219377 Cathepsin K Inhibitor I - Calbiochem

219377
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₃₁H₄₂N₄O₇

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      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
          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

          SDS

          Title

          Safety Data Sheet (SDS) 

          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.