Potent, reversible cathepsin K inhibitor (IC50
= 0.25 nM) that displays > 4000-fold selectivity over cathepsins B, L and S. Displays reduced selectivity in cell-based assays possibly due to lysosomal accumulation. Reduces collagen breakdown and promotes bone deposition in vivo
. Orally active and has intrinsic fluorescence.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity.
Falgueyret et al.
Effects of cathepsin K inhibitors basicity on in vivo off-target activities.
Desmarais et al.
Design and synthesis of tri-ring P3 benamide-containing aminonitriles as potent, selective, orally effective inhibitors of cathepsin K.
Palmer et al.