| 产品描述： | BIX02189 is a potent and selective MEK5 inhibitor with an IC50 of 1.5 nM. BIX02189 also inhibits ERK5 catalytic activity with an IC50 of 59 nM. |
| 靶点： |
MEK5:1.5 nM (IC50);ERK5:59 nM (IC50);CSF1R (FMS):46 nM (IC50);LCK:250 nM (IC50);JAK3:440 nM (IC50);TGFβR1:580 nM (IC50);RPS6KA6 (RSK4):990 nM (IC50);RPS6KA3 (RSK2):2.1 μM (IC50);FGFR1:1 μM (IC50);KIT:1.1 μM (IC50);ABL1:2.4 μM (IC50);MAPK14 (p38 alpha):3.7 μM (IC50);SRC:7.6 μM (IC50);ERK; MEK |
| 体内研究： |
Mice are treated with either 10 mg/kg of BIX02189 (in 25% DMSO) or vehicle control (same volume of 25% DMSO) by intraperitoneal injection. The nuclear localization of Nrf2 is inhibited in aortic endothelial cells from mice treated with BIX02189 |
| 参考文献： |
1. Tatake RJ, et al. Identification of pharmacological inhibitors of the MEK5/ERK5 pathway. Biochem Biophys Res Commun. 2008 Dec 5;377(1):120-5. 2. Hwang AR, et al. Fluvastatin inhibits AGE-induced cell proliferation and migration via an ERK5-dependent Nrf2 pathway in vascular smooth muscle cells. PLoS One. 2017 May 22;12(5):e0178278. 3. Kim M, et al. Laminar flow activation of ERK5 protein in vascular endothelium leads to atheroprotective effect via NF-E2-related factor 2 (Nrf2) activation. J Biol Chem. 2012 Nov 23;287(48):40722-31. |
| 溶解性： |
DMSO : ≥ 49.4 mg/mL (112.14 mM) |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.27 ml |
11.35 ml |
22.699 ml |
| 5 mM |
0.454 ml |
2.27 ml |
4.54 ml |
| 10 mM |
0.227 ml |
1.135 ml |
2.27 ml |
| 50 mM |
0.045 ml |
0.227 ml |
0.454 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。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京