Figure 3
From: Continuous real-time measurement of tumor necrosis factor-α converting enzyme activity on live cells
Validation of the FAM–TAMRA TNF peptide-based assay for specific detection of TACE enzyme activity. (a) GM6001-mediated inhibition of the peptide cleavage by THP-1 cells (•) was compared to GM6001-mediated inhibition of proTNF cleavage from the surface of THP-1 cells (▴). Both curves were similar with an IC50 of 5.5±3 μM for the peptide cleavage and 13±15 μM for the proTNF cleavage (n=3). (b) GW280264X (•), a dual TACE/ADAM-10 inhibitor, induced substantial inhibition in the peptide cleavage at concentrations >10 μM (IC50 4.5±0.3 μM), while selective ADAM-10 inhibitor GI254023X (▴) induced only minimal inhibition (IC50 >100 μM) (n=6). Data presented as mean±s.e.
