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IKK Inhibitor III, BMS-345541-CAS 445430-58-0-Calbiochem
| 产品编号： | 4061693 |
| 规格： | IKK Inhibitor III, BMS-345541, CAS 445430-58-0, is a cell-permeable, potent, selective, and allosteric site-binding inhibitor of IKK-2 (IC50 = ~ 300 nM). |
| CAS NO： | 445430-58-0 |
| 包装规格： | 1 MG |
| 产品类别： | 进口试剂 |
| 品牌： | Sigma-Aldrich |
| 优惠价： | 立即咨询 |
产品别名
445430-58-0
IKK Inhibitor III, BMS-345541-CAS 445430-58-0-Calbiochem
4-(2'-Aminoethyl)amino-1,8-dimethylimidazo[1,2-a]quinoxaline
基本信息
| Empirical Formula【经验(实验)分子式】 | C14H17N5 · 2C2HF3O2 |
| Molecular weight | 483.36 |
| General description【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 µM) and no activity towards IKKε and a panel of more than 15 unrelated protein kinases even at concentrations as high as 100 µM. Inhibits cellular IκBα phosphorylation (IC50 = 4 µM in THP-1 cells) and LPS-induced cytokine production both in vitro (IC50 = 1-5 µM in THP-1 cells) and in 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 µM) and does not inhibit IKKε and a panel of more than 15 unrelated protein kinases even at concentrations as high as 100 µM. Inhibits cellular IκBα phosphorylation (IC50 = 4 µM in THP-1 cells) and LPS-induced cytokine production both in vitro (IC50 = 1-5 µM in THP-1 cells) and in vivo (IC50 = 10 mg/kg in mice). Effectively blocks inflammation and joint destruction in a murine arthritis model. |
| Biochem/physiol Actions【生化/生理作用】 | Cell permeable: yes Target IC50: ~300 nM against IKK-2; 4 µM against cellular IκBα phosphorylation in THP-1 cells; 1-5 µM LPS-induced cytokine production in THP-1 cells Product does not compete with ATP. Reversible: no |
| Warning【警告】 | Toxicity: Standard Handling (A) |
| Physical form【外形】 | Supplied as bis-TFA salt. |
| Other Notes【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. |
| Legal Information【法律信息】 | CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany |
产品性质
| Quality Level【质量水平】 | 100 |
| Assay【测定】 | ≥96% (HPLC) |
| form【形式】 | solid |
| manufacturer/tradename | Calbiochem® |
| storage condition【储存条件】 | OK to freeze desiccated (hygroscopic) protect from light |
| color【颜色】 | off-white |
| solubility【溶解性】 | DMSO: 5 mg/mL |
| shipped in【运输】 | ambient |
| storage temp.【储存温度】 | 2-8℃ |
| packaging【包装】 | 1 mg in Plastic ampoule Packaged under inert gas |
安全信息
| Storage Class Code【储存分类代码】 | 11 - Combustible Solids |
| WGK | WGK 1 |
