Table I.
The ability of M503902 to inhibit purified full-length recombinant human MMPs (expressed in bacculo virus) was determined against synthetic peptide substrates, (substrate concentration at Km)
| Matrixin | Peptide substrate | M503902 |
|
|---|---|---|---|
| IC50 mean ± S.E.M (n=) | Ratio (MMPx/MMP13) | ||
| MMP-13 | MCA-Pro-Cha-Gly-Nva-Dpa-Ala-Arg-NH2 | 0.35 ± 0.05 nM3 | 1 |
| MMP-1 | MCA-Pro-Cha-Gly-Nva-His-Ala-Dpa-NH2 | 119 ± 14.5 nM3 | 340 |
| MMP-2 | MCA-Pro-Cha-Gly-Nva-His-Ala-Dpa-NH2 | 0.1 nM1 | 0.29 |
| MMP-3 | MCA-Pro-Cha-Gly-Nva-His-Ala-Dpa-NH2 | 1.9 nM1 | 5.4 |
| MMP-7 | MCA-Pro-Cha-Gly-Nva-His-Ala-Dpa-NH2 | 325 ± 28.9 nM3 | 929 |
| MMP-8 | MCA-Pro-Cha-Gly-Nva-His-Ala-Dpa-NH2 | 0.6 nM1 | 1.71 |
| MMP-9 | MCA-Pro-Cha-Gly-Nva-His-Ala-Dpa-NH2 | 0.26 ± 0.06 nM5 | 0.74 |
| MMP-12 | MCA-Pro-Cha-Gly-Nva-His-Ala-Dpa-NH2 | 0.45 nM1 | 1.26 |
| MMP-14 | MCA-Pro-Cha-Gly-Nva-His-Ala-Dpa-NH2 | 3.05 ± 0.67 nM5 | 8.7 |
| MMP-19 | MCA-Pro-Leu-Ala-Nva-Dpa-Ala-Arg-NH2 | 7.2 ± 0.24 nM11 | 20.6 |
MMPx = X is the number of matrixin in column 1.