219377 Cathepsin K Inhibitor I - Calbiochem

219377
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Overview

Replacement Information

Key Spec Table

Empirical Formula
C₃₁H₄₂N₄O₇

Pricing & Availability

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219377-5MG
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      Plastic ampoule 5 mg
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      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

      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.