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Merck
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Key Documents

219377

Sigma-Aldrich

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.

别名:

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

经验公式(希尔记法):
C31H42N4O7
分子量:
582.69
分類程式碼代碼:
12352200
NACRES:
NA.77

品質等級

化驗

≥95% (HPLC)

形狀

lyophilized solid

製造商/商標名

Calbiochem®

儲存條件

OK to freeze

顏色

off-white

溶解度

methanol: 1 mg/mL
DMSO: soluble

運輸包裝

wet ice

儲存溫度

−20°C

一般說明

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).

生化/生理作用

Cell permeable: yes
Primary Target
cathepsin K
Product does not compete with ATP.
Reversible: yes
Target Ki: 22 nM against cathepsin K

包裝

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

序列

Cbz-Leu-NH-CH₂-CO-CH₂-NH-Leu-Cbz

重構

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

其他說明

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.

法律資訊

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

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 1

閃點(°F)

Not applicable

閃點(°C)

Not applicable


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