219377
Cathepsin K Inhibitor I
The Cathepsin K Inhibitor I controls the biological activity of Cathepsin K. This small molecule/inhibitor is primarily used for Protease Inhibitors applications.
Synonym(s):
Cathepsin K Inhibitor I, 1,3-Bis(CBZ-Leu-NH)-2-propanone, 1,3-Bis(N-carbobenzoyloxy-L-leucyl)amino Acetone
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About This Item
Empirical Formula (Hill Notation):
C31H42N4O7
Molecular Weight:
582.69
UNSPSC Code:
12352200
NACRES:
NA.77
Recommended Products
Quality Level
Assay
≥95% (HPLC)
form
lyophilized solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
color
off-white
solubility
methanol: 1 mg/mL
DMSO: soluble
shipped in
wet ice
storage temp.
−20°C
General description
A cell-permeable, symmetrical bis(acylamino)ketone compound that acts as a potent, selective, reversible inhibitor of cathepsin K (Ki, = 22 nM). Also shown to inhibit cathepsin K in stably transfected CHO cells (IC50 = 134 nM). Reported to bind to cathepsin K and span both the S- and S′- subsites. Inhibits papain (Ki >10 µM), trypsin (Ki >50 µM), and chymotrypsin (Ki >50 µM) only at higher concentrations. Exhibits greater selectivity for cysteine proteases of the papain family (Ki = 340 nM, 890 nM, and 1-3 µM for cathepsin L, cathepsin S, and cathepsin B, respectively).
A cell-permeable, symmetrical bis(acylamino)ketone that acts as a potent, selective, and reversible inhibitor of cathepsin K (Ki,app = 22 nM). Shown to bind to cathepsin K and span both the S- and S′-subsites. A poor inhibitor of papain (Ki,app >10 µM) but displays greater selectivity towards other proteases of the papain family (Ki,app = 340 nM, 890 nM, and 1.3 µM for cathepsin L, cathepsin S, and cathepsin B respectively). Inhibits trypsin and chymotrypsin activities only at higher concentrations (Ki,app ≥ 50 µM).
Biochem/physiol Actions
Cell permeable: yes
Primary Target
cathepsin K
cathepsin K
Product does not compete with ATP.
Reversible: yes
Target Ki: 22 nM against cathepsin K
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Sequence
Cbz-Leu-NH-CH₂-CO-CH₂-NH-Leu-Cbz
Reconstitution
Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Claveau, D., et al. 2000. Biochem. Pharmacol.60, 759.
LaLonde, J.M., et al. 1999. Biochemistry38, 862.
Yamashita, D.S., et al. 1997. J. Am. Chem. Soc.119, 11351.
LaLonde, J.M., et al. 1999. Biochemistry38, 862.
Yamashita, D.S., et al. 1997. J. Am. Chem. Soc.119, 11351.
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
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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