is a new activator of AMP-activated protein kinase (AMPK).

    2 mg
    $25.00
    5 mg
    $35.00
    All 8 sizes
  • Metformin
    Cat. No.
    A11622

    Metformin

    Synonyms: 1,1-Dimethylbiguanide

    Metformin is an AMP-activated protein kinase (AMPK) activator that improves glycemic control by improving insulin sensitivity and decreasing intestinal absorption of glucose.

    5 mg
    $25.00
    10 mg
    $30.00
    All 7 sizes
  • ex229
    Cat. No.
    A16795

    ex229 (compound 991)

    Synonyms: compound 991

    EX229 (compound 991) is a potent AMPK activator that is 5-10-fold more potent than A769662 in activating AMPK.

    1 mg
    $25.00
    2 mg
    $35.00
    All 8 sizes
  • Danthron
    Cat. No.
    A15571

    Danthron

    Synonyms: Dantron; Chrysazin; 1,8-Dihydroxyanthraquinone

    Danthron is an AMPK activator that plays a critical role in regulating glucose and lipid metabolism. Derived from the traditional Chinese medicinal plant Salvia miltiorrhiza Bunge, Danthron has demonstrated potential in enhancing cellular energy balance. Its biological activity makes it a valuable reagent for research in metabolic disorders and related therapeutic applications.

    100 mg
    $25.00
    1 g
    $30.00
    All 3 sizes
  • PF-06409577
    Cat. No.
    A16801

    PF-06409577

    PF-06409577 is orally bioavailable AMPK activator with EC50 of 7 nM for α1β1γ1 in the TR-FRET assay and it shows no detectable inhibition of hERG in a patch-clamp assay (100 μM) and was not an inhibitor (IC50 > 100 μM) of the microsomal activities of major human cytochrome P450 isoforms.

    2 mg
    $30.00
    5 mg
    $55.00
    All 8 sizes
  • MK-3903
    Cat. No.
    A17063

    MK-3903

    MK-3903 is a potent and selective AMPK activator (EC50 = 8 nM). MK-3903 exhibited robust target engagement in mouse liver following oral dosing, leading to improved lipid metabolism and insulin sensitization in mice.

    1 mg
    $25.00
    5 mg
    $65.00
    All 8 sizes
  • 7-Methoxyisoflavone
    Cat. No.
    A17097

    7-Methoxyisoflavone

    7-Methoxyisoflavone is an isoflavone derivative and also an activator of adenosine monophosphate-activated protein kinase (AMPK).

    50 mg
    $20.00
    100 mg
    $35.00
    All 4 sizes
  • O-304
    Cat. No.
    A19807

    O-304

    O-304 is a first-in-class, orally available pan-AMPK activator, which increases AMPK activity by suppressing the dephosphorylation of pAMPK.

    1 mg
    $55.00
    2 mg
    $80.00
    All 9 sizes
  • IM156
    Cat. No.
    A22320

    IM156

    IM156 (HL156A), a metformin derivative, is a potent activator of AMPK that increases AMPK phosphorylation.

    1 mg
    $25.00
    5 mg
    $70.00
    All 7 sizes
  • ASP4132
    Cat. No.
    A22339

    ASP4132

    ASP4132 is an orally active, potent AMPK activator with an EC50 of 18 nM. ASP4132 has anti-cancer activity and makes tumor regression in breast cancer xenograft mouse models.

    1 mg
    $55.00
    2 mg
    $80.00
    All 8 sizes
  • PF-06679142
    Cat. No.
    A22484

    PF-06679142

    Synonyms: PF-6679142

    PF-06679142 is a potent AMPK activator. PF-06679142 exhibited robust activation of AMPK in rat kidneys as well as desirable oral absorption, low plasma clearance, and negligible renal clearance in preclinical species.

    5 mg
    $100.00
    10 mg
    $180.00
    All 5 sizes
  • Candidusin A
    Cat. No.
    A26035

    Candidusin A

    Synonyms: CHNQD-0803

    Candidusin A is a potent AMPK activator with a KD of 47.28 nM, isolated from the marine fungus Aspergillus candidus. This compound demonstrates significant cytotoxicity, inducing apoptosis in human prostate cancer cell lines such as 22Rv1, PC-3, and LNCaP. Additionally, Candidusin A reduces the expression of adipogenesis-related genes and fat deposition, while negatively regulating the NF-κB-TNFα inflammatory axis to mitigate inflammation. Its diverse biological activities make Candidusin A a valuable tool for research into non-alcoholic steatohepatitis (NASH) and liver injury.

    Out of stock

    All 3 sizes
  • MT 63-78
    Cat. No.
    A30698

    MT 63-78

    MT 63-78 is a specific and potent direct activator of AMP-activated protein kinase (AMPK), exhibiting an EC50 value of 25 μM. This compound not only induces cell mitotic arrest and apoptosis but also effectively inhibits prostate cancer growth through the suppression of lipogenesis and the mTORC1 signaling pathway. MT 63-78 demonstrates significant antitumor effects, making it a valuable reagent for cancer research applications focused on metabolic regulation and cell cycle modulation.

