| 产品描述: | Bay 65-1942 hydrochloride is an ATP-competitive and selective IKKβ inhibitor. |
| 靶点: |
IKKβ;IκB/IKK |
| 体内研究: |
Inhibitors of MEK (AZD6244) and IKK (BAY 65-1942) are used at their IC50 concentrations, as determined by a 48 hour MTS assay, which achieve sufficient inhibition of kinase activity. MYL-R cells are treated for 24 hours with AZD6244 (5 µM), BAY 65-1942 (10 µM), or a combination of these inhibitors at the same concentrations. AZD6244 and BAY 65-1942 demonstrate synergistic inhibition of cell viability at the dose combination (5 µM AZD6244+10 µM BAY 65-1942), which correlates with IC75 (CI = 0.48±0.01). Synergism is also indicated at the IC50 (CI = 0.56±0.09) and IC90 (CI = 0.46±0.02) dose combinations reported by the software (CI values are the mean of three independent experiments, ± standard deviation). AZD6244 and BAY 65-1942 treatment induces 2- and 1.3-fold caspase 3/7 activation, respectively, compared to the DMSO-treated cells. Treatment with a combination of AZD6244 plus BAY 65-1942 leads to a 3.2-fold increase in caspase 3/7 activity |
| 参考文献: |
1. Inhibition of IκB kinase-β protects dopamine neurons against lipopolysaccharide-induced neurotoxicity By Zhang, Feng; Qian, Li; Flood, Patrick M.; Shi, Jing-Shan; Hong, Jau-Shyong; Gao, Hui-Ming J Pharmacol Exp Ther. 2010 June; 333(3): 822-833. 2. Cooper MJ, et al. Application of multiplexed kinase inhibitor beads to study kinome adaptations in drug-resistant leukemia. PLoS One. 2013 Jun 24;8(6):e66755. |
| 溶解性: |
Soluble in DMSO、H2O |
| 保存条件: |
2-8℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.315 ml |
11.576 ml |
23.153 ml |
| 5 mM |
0.463 ml |
2.315 ml |
4.631 ml |
| 10 mM |
0.232 ml |
1.158 ml |
2.315 ml |
| 50 mM |
0.046 ml |
0.232 ml |
0.463 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |