Figure 2
From: Identification and characterization of the novel reversible and selective cathepsin X inhibitors
Selected inhibitors bind reversibly to cathepsin X. (a) Cathepsin X activity was measured immediately (dark grey) after 1-hour pre-incubation with selected compounds, or after 200000-fold dilution in activation buffer using a Centricon (10 kDa cut-off; Millipore) for washing out the compounds (light grey). After removing the compounds almost all cathepsin X activity was regained according to the control (DMSO) except in the case of irreversible inhibitor E-64. Values are means of two independent experiments, performed in duplicate ± S.E.M. (b) After rapid 100-fold dilution of (pre-incubated) cathepsin X (100-fold concentration) and compound (10-fold concentration) cathepsin X activity was measured. 90% of the recovered cathepsin X activity points toward reversible inhibitors with rapid dissociation. Inset: graph representation of activity measurements - control (green), E-64 (blue) and tested compounds (other colors).
