半岛bd体育手机客户端 说明
一般描述
A cell-permeable nitroindolo-guanidinohydrazone compound that acts as a potent, ATP-competitive, and highly selective Chk2 inhibitor (IC50= 138 and 570 nM against the phosphorylation of histone H1 by Chk2 in the presence of 10 ?M and 1 mM of ATP, respectively), while exhibiting much reduced or no activity against a panel of 52 other cellular kinases, including Chk1 (IC50= 15.73 and 55 ?M against substrate phosphorylation and Chk1 autophosphorylation with 10 ?M ATP). Shown to effectively suppress radiation-induced phosphorylation of Chk2 (on Ser516) and its downstream substrate Cdc25c (on Ser216) in MCF7 cultures (IC50<10 ?M) and reduce the sensitivity of wild-type murine thymocytes to radiation-induced apoptosis to the level seen in Chk2-/-cultures.
A cell-permeable nitroindolo-guanidinohydrazone compound that acts as a potent, ATP-competitive, and highly selective Chk2 inhibitor (IC50= 138 and 570 nM against the phosphorylation of histone H1 by Chk2 in the presence of 10 ?M and 1 mM of ATP, respectively), while exhibiting much reduced or no activity against a panel of 52 other cellular kinases, including Chk1 (IC50= 15.73 and 55 ?M against substrate phosphorylation and Chk1 autophosphorylation with 10 ?M ATP). Shown to effectively suppress radiation-induced phosphorylation of Chk2 (on Ser516) and its downstream substrate Cdc25c (on Ser216) in MCF7 cultures (IC50<10 ?M) and reduce the sensitivity of wild-type murine thymocytes to radiation-induced apoptosis to the level seen in Chk2-/-cultures.
包装
10 mg in Glass bottle
Packaged under inert gas
警告
Toxicity: Standard Handling (A)
重悬
Following reconstitution, aliqout and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
其他说明
Jobson, A.G., et al. 2009.J. Pharmacol. Exp. Ther.331,816.
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 | C18H17N7O3 |
分子量 | 379.37 |
半岛bd体育手机客户端 性质
质量水平 | 100 |
测定 | ≥95% (HPLC) |
形式 | solid |
manufacturer/tradename | Calbiochem? |
储存条件 | OK to freeze desiccated (hygroscopic) protect from light |
颜色 | orange |
溶解性 | DMSO: 5 mg/mL |
运输 | ambient |
储存温度 | ?20℃ |
安全信息
储存分类代码 | 11 - Combustible Solids |
WGK | WGK 3 |
闪点(F) | Not applicable |
闪点(C) | Not applicable |
Sigma-Aldrich