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. 2018 Apr 25;293(23):8874–8885. doi: 10.1074/jbc.RA118.003547

Figure 1.

Figure 1.

Biochemical characterization of SBI-0206965. A, structures of SBI-0206965 and compound C. B, inhibition of AMPK α1β1γ1- and ULK1-phosphorylation of S108tide by SBI-0206965 and compound C. Error bars, mean percentage kinase activity versus untreated ± S.E. (error bars) (n = 3). **, p < 0.01; ***, p < 0.001; ****, p < 0.0001 by one-way ANOVA with post hoc Dunnett's multiple-comparison test versus untreated kinase. ####, p < 0.0001 by one-way ANOVA with post hoc Dunnett's multiple-comparison test versus compound C–treated AMPK. Shown are dose-response curves for SBI-0206965 inhibition of ULK1, AMPK α1β1γ1, and AMPK α2β1γ1 (C) and compound C inhibition of ULK1 and AMPK α1β1γ1 (D). For C and D, assays were performed at fixed 200 μm ATP. IC50 values (μm) ± S.E. were calculated from triplicate experiments. E, Thr-172 phosphorylation assay. Bacterially expressed AMPK α2β1γ1 was incubated with LKB1 in the presence of SBI-0206965, and pThr-172 was measured by immunoblotting. Error bars, mean pThr-172/α (arbitrary units) ± S.E. (n = 3).