CAS:167869-21-8PD98059

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PD98059 2-(2-氨基-3-甲氧基苯基)-4H-1-苯并吡喃-4-酮 Cat No. FB08037Cas No. 167869-21-8

PD98059 is a non-ATP competitive MEK inhibitor with IC50 of 2 μM, specifically inhibits MEK-1-mediated activation of MAPK and does not directly inhibit ERK1 or ERK2.

规格	价格	促销价格	库存

18817579266

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18817579266

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实验数据

储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.7414 mL
- 18.7070 mL
- 37.4139 mL
- 5 mM
- 0.7483 mL
- 3.7414 mL
- 7.4828 mL
- 10 mM
- 0.3741 mL
- 1.8707 mL
- 3.7414 mL
计算器摩尔计算器总药量计算器工作液计算器

技术信息

CAS号

167869-21-8

储存条件

粉末: -20°C 3 年

液体: -80°C 12 月

分子式

C16H13NO3

运输

蓝冰

分子量

267.28

别名

溶解度

DMSO	25.0 mg/mL (93.5 mM) warming
Water	insoluble

动物实验配方

IP	2% DMSO+2% Tween80+30% PEG300+water	0.5 mg/mL	clear
PO	0.5% CMC-Na	20 mg/mL	suspension

靶点数据

生物活性

靶点 MEK

IC50:2μM
描述MEKs, which are members of the MAPKK family, can activate both ERK1 and ERK2 by catalyzing the phosphorylation on T202/Y204. Also MEK itself can be phosphorylated and activated through Ras when the upstream signaling is activated by extracellular stimuli, including growth factors, hormones etc.. PD98059 is MEK1/2-specific inhibitor with IC50=~10uM (measured by phosphorylation level of MAPK-KA catalyzed by GST-MEK1) with no effect on ERK. Pre-incubation of PD98059 can inhibit PDGF-stimulated tyrosine phosphorylation of MAPK while preventing thymidine incorporation with an IC50 of 7 uM in 3T3 cells. PD98059 did not show significant inhibitory activity on Raf kinase, cAMP-dependent kinase, protein kinase C, v-Src, EGF receptor kinase, insulin receptor kinase, PDGFreceptor kinase, and PI3Ks, which shows the high selectivity of it ^[1]. PD98059 is the first generation small molecule inhibitors of MEK1/2. PD98059 does not interfere with Raf access to MEK1/2 for it did not affect serum-induced MEK1/2 phosphorylation ^[2].
作用机制PD 098059 does not complete for ATP binding or MAPK binding to MEK and most likely inhibits through an allosteric mechanism.^[1]
动物研究
剂量
Mice: 10 mg/kg^[3]

给药途径
i.v.

动物研究
剂量	Mice: 10 mg/kg^[3]
给药途径	i.v.