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U0126-EtOH

现货
Catalog No.
A1337
MEK1/2抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 550.00
现货
5mg
¥ 500.00
现货
25mg
¥ 1,050.00
现货
100mg
¥ 3,300.00
现货

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Background

U0126-EtOH is a selective inhibitor of MEK1 and MEK2 with IC50 values of 70 nM and 60 nM, resepctively [1].

U0126 was screened out as an anti-inflammatory agent that inhibited AP-1 transcription with IC50 value of 1μM and had no interactions with GREs. U0126 binds MEK1/2 in a unique site. This inhibition of MEK1/2 is noncompetitive with ERK and ATP. U0126 showed no effects on other MAPKKs. In HT22 cells, U0126 treatment significantly inhibited the cell injury caused by oxidative glutamate toxicity and remarkably blocked the phosphorylation of ERK1/2. Besides that, U0126 exerted no neuroprotection against other stimuli such as TNFα and actinomycin D. U0126 treatment also protected the primary cultured cortical neurons from oxidative glutamate toxicity and hypoxia/reoxygenation [1, 2].

References:
[1] Duncia J V, Santella III J B, Higley C A, et al. MEK inhibitors: the chemistry and biological activity of U0126, its analogs, and cyclization products. Bioorganic & Medicinal Chemistry Letters, 1998, 8(20): 2839-2844.
[2] Satoh T, Nakatsuka D, Watanabe Y, et al. Neuroprotection by MAPK/ERK kinase inhibition with U0126 against oxidative stress in a mouse neuronal cell line and rat primary cultured cortical neurons. Neuroscience letters, 2000, 288(2): 163-166.

文献引用

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt426.56
Cas No.1173097-76-1
FormulaC18H16N6S2.C2H6O
Solubility≥21.328mg/mL in DMSO
Chemical Name(2Z,3Z)-2,3-bis[amino-(2-aminophenyl)sulfanylmethylidene]butanedinitrile;ethanol
SDFDownload SDF
Canonical SMILESCCO.C1=CC=C(C(=C1)N)SC(=C(C#N)C(=C(N)SC2=CC=CC=C2N)C#N)N
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

HT22细胞

溶解方法

该化合物在DMSO中的溶解度大于10 mM。若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月。

反应条件

10 μM, 24小时

实验结果

使用含或不含不同浓度抑制剂的5mM谷氨酸溶液处理细胞,处理后24小时,通过MTT测定法测定HT22细胞的活力。结果表明,U0126以剂量依赖性方式抑制谷氨酸毒性引起的细胞死亡。10 μM的U0126可以特异性抑制MEK1/2,在此浓度下,U0126可以完全抑制细胞损伤。

动物实验[2]:

动物模型

雄性BALB/c 小鼠

剂量

腹腔注射,7.5、15和30 mg/kg

实验结果

通过腹腔注射20μg OVA和4mg的Al(OH)3使小鼠致敏。在最后一次OVA气溶胶攻击后24小时收集BAL液。与PEG对照相比,U0126(7.5、15和30 mg/kg)显著降低了BAL液中回收的总细胞数,这主要是由于U0126以剂量依赖性的方式显著减少嗜酸性粒细胞的数量。在用盐水气雾剂造成的致敏小鼠中,U0126对BAL液体中的细胞计数没有产生任何抑制作用。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。

References:

[1] Satoh T, Nakatsuka D, Watanabe Y, et al. Neuroprotection by MAPK/ERK kinase inhibition with U0126 against oxidative stress in a mouse neuronal cell line and rat primary cultured cortical neurons. Neuroscience letters, 2000, 288(2): 163-166.

[2] Duan W, Chan J H P, Wong C H, et al. Anti-inflammatory effects of mitogen-activated protein kinase kinase inhibitor U0126 in an asthma mouse model. The Journal of Immunology, 2004, 172(11): 7053-7059.

生物活性

描述 U0126-EtOH是一种高选择性的MEK1/2抑制剂,IC50值为0.07 μM/0.06 μM,对ΔN3-S218E/S222D MEK的亲和性比PD98059高100倍。
靶点 MEK1 MEK2        
IC50 0.07 μM 0.06 μM        

质量控制

质量控制和MSDS

批次:

化学结构

U0126-EtOH

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