Catalog No.
Product Name
Application
Product Information
Citations
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AMPK activator
Acadesine is a selective activator of AMPK in both hepatocytes and adipocytes.
- R. Lim, .et al. , Placenta, 2015, Apr;36(4):454-62 PMID: 25659498
- Stella Liong, .et al. , J Physiol Biochem, 2015, Dec;71(4):703-17 PMID: 26407807
- Phenformin hydrochloride is a hydrochloride salt of phenformin from the biguanide drug class that displays anti-diabetic activity.
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AMPK activator
A-769662 is a new activator of AMP-activated protein kinase (AMPK).- Daniel Missailidis, .et al. , Int J Mol Sci., 2021, Feb; 22(4): 2046 PMID: 33669532
- Lieberthal W, .et al. , Am J Physiol Renal Physiol, 2019, 2019 PMID: 30995114
- Kikuchi H, .et al. , Kidney Int, 2018, Nov 13. pii: S0085-2538(18)30635-5 PMID: 30455054
- Schneider H, .et al. , Hypertension, 2015, Jul;66(1):108-16 PMID: 26034200
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AMP-activated protein kinase (AMPK) activator
Metformin is an AMP-activated protein kinase (AMPK) activator that improves glycemic control by improving insulin sensitivity and decreasing intestinal absorption of glucose.- Jingyeong Shin, .et al. , Chemical Engineering Journal, 2023, December
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AMPK inhibitor
BML-275 is a cell-permeable pyrazolopyrimidine compound shown to be an AMP-activated protein kinase (AMPK) and fatty acid synthase inhibitor.- Yinhua Ni, .et al. , J Agric Food Chem, 2024, Jul 31;72(30):16708-16725 PMID: 39016108
- Yinhua Ni, .et al. , J Nutr Biochem, 2024, Mar:125:109569 PMID: 38185346
- Yu-Ting Chen, .et al. , World Neurosurg, 2023, Dec:180:e350-e363 PMID: 37757945
- Yang PM, .et al. , Am J Cancer Res, 2019, Oct 1;9(10):2120-2139 PMID: 31720078
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BMP inhibitor
Dorsomorphin, also known as BML-275, is a selective small molecule inhibitor of BMP signaling, which promotes cardiomyogenesis in embryonic stem cells. Dorsomorphin reverses the mesenchymal phenotype of breast cancer initiating cells by inhibition of bone morphogenetic protein signaling.- Guanya Li, .et al. , J Virol, 2024, Sep 17;98(9):e0060424 PMID: 39194241
- Kameshima S, .et al. , Apoptosis, 2019, Feb 8 PMID: 30737648
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AMPK activator
GSK621 is a potent and selective AMPK agonist.- Harvey W. Smith, .et al. , Nat Commun, 2019, 10, 2901(2019) PMID: 31263101
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NUAK1 inhibitor
HTH-01-015 is a potent and selective inhibitor of NUAK1 (IC50 = 100 nM) and does not affect the activity of a panel of 139 other kinases, including additional AMPK family members. -
AMPK activator
EX229 (compound 991) is a potent AMPK activator that is 5-10-fold more potent than A769662 in activating AMPK.- CN Koyani, .et al. , Pharmacol Res, 2020, May 17;158:104870 PMID: 32434052
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AMPK activator
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. -
AMPK activator
7-Methoxyisoflavone is an isoflavone derivative and also an activator of adenosine monophosphate-activated protein kinase (AMPK). -
mitochondria-targeted antioxidant
Demethyleneberberine is a natural mitochondria-targeted antioxidant. -
bitter taste receptor TAS2R1 agonist
Amarogentin (AG), a secoiridoid glycoside mainly extracted from Swertia and Gentiana roots, exhibits anti-oxidative, anti-tumour, and anti-diabetic activities. Amarogentin is an agonist for the bitter taste receptor TAS2R1 and inhibits in LAD-2 cells substance P-induced production of newly synthesized TNF-α. -
NF-κB inhibitor
Urolithin B is one of the gut microbial metabolites of ellagitannins, and has anti-inflammatory and antioxidant effects. Urolithin B is also a regulator of skeletal muscle mass. -
AMPK activator
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. -
HDAC inhibitor
Marein is a natural compound with multifaceted pharmacological properties, including HDAC inhibition with an IC₅₀ of 100 μM. It exerts neuroprotective effects by preserving mitochondrial function and activating the AMPK signaling pathway. In HepG2 cells, Marein improves high glucose–induced insulin resistance by enhancing glucose uptake via the CaMKK/AMPK/GLUT1 pathway, promoting glycogen synthesis through the IRS/Akt/GSK-3β pathway, and suppressing gluconeogenesis via the Akt/FoxO1 axis. Additionally, Marein possesses antioxidative, antihypertensive, antihyperlipidemic, and antidiabetic properties, making it a promising candidate for metabolic and neurodegenerative disease research. -
AMPK Agonist
10-Gingerol is an AMPK agonist derived from ginger oleoresin, exhibiting notable anti-inflammatory, antioxidant, and anti-proliferative properties. It effectively suppresses neointimal hyperplasia and inhibits the proliferation of vascular smooth muscle cells. Demonstrating significant radical scavenging activities, 10-Gingerol has IC50 values of 10.47 μM against DPPH, 1.68 μM against superoxide, and 1.35 μM against hydroxyl radicals. This compound also inhibits MDA-MB-231 tumor cell line proliferation with an IC50 of 12.1 μM, while targeting the PI3K/Akt signaling pathway to suppress proliferation, migration, invasion, and promote apoptosis. It holds potential for research applications in ulcerative colitis. -
ENO1 Inhibitor/AMPK Activator.
