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Merck

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
NACRES:
NA.77
UNSPSC Code:
12352200
Assay:
≥95% (HPLC)
Form:
lyophilized solid
Quality level:
Storage condition:
OK to freeze
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Product Name

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.

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

Quality Level

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

Disclaimer

Toxicity: Standard Handling (A)

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).

Other Notes

Cbz-Leu-NH-CH₂-CO-CH₂-NH-Leu-Cbz
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.

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Storage Class

11 - Combustible Solids

wgk

WGK 1

flash_point_f

Not applicable

flash_point_c

Not applicable


Certificates of Analysis (COA)

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