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• 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。

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *