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, and modulation of insulin secretion 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.
||AICAR is an activator of AMP-activated protein kinase (AMPK), down-regulates the insulin receptor expression in HepG2 cells.
||Dorsomorphin dihydrochloride is a potent and selective AMPK inhibitor, that is competitive with ATP, with Ki of 109±16 nM in the absence of AMP.
||Phenformin (hydrochloride) is a hydrochloride salt of phenformin that is an anti-diabetic drug from the biguanide class, can activate AMPK activity.
||HTH-01-015 is a selective NUAK1 inhibitor (IC50 is 100 nM). HTH-01-015 inhibits NUAK1 with >100-fold higher potency than NUAK2 (IC50 of >10 μM).
||A-769662 is a potent, reversible AMPK activator with EC50 of 0.8 μM, and has little effect on GPPase/FBPase activity.
||Metformin (hydrochloride) is a first-line drug for the treatment of type 2 diabetes and there is increasing evidence of a potential efficacy of this agent as an anti-cancer drug.
||WZ4003 is the first potent and highly specific NUAK kinase inhibitor with IC50 of 20 nM/100 nM for NUAK1/NUAK2, without significant inhibition on other 139 kinases.
||YLF-466D is a newly developed AMPK activator, which inhibits platelet aggregation.
||AICAR (Acadesine) phosphate
||AICAR phosphate is an activator of AMP-activated protein kinase (AMPK), down-regulates the insulin receptor expression in HepG2 cells.
||BAY-3827 (BAY3827) is a potent, selective inhibitor of AMPK as tool compound to evaluate the therapeutic potential of AMPK
inhibition in MYC-dependent tumors.
||PF-06409577(PF06409577, PF 6409577) is a potent, selective AMPK β1-containing isoforms activator with TR-FRET EC50 of 7.0 and 6.8 nM for α1β1γ1 and α2β1γ1, respectively.
||GSK621 (GSK-621) is a potent, specific AMPK agonist (activator), induces cytotoxicity in AML (IC50=13-30 uM) but not in normal hematopoietic cells.
||A potent, selective, allosteric pan-AMPK activator with EC50 of 1-60 nM for all 12 mammalian AMPK isoforms.
||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.
||A small molecule AMPK activator that dose-dependently increases AMPK activity of α1-, α2-, β1- and β2-containing complexes at 50 uM.
||A potent, allosteric, α1-selective small molecule activator of AMPK (EC50=20 nM).