TABLE 1.
Summary of IC50 values for BSIs in an in vitro BACE1 assay under various conditions
| Parameter | IC50 ± S.D. |
IC50 ratio (swe:wt) | |
|---|---|---|---|
| Wt | Swe | ||
| nm | |||
| β-Secretase inhibitor compound | |||
| OM99–2 | 3.3 ± 0.3 | 2.4 ± 0.1 | 0.7 |
| Inhibitor IV | 12.4 ± 2.3 | 9.8 ± 0.9 | 0.8 |
| Reaction timea | |||
| 3 h | 3.5 ± 0.5 | 4.1 ± 1.0 | 1.2 |
| 6 h | 5.4 ± 1.9 | 8.2 ± 1.4 | 1.5 |
| 24 h | 6.0 ± 1.1 | 9.4 ± 0.5 | 1.5 |
| Substrate/enzyme ratioa | |||
| 200:1 | 19 ± 2 | 23 ± 6 | 1.2 |
| 50:4 | 21 ± 3 | 28 ± 6 | 1.3 |
| 25:8 | 24 ± 5 | 32 ± 6 | 1.4 |
| 16:16 | 26 ± 6 | 46 ± 10 | 1.7 |
| pHa | |||
| 4.6 | 5.6 ± 1.0 | 5.0 ± 1.1 | 0.9 |
| 6.2 | 5.6 ± 0.4 | 4.6 ± 1.7 | 0.8 |
a These experiments were performed using Inhibitor IV.