半岛bd体育手机客户端 说明
一般描述
A cell-permeable quinoxaline compound that displays anti-inflammatory properties. Acts as a potent, selective, and allosteric site-binding inhibitor of IKK-2 (IC50= ~ 300 nM). Exhibits ~10-fold greater selectivity over IKK-1 (IC50= ~ 4 ?M) and no activity towards IKKε and a panel of more than 15 unrelated protein kinases even at concentrations as high as 100 ?M. Inhibits cellular IκBα phosphorylation (IC50= 4 ?M in THP-1 cells) and LPS-induced cytokine production bothin vitro(IC50= 1-5 ?M in THP-1 cells) andin vivo(IC50= 10 mg/kg in mice). Effectively blocks inflammation and joint destruction in a murine arthritis model.
A cell-permeable, potent, selective, and allosteric site-binding inhibitor of IKK-2 (IC50~300 nM) that displays anti-inflammatory properties. Exhibits ~10-fold greater selectivity for IKK-2 over IKK-1 (IC50~4.0 ?M) and does not inhibit IKKε and a panel of more than 15 unrelated protein kinases even at concentrations as high as 100 ?M. Inhibits cellular IκBα phosphorylation (IC50= 4 ?M in THP-1 cells) and LPS-induced cytokine production bothin vitro(IC50= 1-5 ?M in THP-1 cells) andin vivo(IC50= 10 mg/kg in mice). Effectively blocks inflammation and joint destruction in a murine arthritis model.
包装
1 mg in Plastic ampoule
Packaged under inert gas
生化/生理作用
Cell permeable: yes
Target IC50: ~300 nM against IKK-2; 4 ?M against cellular IκBα phosphorylation in THP-1 cells; 1-5 ?M LPS-induced cytokine production in THP-1 cells
Product does not compete with ATP.
Reversible: no
警告
Toxicity: Standard Handling (A)
外形
Supplied as bis-TFA salt.
其他说明
Townsend, R.M., et al. 2004.Transplantation77,1090.
MacMaster, J.F., et al. 2003.Inflamm. Res.52,508.
McIntyre, K.W., et al. 2003.Arthritis Rheum.48,2652.
Burke, J. R., et al. 2003.J. Biol. Chem.278,1450.
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 | C14H17N5· 2C2HF3O2 |
| 分子量 | 483.36 |
半岛bd体育手机客户端 性质
| 质量水平 | 100 |
| 测定 | ≥96% (HPLC) |
| 形式 | solid |
| manufacturer/tradename | Calbiochem? |
| 储存条件 | OK to freeze desiccated (hygroscopic) protect from light |
| 颜色 | off-white |
| 溶解性 | DMSO: 5 mg/mL |
| 运输 | ambient |
| 储存温度 | 2-8℃ |
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
m.cnreagent.com
