PD 98059

    • 货号:MC0260
      • CasNo:
      • 167869-21-8
      • 分子式:
      • C16H13NO3
      • 纯度:
      • >98%
      • 靶点:
      • MEK
      • IC50:
      • IC50: 5 μM (MEK)[1]
      • 体外研究:
      • Concentrations of PD98059 of ≤20 μM are not cytotoxic to cultured MCF10A, MCF10A-Neo, and MCF10A-NeoT cells. However, PD98059 is weakly cytostatic to all three lines at concentrations of ≥10 μM. Treatment of MCF10A-Neo and MCF10A-NeoT cultures with concentrations of PD98059 up to 20 μM for 2-22 hr does not alter the total ERK content. However, treatment with PD98059 does result in concentration-dependent reductions in the dually phosphorylated forms of ERK1 and ERK2. Within 2 hr of a 10-μM treatment, phosphorylated ERK contents are reduced ~74% and ~86% in MCF10A-Neo and MCF10A-NeoT cultures, respectively (IC50=1 μM). Within 22 hr of treatment, phosphorylated ERK forms are almost completely eliminated in both cell lines[1]. PD98059 (PD 098059) prevents the activation of MAPKK1 by Raf or MEK kinase in vitro at concentrations (IC50=2-7 μM). PD98059 inhibits both the activation and phosphorylation of MAPKK1 in vitro by either c-Raf or MEK kinase with IC50 values of 4±2 μM. Incubation of S
      • 体内研究:
      • The treatment of mice with PD98059 significantly reduces the level of p-ERK1/2. Moreover, a significant increase in the phospho-p38 expression is observed in Zymosan-treated mice at 18 h after Zymosan administration compared to the sham-operated mice. The treatment with PD98059 significantly reduces the p38 expression[3]. Repeated treatment with PD98059 attenuates mechanical allodynia measured by the von Frey test three (18.0 g±0.8, n=10) and seven (20.21 g±0.67, n=26) days after CCI in comparison to the vehicle-treated CCI-exposed rats (15.1 g±1.3, n=7 and 14.21 g±0.44, n=28, respectively). Repeated injection of PD98059 diminishes thermal hyperalgesia, as is evaluated by the cold plate test, three (17.5 s±2.1, n=10) and seven (25.54 s±1.03, n=26) days following CCI compared to vehicle-treated CCI-exposed rats (11.5 s±1.8, n=7 and 11.4 s±0.88, n=28, respectively)[4].
      • 简介:
      • PD 98059 is a selective inhibitor of MEK and blocker of MAPK IC50: 5 μM (MEK)[1]
      • 特异性:
      • Target: MEK. Fields: PD 98059 is a selective inhibitor of MEK and blocker of MAPK IC50: 5 μM (MEK)[1]
      • 稀释:
      • IC50: 5 μM (MEK)[1]
      • 浓度:
      • >98%
      • 储存:
      • 2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO
      • 其他名称:
      • PD-98059,PD98059
      • 分子量:
      • 267.28
      • 产品图片