Z-FY-CHO Chemical Properties

Boiling point:

726.5±60.0 °C(Predicted)

Density 

1.249±0.06 g/cm3(Predicted)

storage temp. 

-15°C

solubility 

Soluble in DMSO (up to 30 mg/ml) or in Ethanol (up to 50 mg/ml)

pka

9.87±0.15(Predicted)

form 

solid

color 

Off-white to pale yellow

Stability:

Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 1 month.

Z-FY-CHO Usage And Synthesis

Description

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

Uses

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.

References

1) Woo et al. (1995), Peptidyl aldehyde derivatives as potent and selective inhibitors of cathepsin L; Bioorg. Med. Chem. Lett., 5 1501 2) Woo et al. (1996), Suppressive effect of N-(benzyloxycarbonyl)-L-phenylalanyl-L-tyrosinal on bone resorption in vitro and in vivo; Eur. J. Pharmacol., 300 131 3) James et al. (2001) Potent and selective cathepsin L inhibitors do not inhibit human osteoclast resoption in vitro; J. Biol. Chem., 276 11507 4) Kaasik et al. (2005), Up regulation if lysosomal cathepsin L and autophagy during neuronal death induced by reduced serum and potassium; Eur. J. Neurosci., 22 1023

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