Inhibitory potency of Ro 32-7315 (nanomolar) against recombinant TACE, selected human MMPs, and LPS-induced TNF-α release in THP cells and whole blood
| Assay Mixture | IC50 |
|---|---|
| nM | |
| Enzyme assay | |
| TACE | 5.2 (n = 3) |
| Collagenase 1 (MMP 1) | 500 (n = 2) |
| Collagenase 2 (MMP 8) | 25 (n = 2) |
| Collagenase 3 (MMP 13) | 110 (n = 2) |
| Stromelysin 1 (MMP 3) | 190 (n = 2) |
| Gelatinase A (MMP 2) | 250 (n = 2) |
| Gelatinase B (MMP 9) | 100 (n = 2) |
| Metalloelastase (MMP 12) | 11 (n = 2) |
| Matrilysin 1 (MMP 7) | 250 (n = 2) |
| Cellular assay | |
| THP-1 cells | 350 ± 14 (n = 5) |
| Rat whole blood | 110 ± 18 (n = 5) |
| Human whole blood | 2400 ± 500 (n = 5) |
Ro 32-7315 was serially diluted from an initial concentration of 10 mM for IC50 determination. A constant vehicle concentration (0.5% or 0.8% DMSO) was maintained in the final assay mixture.