Uptake characteristics of marizomib and NPI-0047 in RPMI 8226 and PC-3 cells
Total uptake was in the absence of unlabeled inhibitor. Diffusional component was uptake in the presence of unlabeled inhibitor.
| Compound | Cell Line | Uptake at 1 Min | Km | Vmax | Diffusional Component | |
|---|---|---|---|---|---|---|
| Total Uptake | Diffusional Component | |||||
| pmol/mg protein | μM | pmol/mg protein/min | μl/mg/min | |||
| Marizomib | RPMI | 0.08 ± 0.02 | 0.04 ± 0.02 | 0.4 ± 0.2 | 3.5 ± 2.1 | 1.4 ± 1.2 |
| NPI-0047 | RPMI | 0.10 ± 0.01 | 0.05 ± 0.01 | 0.2 ± 0.3 | 1.1 ± 1.4 | 3.4 ± 1.3 |
| Marizomib | PC-3 | 0.90 ± 0.06 | 0.48 ± 0.08 | 0.08 ± 0.2 | 3.0 ± 5.4 | 104 ± 9.1 |
| NPI-0047 | PC-3 | 0.93 ± 0.07 | 0.55 ± 0.06 | 0.03 ± 0.2 | 1.4 ± 4.0 | 91 ± 8.3 |