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PD98059;167869-21-8

简要描述:PD98059是一种非ATP竞争性的MEK抑制剂,无细胞试验中IC50为2 μM,特异性抑制MEK-1介导的MAPK激活;不直接抑制ERK1或ERK2。PD98059不会抑制已经被c-Raf磷酸化的 MEK1。

  • 产品型号:abs810010
  • 厂商性质:生产厂家
  • 更新时间:2024-03-03
  • 访  问  量:962

详细介绍

品牌absinCAS167869-21-8
分子式C16H13NO3纯度>98 %
分子量267.28货号abs810010
规格5mg;10mg;50mg供货周期现货
主要用途-应用领域化工,生物产业,综合
产品描述
描述

PD98059是一种非ATP竞争性的MEK抑制剂,无细胞试验中IC50为2 μM,特异性抑制MEK-1介导的MAPK激活;不直接抑制ERK1或ERK2。PD98059不会抑制已经被c-Raf磷酸化的 MEK1。

纯度
>98%
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
基本信息
别名
PD-98059,PD98059
外观
Lyophilized powder
可溶性/溶解性
DMSO:14 mg/mL warmed (52.37 mM)
生物活性
靶点
MEK1
In vitro(体外研究)
PD98059 inhibits either basal MEK1 or a partially activated MEK produced by mutation of serine at residues 218 and 222 to glutamate (MEK-2E) with IC50 of 2 μM. PD98059 does not inhibit the MAPK homologues JNK and P38. PD98059 is highly selective against MEK, as it does not inhibit a number of other kinase activities including Raf kinase, cAMP-dependent kinase, protein kinase C, v-Src, epidermal growth factor (EGF) receptor kinase, insulin receptor kinase, PDGF receptor kinase, and phosphatidylinositol 3-kinase. PD98059 inhibits PDGF-stimulated activation of MAPK and thymidine incorporation into 3T3 cells with IC50 of ~10 μM and ~7 μM, respectively. PD98059 potently prevents the activation of MEK1 by Raf or MEK kinase with IC50 of 4 μM, and weakly inhibits the activation of MEK2 by Raf with IC50 of 50 μM. PD98059 does not inhibit the activation of MEK homologues MKK4 and RK kinase that participate in stress and interleukin-1-stimulated kinase cascades in KB and PC12 cells, and the activation of p70 S6 kinase by insulin or epidermal growth factor in Swiss 3T3 cells. PD98059 completely blocks the nerve growth factor (NGF)-induced differentiation of PC12 cells without altering cell viability. PD98059 inhibits the proliferation of RAW264.7 cells in the culture containing RANKL in a dose-dependent manner, resulting in an apparent decrease of TRAP-positive cells.
In vivo(体内研究)
Treatment of mice 30 minutes before focal cerebral ischemia with PD98059 protects against damage, resulting in a decrease in infarct volume. Pretreated with PD98059 (10 mg/kg per i.v. injection) 30 minutes before and then together with hourly cerulein injections for 3 hours significantly ameliorates cerulein-induced acute pancreatitis ipancreatitis on the basis of pancreatic wet weight and histology. Administration of PD98059 (10 mg/kg) in mice 1 hour after carrageenan causes a reduction in all the parameters of inflammation measured.
参考文献
参考文献
[1] Dudley DT, et al. Proc Natl Acad Sci U S A, 1995, 92(17), 7686-7689.
[2] Alessi DR, et al. J Biol Chem, 1995, 270(46), 27489-27494.
[3] Pang L, et al. J Biol Chem, 1995, 270(23), 13585-13588.
分子结构图

温馨提示:本产品仅作科研实验使用,不支持临床等研究


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