Ro 31-8220 Mesylate

    
99%

Ro 31-8220 Mesylate

源叶(MedMol)
S80315 一键复制产品信息
138489-18-6
C25H23N5O2S·CH4O3S
553.65
双吲哚马来酰亚胺 IX 甲烷磺酸盐
货号 规格 价格 上海 北京 武汉 南京 购买数量
S80315-5mg 99% ¥240.00 5 - - -
S80315-10mg 99% ¥340.00 6 - - -
S80315-50mg 99% ¥800.00 2 - - -
产品介绍 参考文献 质检证书(COA) 摩尔浓度计算器 相关产品

产品介绍

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.

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
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