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Request The Product List ofAMPK AMPK

AMPK (AMP-activated protein kinase) is an enzyme that plays a role in cellular energy homeostasis. It consists of three proteins (subunits) that together make a functional enzyme. The net effect of AMPK activation is stimulation of hepatic fatty acid oxidation andketogenesis, inhibition of cholesterol synthesis, lipogenesis, and triglyceride synthesis, inhibition of adipocyte lipolysis and lipogenesis, stimulation of skeletal muscle fatty acid oxidation and muscle glucose uptake by pancreatic beta-cells. AMPK acts as a metabolic master switch regulating several intracellular systems including the cellular uptake of glucose, the β-oxidation of fatty acids and the biogenesis of glucose transporter 4 (GLUT4) and mitochondria.

Cat. No. Product Name CAS No. Information



A potent, allosteric, α1-selective small molecule activator of AMPK (EC50=20 nM); inhibits de novo lipogenesis in cellular and animal models of hyperlipidemia; the cell-permeable prodrug of compound 2 (AMPK-Activator-2).




EX-229 is a small molecule AMPK activator that dose-dependently increases AMPK activity of α1-, α2-, β1- and β2-containing complexes at 50 uM; induces AMPK activation and glucose uptak in a wortmannin-independent manner; increases fatty acid oxidation in L6 myotubes.




PF-739 is a novel potent, pan-AMPK activator with similar potency for all AMPK heterotrimers; increases the phosphorylation of the AMPK substrate ACC at S79 with EC50 of 121 nM, potently inhibits de novo lipogenesis (IC50=25 nM) in primary rat hepatocytes; increases PGC1a transcription and mitochondrial content, effectively activats AMPK in hepatocytes and in skeletal muscle; caused a rapid lowering of plasma glucose levels with no impact on hepatic glucose production in diabetic mice.




MK-8722 is a potent, selective, allosteric pan-AMPK activator with EC50 of 1-60 nM for all 12 mammalian AMPK isoforms; exhibits higher affinity for β1-containing (1-6 nM) versus β2-containing (15-63 nM) pAMPK complexes; increases glucose uptake into skeletal muscle in vitro and in vivo, but induces cardiac hypertrophy.




PF-06685249 is a novel potent, orally active, α1β1γ1/α2β1γ1-isoform selective AMPK activator with Kd of 14 nM, EC50 of 12 nM for α1β1γ1-AMPK, shows minimal activity at the β2-containing isoforms (α1β2γ1, α2β2γ1, α2β2γ3); demonstrates in vivo target engagement experiment in ZSF-1 rats, an obese/diabetic rodent model of diabetic nephropathy.



BL-AD008 (BL-AD 008) is a novel small molecule, dual-target activator targeting AMPK/ZIPK; demonstrates remarkable anti-proliferative activities toward cervical cancer cells and could induce apoptosis by death-receptor and mitochondrial pathways; also shows anti-tumor activities and induces apoptosis by targeting AMPK/ZIPK in vivo.


AICAR phosphate


AICAR phosphate (Acadesine, AICA Riboside, NSC 105823) is a selective AMPK activator in both hepatocytes and adipocytes; inhibits the synthesis of fatty acids and sterols and inactivates HMG-CoA reductase in rat hepatocytes at 0.5 mM, inhibits insulin-stimulated glucose and reduces GLUT4 translocation in 3T3-L1 adipocytes; down-regulates the insulin receptor expression in HepG2 cells.




A-769662 is a small molecule AMPK activator that directly stimulates partially purified rat liver AMPK (EC50=0.8 uM) and inhibits fatty acid synthesis in primary rat hepatocytes (IC50=3.2 uM); decreases hepatic expression of PEPCK, G6Pase, and FAS, lowered plasma glucose by 40%, reduces body weight gain and significantly decreases both plasma and liver triglyceride levels in ob/ob mice (30 mg/kg b.i.d.); also directly inhibits Na(+)-K(+)-ATPase, decreases the sodium pump cell surface abundance in L6 skeletal muscle cells.




HTH-01-015 is a potent, specific NUAK1 (AMPK-related kinase 5, ARK5) inhibitor with IC50 of 100 nM, displays >100-fold higher potency than NUAK2; also does not markedly suppress the activity of any of the other 139 protein kinases, including AMPK; suppresses NUAK1-mediated MYPT1 phosphorylation in vivo, the NUAK1 mutation (A195T) renders resistant to HTH-01-015; significantly inhibits migration the proliferation of MEFs (mouse embryonic fibroblasts).




Dorsomorphin (BML-275, Compound C) is a potent, selective and reversible AMPK inhibitor with Ki of 109 nM, shows no no significant activity on ZAPK, SYK, PKCθ, PKA and JAK3; inhibits AMPK activation induced by AICAR and Metformin, also inhibits bone morphogenetic protein (BMP) type I receptors (ALK2, ALK3 and ALK6); promotes cardiomyogenesis in mouse embryonic stem cells (ESCs) in vitro, induces autophagy in cancer cell lines via a mechanism independent of AMPK inhibition.

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