Table 3. Inhibition of MMP-1, MMP-2, MMP-8, MMP-9, MMP-13, and MMP-14 activity by compounds 4, 20 and 24.
Assays were performed using 40 μM of each compound and fTHP-15 as substrate as described.5 Enzyme concentrations were 10 nM for MMP-2, MMP-9, and MMP-14, 2.3 nM for MMP-13, 4 nM for MMP-1, and 2 nM for MMP-8.
| Target | Inhibition (%) at [inhibitor] = 40 μM | ||
|---|---|---|---|
| 4 | 20 | 24 | |
| MMP-1 | 0 | 0 | 0 |
| MMP-2 | 25 ± 11 | 19 ± 2.1 | 26 ± 9.2 |
| MMP-8 | 17 ± 3.0 | 0 | 8.0 ± 5.0 |
| MMP-9 | 10 ± 4.0 | 7.0 ± 3.0 | 16 ± 4.0 |
| MMP-13 | 51 ± 0 | 67 ± 2.0 | 61 ± 1.0 |
| MMP-14 | 22 ± 5.0 | 20 ± 6.0 | 31 ± 9.0 |