YLF-466D is an allosteric AMPK activator.
YLF466D activated recombinant human 111, 211 and rat liver AMPK. It also activated AMPK -subunit truncations containing an autoinhibitory domain(AID) and exhibited additivity with AMP and A-769662. Molecular docking of YLF466D with the S pombe AMPKa (25-351) suggests it may bind in the cleft between the kinase domain and the AID antagonizing the auto-inhibition distinct from AMP and A-769662. Incubation of YLF466D in Hela cells activated cellular AMPK without detectable changes in AMP:ATP ratio, proving AMPK was allosterically activated by YLF466D. YLF466D activated cellular AMPK in both L6 myotubes and HepG2 cells with evoking intracellular AMP:ATP ratio accompanied by depolarizing mitochondria membrane potential, but has no effect on the dephosphorylation of PP2C on AMPK. Thus, YLF466D activated cellular AMPK through dual mechanisms [1].
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