Cat. No. 3066
Chemical Name: N-[1-[[(Cyanomethyl)amino]carbonyl]
Biological ActivityPotent, 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.
Certificate of Analysis / Product Datasheet / Safety Datasheet
References are publications that support the products' biological activity.
Desmarais et al (2008) Effects of cathepsin K inhibitors basicity on in vivo off-target activities. Mol.Pharmacol. 73 147. PMID: 17940194.
Falgueyret et al (2005) Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity. J.Med.Chem. 48 7535. PMID: 16302795.
Palmer et al (2005) Design and synthesis of tri-ring P3 benamide-containing aminonitriles as potent, selective, orally effective inhibitors of cathepsin K. J.Med.Chem. 48 7520. PMID: 16302794.
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