Kinetic constants for hPCFT
Kinetic constants for compound 1 and Pmx (Kt and Vmax) were determined with [3H]compound 1 and [3H]Pmx, respectively, and calculated from Lineweaver Burk plots with R1–11-PCFT4 HeLa cells. Results are presented as mean values ± S.E. from three experiments.
| Substrate and Parameter | pH 5.5 | pH 6.8 |
|---|---|---|
| Pmx | ||
| Kt, μM | 0.03 ± 0.003 | 4.43 ± 0.253 |
| Vmax, pmol · mg−1 · min−1 | 1.27 ± 0.023 | 2.18 ± 0.317 |
| Vmax/Kt | 42.3 | 0.49 |
| Compound 1 | ||
| Kt, μM | 0.02 ± 0.013 | 5.91 ± 1.36 |
| Vmax, pmol · mg−1 · min−1 | 1.76 ± 0.154 | 3.08 ± 0.451 |
| Vmax/Kt | 88 | 0.52 |