Novel Small-Molecule AMP-Activated Protein Kinase Allosteric Activator with Beneficial Effects in db/db Mice
Figure 1
Activation of human AMPK heterotrimers by ZLN024.
(A) The structure of ZLN024 (molecular weight = 325.2). (B) The activation curve for ZLN024 and recombinant human AMPK α1β1γ1 (n = 2), α2β1γ1(n = 2) (C), α1β2γ1(n = 3) (D) and α2β2γ1(n = 3) (E). (F) ZLN024 concentration-dependently stimulates AMPK and ACC phosphorylation in L6 myotubes after incubation for 3 hr. The ratio of the phosphorylation level to the protein level of AMPK and ACC was determined (n = 3). (G) The time course of the stimulation of AMPK and ACC phosphorylation by ZLN024 (20 µmol/l). Metformin (2 mmol/l) was used as a positive control. The ratio of the phosphorylation level to the protein level of AMPK and ACC was determined (n = 3). #, P<0.1,*, P<0.05, **, P<0.01 compared with the untreated control.