A potent and selective inhibitor of cathepsin L, IC50=0.85 nM 1 selective over cathepsin B and calpain II (IC50s=85.1 and 184 nM respectively). Suppresses osteoclastic pit formation at 1.5 nM and markedly inhibited parathyroid hormone-stimulated osteoclastic bone resorption.2 Also inhibits cathepsin K (Kis=0.052 and 1.57 nM for cat L and cat K respectively) and partially provides the basis for the finding that cathepsin K is the protease responsible for osteoclastic bone resorption.3 Provides partial protection against serum and potassium deprivation-induced neuronal death.4 Active in vivo.2
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