Table 1 Effect of MK-2206 on insulin-stimulated phosphorylation of Akt and its substrates, GLUT4 translocation and glucose uptake in 3T3-L1 adipocytes

IC50 values and R2 were calculated using data from Figures 1(B)–1(D). The percentage of inhibition was calculated by quantification of Western blot analysis in Figure 1 for phosphorylation of Akt and its substrates, and Figure 2 for glucose uptake and for GLUT4 assay. Values are expressed as the percentage of inhibition as compared with 1 μM insulin-treated cells.

SubstrateIC50 (μM)R2Inhibition (%)
Thr308 Akt0.111.0088.66
Ser473 Akt0.181.0083.23
Ser588 AS1600.040.9890.91
Thr642 AS1600.260.9980.58
Thr1462 TSC20.270.9179.36
Ser256 FoxO10.040.9598.20
Ser246 PRAS400.650.8469.58
Ser21 GSK3α0.560.9865.44
Ser9 GSK3β1.010.9653.66
PM GLUT40.470.9954.30
Glucose uptake0.140.9863.69