半岛bd体育手机客户端 说明
一般描述
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 ?M) but displays greater selectivity towards other proteases of the papain family (Ki,app= 340 nM, 890 nM, and 1.3 ?M for cathepsin L, cathepsin S, and cathepsin B respectively). Inhibits trypsin and chymotrypsin activities only at higher concentrations (Ki,app≥ 50 ?M).
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 ?M), trypsin (Ki>50 ?M), and chymotrypsin (Ki>50 ?M) only at higher concentrations. Exhibits greater selectivity for cysteine proteases of the papain family (Ki= 340 nM, 890 nM, and 1-3 ?M for cathepsin L, cathepsin S, and cathepsin B, respectively).
包装
5 mg in Plastic ampoule
Packaged under inert gas
生化/生理作用
Primary Target
cathepsin K
Product does not compete with ATP.
Reversible: yes
Cell permeable: yes
Target Ki: 22 nM against cathepsin K
警告
Toxicity: Standard Handling (A)
序列
Cbz-Leu-NH-CH?-CO-CH?-NH-Leu-Cbz
重悬
Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
其他说明
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.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
基本信息
经验(实验)分子式 | C31H42N4O7 |
分子量 | 582.69 |
半岛bd体育手机客户端 性质
质量水平 | 100 |
测定 | ≥95% (HPLC) |
形式 | lyophilized solid |
manufacturer/tradename | Calbiochem? |
储存条件 | OK to freeze |
颜色 | off-white |
溶解性 | methanol: 1 mg/mL DMSO: soluble |
运输 | wet ice |
储存温度 | ?20℃ |
安全信息
储存分类代码 | 11 - Combustible Solids |
WGK | WGK 1 |
闪点(F) | Not applicable |
闪点(C) | Not applicable |
Sigma-Aldrich