    1 mg
    $65.00
    5 mg
    $140.00
    All 6 sizes
  • GL-V9
    Cat. No.
    A32395

    GL-V9

    GL-V9 is an AMPK activator that modulates cellular metabolism and promotes apoptosis in HepG2 cells, with an IC50 of 35.2 μM. It induces cell cycle arrest at the G2/M phase and alters mitochondrial membrane potential, leading to increased intracellular reactive oxygen species. By inhibiting the pentose phosphate pathway and enhancing fatty acid oxidation via AMPK activation, GL-V9 significantly impedes cancer cell metastasis and demonstrates antitumor efficacy in mouse models, making it a valuable tool for cancer research.

    1 mg
    $160.00
    5 mg
    $395.00
    All 6 sizes
  • Thalidezine
    Cat. No.
    A32724

    Thalidezine

    Thalidezine is a selective activator of AMP-activated protein kinase (AMPK), a crucial regulator of cellular energy homeostasis. It has been shown to promote autophagic cell death in anti-apoptotic cancer cells by modulating energy metabolism. Thalidezine serves as a valuable tool for investigating the mechanisms of apoptosis and potential therapeutic interventions in cancer research.

    1 mg
    $460.00
    5 mg
    $945.00
    All 2 sizes
  • NFAT-133
    Cat. No.
    A36087

    NFAT-133

    NFAT-133 is an aromatic polyketide that functions as an AMPK activator. It enhances glucose uptake in muscle cells, showing potential as an antidiabetic agent. Additionally, NFAT-133 suppresses T-cell proliferation and IL-2 expression by inhibiting the transcriptional activity of nuclear factor of activated T-cells (NFAT), exhibiting immunosuppressive properties. This compound also reduces nitric oxide production in RAW264.7 cells stimulated by lipopolysaccharide (LPS), without displaying antibacterial or cytotoxic effects.

    Out of stock

    All 3 sizes
  • RSVA405
    Cat. No.
    A36503

    RSVA405

    RSVA405 is a potent, orally bioavailable activator of AMP-activated protein kinase (AMPK), exhibiting an EC50 of 1 μM. This compound enhances CaMKKβ-mediated activation of AMPK, leading to the inhibition of mTOR and promotion of autophagy, which in turn increases the degradation of amyloid beta (Aβ). Additionally, RSVA405 demonstrates anti-inflammatory properties by inhibiting STAT3 activity, and is applicable in obesity research.

    5 mg
    $35.00
    10 mg
    $60.00
    All 6 sizes
  • HSF1/AMPK activator 1
    Cat. No.
    A37027

    HSF1/AMPK activator 1

    HSF1/AMPK activator 1 is a potent modulator of the HSF1/AMPK axis, targeting the TGF-β1/Smad signaling pathway. This compound demonstrates significant anti-hepatic fibrosis activity by inhibiting fibrosis formation and cell proliferation in activated hepatic stellate cells. Additionally, HSF1/AMPK activator 1 effectively alleviates liver injury and symptoms of hepatic fibrosis in fibrotic mouse models. It is a valuable tool for research focused on hepatic fibrosis and related metabolic disorders.

    Out of stock

    All 3 sizes
  • Isovaleric acid
    Cat. No.
    A37153

    Isovaleric acid

    Isovaleric acid is an AMPK activator known for its role in inhibiting osteoclast differentiation through the stimulation of AMPK phosphorylation. Additionally, it promotes colonic smooth muscle relaxation via the activation of the cAMP/PKA pathway. This compound is applicable in research focusing on skeletal diseases, including osteoporosis, as well as intestinal disorders.

    50 mg
    $20.00
    100 mg
    $25.00
    All 7 sizes
  • Malvidin-3-O-arabinoside chloride
    Cat. No.
    A39463

    Malvidin-3-O-arabinoside chloride

    Malvidin-3-O-arabinoside chloride is an AMPK inducer that enhances cellular autophagy. This compound is recognized for its ability to mitigate oxidative damage induced by ethyl carbamate through the activation of AMPK signaling pathways. Its biological activity supports research applications focused on metabolic disorders and oxidative stress-related conditions.

    1 mg
    $230.00
    5 mg
    $585.00
    All 2 sizes
  • OSU-53
    Cat. No.
    A39621

    OSU-53

    OSU-53 is an orally active AMPK activator and a direct mTOR inhibitor, exhibiting an EC50 of 0.3 μM. This compound induces autophagy by facilitating the conversion of LC3 I to LC3 II and plays a crucial role in modulating energy homeostasis by downregulating fatty acid biosynthesis while enhancing oxidative metabolism through upregulation of PGC1α and NRF-1. OSU-53 demonstrates antitumor activity across various cancer models, including breast and thyroid cancers, making it a valuable tool for cancer research and metabolic studies.

    25 mg
    $1,405.00
    50 mg
    $1,790.00
    All 3 sizes

Items 1-25 of 71

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