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• 产品描述： Ro 31-8220 mesylate is a potent PKC inhibitor, with IC50s of 5, 24, 14, 27, 24 and 23 nM for PKCα, PKCβI, PKCβII, PKCγ, PKCε and rat brain PKC, respectively. Ro 31-8220 also significantly inhibits MAPKAP-K1b, MSK1, S6K1 and GSK3β (IC50s, 3, 8, 15, and 38 nM, respectively), with no effect on MKK3, MKK4, MKK6 and MKK7.

• 靶点： PKC-α:5 nM (IC50);PKC-βI:24 nM (IC50);PKC-βII:14 nM (IC50);PKC-γ:27 nM (IC50);PKC-ε:24 nM (IC50);Rat Brain PKC:23 nM (IC50);MAPKAP-K1b:3 nM (IC50);MSK1:8 nM (IC50);S6K1:15 nM (IC50);GSK3β:38 nM (IC50);PKC

• 体内研究：
  Ro 31-8220 (6 mg/kg/d, s.c.) is well tolerated, and has half-life of 5.7 hours in mice. Ro 31-8220-treated MLP−/− mice show a dramatic rescue in fractional shortening after treatment for 6 weeks, but the WT mice shows no change

• 参考文献：
  1. Wilkinson SE, et al. Isoenzyme specificity of bisindolylmaleimides, selective inhibitors of protein kinase C. Biochem J. 1993 Sep 1;294 (Pt 2):335-7. 2. Davies SP, et al. Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J. 2000 Oct 1;351(Pt 1):95-105. 3. Tian F, et al. Inhibition of protein kinase C protects against paraoxon-mediated neuronal cell death. Neurotoxicology. 2007 Jul;28(4):843-9. Epub 2007 Apr 20. 4. Hambleton M, et al. Pharmacological- and gene therapy-based inhibition of protein kinase Calpha/beta enhances cardiac contractility and attenuates heart failure. Circulation. 2006 Aug 8;114(6):574-82.

• 溶解性： DMSO  :  35.71  mg/mL  (64.50  mM;  Need  ultrasonic)    H2O  :  <  0.1  mg/mL  (insoluble)

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	1.806 ml	9.031 ml	18.062 ml
  5 mM	0.361 ml	1.806 ml	3.612 ml
  10 mM	0.181 ml	0.903 ml	1.806 ml
  50 mM	0.036 ml	0.181 ml	0.361 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 *