AMP-activated protein kinase (AMPK; EC is a heterotrimeric enzyme with a key role in regulating cellular energy metabolism, cell growth and cell polarity. In response to a change in the intracellular AMP:ATP or ADP:ATP ratios it activates energy-producing pathways and inhibits energy-consuming processes. Furthermore, AMPK is regulated by a diverse range of hormones among which leptin, adiponectin, ciliary neurotrophic factor and ghrelin. Of the three subunits α, β, and γ that constitute the protein kinase, the α-subunit hosts the catalytic domain, while the latter two subunits β, and γ fulfill a regulatory function. Activation of AMPK is triggered by phosphorylation of a threonine residue, which lies in the activation segment of the amino-terminal kinase domain of the α-subunit and results in a several-hundred-fold increase in activity. In mammals, calcium/calmodulin-dependent protein kinase kinase-β (CaMKKβ), LKB1, and transforming growth factor-β-activated kinase 1 (TAK1)  are the predominant kinases upstream of AMPK[1]. In turn, activated, phosphorylated AMPK can be inactivated by protein phosphatases (PP), e.g. PP2A, PP2Cα and Ppm1E. Currently, AMPK is viewed as an important molecular target since it is believed that novel AMPK modulators may be useful in the therapy of cancer, metabolic, and neurodegenerative diseases, such as type 2 diabetes, Alzheimer’s disease, and aging[2],[3].

[1] Structure of mammalian AMPK and its regulation byADP. B. Xiao. Nature 2011, 472, 230-233.
[2] AMP-activated protein kinase (AMPK) controls the aging process via an integrated signaling network. A. Salminena, K. Kaarnirantac. Ageing Res. Rev. 2012, 11, 230-241.
[3] AMPK: a nutrient and energy sensor that maintains energy homeostasis. D.G. Hardie, F.A. Ross,  S.A. Hawley. Nature Rev. Mol. Cell Biol. 2012, 13, 251-262.

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1466 A 769662 AMPK activator €85.00
2389 AICAR Potent AMPK activator and inducer of differentiation of NSCs €45.00
3211 BC1618 Potent, orally bioavailable, and metabolically stable Fbxo48 inhibitor €120.00
2021 HL 010183 Metformin derivative; AMPK activator €135.00
3206 YW2065 Inhibitor of Wnt/β-catenin signalling; AMPK activator €95.00
2445 ZLN 024 Allosteric activator of AMP-activated protein kinase (AMPK) €90.00

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