Table 2

Protease inhibitory activity of the matrix metalloproteinase MMP Inhibitor PD 166793

Enzyme ClassificationIC502-a
μM
MMP2-b
 Interstitial collagenase
  MMP-16.100
 Stromelysins
  MMP-30.012
  MMP-78.100
 Gelatinases
  MMP-20.047
  MMP-99.900
ACE>100 (n/c)2-c
Neutral endopeptidase>100 (n/c)2-c
Endothelin-converting enzyme>100 (n/c)2-c
Tumor necrosis factor α-converting enzyme>100 (n/c)2-c
  • 2-a Data expressed as concentration necessary to inhibit 50% of maximal enzyme activity.

  • 2-b MMP activity assays determined with recombinant human MMP constructs of the catalytic domain and an artificial substrate assay system.

  • 2-c PD166793 was not active at up to 100 μM and therefore a true IC50 was not computed (n/c).