219381

Cathepsin K Inhibitor III

The Cathepsin K Inhibitor III controls the biological activity of Cathepsin K. This small molecule/inhibitor is primarily used for Protease Inhibitors applications.

• Synonym(s): Cathepsin K Inhibitor III, Inhibitor I, 1-(N-Benzyloxycarbonyl-leucyl)-5-(phenylalanyl-leucyl)carbohydrazide, Z-L-NHNHCONHNH-LF-NH₂
• Empirical Formula (Hill Notation): C₃₀H₄₃N₇O₆
• Molecular Weight: 597.71
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• Assay: ≥97% (HPLC)
• form: lyophilized solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; desiccated (hygroscopic)
• color: white
• solubility: DMSO: 1 mg/mL
• shipped in: wet ice
• storage temp.: −20°C

Description

General description

A cell-permeable peptidyl bis-carbohydrazide compound that acts as a potent, selective, and reversible inhibitor of cathepsin K (K_i,app = 9.7 nM). At higher concentrations, also inhibits the activities of cathepsin L, cathepsin B, and papain (K_i,app = 120 nM, 5.1 µM, and 2.3 µM, respectively). Completely blocks cathepsin K activity in primary human synovial fibroblast cultures at 1 µM.

A cell-permeable, potent, selective, reversible inhibitor of cathepsin K (K_i,app = 9.7 nM). At higher concentrations also inhibits the activities of cathepsin L, cathepsin B, and papain (K_i,app = 120 nM, 5.1 mM, and 2.3 µM, respectively). Reported to completely block cathepsin K activity in primary human synovial fibroblast cultures at a concentration of 1 µM.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
Cathepsin K

Product does not compete with ATP.

Reversible: yes

Target K_i: 9.7 nM against cathepsin K

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Sequence

H-Phe-Leu-NHNH-CO-NHNH-Leu-Z

Physical form

Supplied as a trifluoroacetate salt.

Reconstitution

Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Wang, D., et al. 2002. Biochemistry41, 8849.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 1
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable