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CAS No.: 1173097-76-1

2,3-Bis(amino((2-aminophenyl)thio)methylene)succinonitrile compound with ethanol (1:1) Catalog No. CSN12171

Synonyms: CCG-268966;U-0126

U0126 ethanol is a highly selective inhibitor of MEK1/2 with IC50 of 0.07 μM/0.06 μM.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 MEK1

IC50:0.07μM MEK2

IC50:0.06μM
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.. U0126 is a selective MEK1/2 inhibitor with IC50 value of 70/60nM, but not ERK or Raf^[1]^[2]. Co-treatment with U0126 for 15min at concentration ranging in 1nM-10μM caused inhibition of PMA-induced p-ERK, the target of MEK1/2 in a dose-dependent manner in COS-7 cells. An in vitro study showed that U0126 represented much more potency to both wild type and ΔN3-S218E/S222D MEK compared with the another MEK1/2 inhibitor, PD98059^[2]. An in vivo study showed that U0126 is brain-permeable. Intravenous injection with U0126 at dose of 100mg/kg could reduce p-ERK1/2 in hippocampus after 10 min of reperfusion after 3.5 min bilateral carotid artery occlusion in male gerbils. Intravenous administration of U0126 at dose of 100-200mg/kg showed protective effect on the hippocampus against forebrain ischemia in male gerbils. Moreover, treatment with U0126 at 3 hours post ischemia significantly reduced volume after transient focal cerebral ischemia, accompanied with reduced p-ERK in the damaged brain areas^[3]. Also, it has been reported that U0126 helped maintain human pluripotent stem cells^[4].
作用机制U0126 is a non-competitive inhibitor of MEK1/2, which can bind a common or two overlapping sites on MEK.^[2]
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
COS-7 cells	-	Function assay	-	Inhibitory concentration against AP-1 transcription in COS-7 cells， IC50=1 μM.	15006386
HCT116 cells	-	Function assay	-	Ability of compound to inhibit anchorage independent colony formation (soft agar growth assay) in HCT116 cells, IC50=19.4 μM.	15225706
HeLa cells	-	Function assay	-	Inhibition of EGF-stimulated Elk1-luciferase reporter assay in HeLa cells, IC50=0.29 μM.	15225706

更多
动物研究
剂量
Mice: 30 mg/kg^[7] (p.o.) Rat: 30 mg/kg^[8] (i.p.), 30 mg/kg^[9] (s.c.)

给药途径
p.o., i.p., s.c.
参考文献

动物研究
剂量	Mice: 30 mg/kg^[7] (p.o.) Rat: 30 mg/kg^[8] (i.p.), 30 mg/kg^[9] (s.c.)
给药途径	p.o., i.p., s.c.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.6282 mL
- 13.1409 mL
- 26.2819 mL
- 5 mM
- 0.5256 mL
- 2.6282 mL
- 5.2564 mL
- 10 mM
- 0.2628 mL
- 1.3141 mL
- 2.6282 mL

技术信息

CAS号

1173097-76-1

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H22N6OS2

运输

蓝冰

分子量

426.56

别名

CCG-268966;U-0126

溶解度

DMSO	300.0 mg/mL (703.3 mM)
Water	insoluble

动物实验配方

IP	2% DMSO+2% Tween80+40% PEG300+water	6 mg/mL	clear
PO	0.5% CMC-Na	35 mg/mL	suspension

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靶点	Description	IC50
MEK1		IC50:0.07μM
MEK2		IC50:0.06μM

2,3-Bis(amino((2-aminophenyl)thio)methylene)succinonitrile compound with ethanol (1:1) Catalog No. CSN12171

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