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219381

Sigma-Aldrich

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

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About This Item

Empirical Formula (Hill Notation):
C30H43N7O6
Molecular Weight:
597.71
UNSPSC Code:
12352200
NACRES:
NA.77

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

General description

A cell-permeable peptidyl bis-carbohydrazide compound that acts as a potent, selective, and reversible inhibitor of cathepsin K (Ki,app = 9.7 nM). At higher concentrations, also inhibits the activities of cathepsin L, cathepsin B, and papain (Ki,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 (Ki,app = 9.7 nM). At higher concentrations also inhibits the activities of cathepsin L, cathepsin B, and papain (Ki,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 Ki: 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

Storage Class Code

11 - Combustible Solids

WGK

WGK 1

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Regulatory Listings

Regulatory Listings are mainly provided for chemical products. Only limited information can be provided here for non-chemical products. No entry means none of the components are listed. It is the user’s obligation to ensure the safe and legal use of the product.

JAN Code

219381-MG:
219381-1MG:

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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