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219377 Sigma-Aldrich

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.

Synonym: 1,3-Bis(CBZ-Leu-NH)-2-propanone, 1,3-Bis(N-carbobenzoyloxy-L-leucyl)amino Acetone, Cathepsin K Inhibitor I - Calbiochem

  • Empirical Formula (Hill Notation) C31H42N4O7

  • Molecular Weight 582.69

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Properties

assay   ≥95% (HPLC)
form   lyophilized solid
mfr. no.   Calbiochem®
storage condition   OK to freeze
storage conditions   -20C
color   off-white
solubility   methanol: 1 mg/mL
  DMSO: soluble
shipped in   wet ice

Description

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).

Packaging

5 mg in Plastic ampoule

Biochem/physiol Actions

Cell permeable: yes

Primary Target
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.

Safety & Documentation

Safety Information

Safety Information for this product is unavailable at this time.

Documents

Certificate of Analysis (COA)

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