SU212 acts as an ENO1 inhibitor and AMPK activator, selectively inducing oxidative phosphorylation while reducing glycolysis and glucose uptake in tumor cells. This compound binds directly to ENO1, promoting apoptosis and ENO1 degradation through proteasomal and autophagic pathways, without affecting normal cells. Additionally, SU212 leads to mitotic arrest and apoptosis in triple-negative breast cancer (TNBC) cells, showcasing significant anti-tumor activity in vitro. It inhibits tumor growth and metastasis in various in vivo models, including syngeneic, xenograft, and diabetic mice, and has demonstrated an excellent safety profile, making it a valuable tool for research in TNBC, diabetes, and fatty liver disease. -
AMPK Activator
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. -
AMPK Activator
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. -
NF-κB Inhibitor/Nrf2/AMPK Activator
Panduratin A is a potent inhibitor of the NF-κB signaling pathway, recognized for its significant anti-inflammatory and antioxidant properties. It demonstrates protective effects against nephrotoxicity induced by Colistin, primarily by mitigating oxidative stress and enhancing mitochondrial function. Additionally, Panduratin A activates autophagy through an AMPK-dependent mechanism and exhibits potential anti-tuberculosis and antiviral activities by inhibiting the methyltransferase of SARS-CoV-2. These diverse biological activities make Panduratin A a valuable tool in various areas of research, including inflammation, cellular stress responses, and infectious diseases. -
MARK/SIK/AMPK Inhibitor
MRT199665 is a potent, ATP-competitive inhibitor targeting MARK, SIK, and AMPK pathways, exhibiting IC50 values of 2 nM for MARK1, 10 nM for AMPKα1, and 110 nM for SIK1. This compound induces apoptosis in MEF2C-activated human acute myeloid leukemia (AML) cells by effectively inhibiting the phosphorylation of the SIK substrate CRTC3 at S370. MRT199665 serves as a valuable tool for investigating the roles of MARK, SIK, and AMPK in cellular signaling and cancer biology. -
AMPK Activator
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. -
AMPK Activator
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. -
AMPK Activator
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. -
HSF1/AMPK Axis Activator
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. -
AMPK Activator
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. -
AMPK Activator
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. -
AMPK Activator
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. -
AMPK Inducer
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. -
AMPK Activator/mTOR Inhibitor
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. -
AMPK Activator
Foenumoside B is a triterpene saponin that activates AMP-activated protein kinase (AMPK) signaling. This compound inhibits PPARγ-induced adipogenesis and promotes lipid metabolism shift towards lipolysis. Foenumoside B is useful for investigating obesity and related metabolic disorders, making it a valuable tool for research in metabolic health. -
AMPK Activator
IMM-H007 is a potent AMPK (AMP-activated protein kinase) activator and TGFβ1 (transforming growth factor β1) antagonist. This compound exhibits cardioprotective effects by activating AMPK, which subsequently reduces endothelial inflammation through the inactivation of NF-κB and JNK/AP1 signaling pathways. Additionally, IMM-H007 regulates lipid metabolism, effectively resolving hepatic steatosis in high-fat diet-fed hamsters. It is suitable for research applications focused on nonalcoholic fatty liver disease (NAFLD) and inflammatory atherosclerosis. -
AMPK Activator
AMPK Activator 18 is a potent allosteric activator of AMPK complexes, particularly those containing the β2 isoform. It effectively activates α2-containing AMPK α2β2γ1 and α2β2γ3 complexes, exhibiting EC50 values of 17.2 nM and 82.1 nM, respectively. This compound stimulates β2-AMPK in cellular contexts and enhances glucose uptake in isolated skeletal muscle. Additionally, AMPK Activator 18 promotes phosphorylation of acetyl-coenzyme A carboxylase (ACC) and AMPK at the α-T172 site, making it a valuable tool for research in type 2 diabetes. -
AMPK Inhibitor
AMPK activator 16 is a potent AMP-activated protein kinase (AMPK) activator that effectively enhances AMPK signaling. It promotes the phosphorylation of AMPK, subsequently increasing the levels of phosphorylated acetyl-CoA carboxylase (p-ACC) and phosphorylated raptor (p-raptor) in N2a cells. This compound is instrumental in studies exploring metabolic regulation and signaling pathways linked to energy homeostasis and cellular stress responses. -
AMPK Activator
Galegine hemisulfate is a guanidine derivative that functions as an AMPK activator. It has demonstrated potential in promoting weight loss in mice and effectively activates AMPK in 3T3-L1 adipocytes, L6 myotubes, H4IIE rat hepatoma, and HEK293 human kidney cell lines. Additionally, Galegine hemisulfate exhibits antibacterial properties, with a minimum inhibitory concentration of 4 mg/L against strains of Staphylococcus aureus, making it relevant for various biological research applications.
