Millipore Sigma Vibrant Logo
Attention: We have moved. Merck Millipore products are no longer available for purchase on MerckMillipore.com.Learn More

219377 Cathepsin K Inhibitor I - Calbiochem

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

Cathepsin K Inhibitor I - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 1,3-Bis(CBZ-Leu-NH)-2-propanone, 1,3-Bis(N-carbobenzoyloxy-L-leucyl)amino Acetone

Primary Target: cathepsin K
219377
Purchase on Sigma-Aldrich

Overview

Replacement Information

Key Spec Table

Empirical Formula
C₃₁H₄₂N₄O₇

Products

Catalogue NumberPackaging Qty/Pack
219377-5MGCN Plastic ampoule 5 mg
Description
OverviewA 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).
Catalogue Number219377
Brand Family Calbiochem®
Synonyms1,3-Bis(CBZ-Leu-NH)-2-propanone, 1,3-Bis(N-carbobenzoyloxy-L-leucyl)amino Acetone
References
ReferencesClaveau, D., et al. 2000. Biochem. Pharmacol. 60, 759.
LaLonde, J.M., et al. 1999. Biochemistry 38, 862.
Yamashita, D.S., et al. 1997. J. Am. Chem. Soc. 119, 11351.
Product Information
ATP CompetitiveN
FormOff-white lyophilized solid
Hill FormulaC₃₁H₄₂N₄O₇
Chemical formulaC₃₁H₄₂N₄O₇
ReversibleY
Quality LevelMQ100
Applications
Biological Information
Primary Targetcathepsin K
Primary Target K<sub>i</sub>22 nM against cathepsin K
Purity≥95% by HPLC
Physicochemical Information
Cell permeableY
Peptide SequenceCbz-Leu-NH-CH₂-CO-CH₂-NH-Leu-Cbz
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Blue Ice Only
Toxicity Standard Handling
Storage -20°C
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalogue Number GTIN
219377-5MGCN 04055977201598

Documentation

Cathepsin K Inhibitor I - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

Cathepsin K Inhibitor I - Calbiochem Certificates of Analysis

TitleLot Number
219377

References

Reference overview
Claveau, D., et al. 2000. Biochem. Pharmacol. 60, 759.
LaLonde, J.M., et al. 1999. Biochemistry 38, 862.
Yamashita, D.S., et al. 1997. J. Am. Chem. Soc. 119, 11351.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision05-June-2008 RFH
Synonyms1,3-Bis(CBZ-Leu-NH)-2-propanone, 1,3-Bis(N-carbobenzoyloxy-L-leucyl)amino Acetone
DescriptionA 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).
FormOff-white lyophilized solid
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₃₁H₄₂N₄O₇
Peptide SequenceCbz-Leu-NH-CH₂-CO-CH₂-NH-Leu-Cbz
Purity≥95% by HPLC
SolubilityMethanol (1 mg/ml) or DMSO
Storage -20°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesClaveau, D., et al. 2000. Biochem. Pharmacol. 60, 759.
LaLonde, J.M., et al. 1999. Biochemistry 38, 862.
Yamashita, D.S., et al. 1997. J. Am. Chem. Soc. 119, 11351.