Z-FY-CHO

Z-Phe-Tyr-CHO (167498-29-5) is 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

Z-Phe-Tyr-aldehyde is a cathepsin L inhibitor useful in the study of human osteoclast resorption and drug development for the treatment of coronavirus disease.

cathepsin L

[1] JE-TAE WOO. Peptidyl aldehyde derivatives as potent and selective inhibitors of cathepsin L[J]. Bioorganic & Medicinal Chemistry Letters, 1995, 5 14: Pages 1501-1504. DOI:10.1016/0960-894x(95)00236-m
[2] JE-TAE WOO . Suppressive effect of N-(benzyloxycarbonyl)-l-phenylalanyl-l-tyrosinal on bone resorption in vitro and in vivo[J]. European journal of pharmacology, 1996, 300 1: Pages 131-135. DOI:10.1016/0014-2999(95)00858-6
[3] I E JAMES. Potent and selective cathepsin L inhibitors do not inhibit human osteoclast resorption in vitro.[J]. The Journal of Biological Chemistry, 2001, 276 15: 11507-11511. DOI:10.1074/jbc.m010684200
[4] ALLEN KAASIK. Up-regulation of lysosomal cathepsin L and autophagy during neuronal death induced by reduced serum and potassium[J]. European Journal of Neuroscience, 2005, 22 5: 1023-1031. DOI:10.1111/j.1460-9568.2005.04279.x