Table 1. Kinetic analysis of inhibition by AcPH and AcPMe of intramitochondrial PDHC without preincubation with the analogs.
| AcPH | AcPMe | ||
|---|---|---|---|
| Vmax (μmol NADH/(min × mg protein)) | Ki (μM) | Vmax (μmol NADH/(min × mg protein)) | Ki (μM) |
| 0.1 | 0.1 | 0.13 | 40 |
| Inhibitor concentration (μM) | Kmapp (μM) | Inhibitor concentration (μM) | Kmapp (μM) |
| 0 | 12.5 | 0 | 18.7 |
| 0.001 | 18.1 | 10 | 14.4 |
| 0.01 | 19.4 | 50 | 27.5 |
| 0.1 | 31.0 | 100 | 41.1 |
| 0.5 | 324.2 | 500 | 173.4 |
Vmax and Km data were obtained by non-linear regression of the experimental dependences presented in Figures 4A, 4B, to the Michaelis-Menten equation using Prism 5.0 software (Graphpad). Ki is the x-axis intercept when plotting apparent Km (Kmapp) obtained at different inhibitor concentrations divided by Vapp against AcPH and AcPMe concentrations (Figure 4F).