U120
U0126 钛酸乙酯 单乙醇盐
≥98% (HPLC), MEK inhibitor, powder
别名:
1,4-二氨基-2,3-二氰基-1,4-双（邻-氨基苯硫醇）丁二烯钛酸乙酯 单乙醇盐
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选择尺寸
关于此项目
经验公式（希尔记法）:
C18H16N6S2 · C2H5OH
化学文摘社编号:
分子量:
426.56
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
MDL number:
产品名称
U0126 钛酸乙酯 单乙醇盐, ≥98% (HPLC), powder
SMILES string
N#CC(C(C#N)=C(N)SC1=C(N)C=CC=C1)=C(N)SC2=C(N)C=CC=C2.CCO
InChI key
CFQULUVMLGZVAF-UHFFFAOYSA-N
InChI
1S/C18H16N6S2.C2H6O/c19-9-11(17(23)25-15-7-3-1-5-13(15)21)12(10-20)18(24)26-16-8-4-2-6-14(16)22;1-2-3/h1-8H,21-24H2;3H,2H2,1H3
assay
≥98% (HPLC)
form
powder
storage condition
protect from light
color
white to off-white
solubility
DMSO: >10 mg/mL (Stock solutions in DMSO should be used within a month. Acidic solutions exhibit weaker inhibition)
storage temp.
2-8°C
Quality Level
Gene Information
human ... MAP2K1(5604), MAP2K2(5605)
Application
U0126乙醇盐已用作一种MEK抑制剂，用在鸡胚乳房肌衍生的单核肌原细胞中。U0126 也已用于研究淀粉样蛋白前体蛋白（APP）敲除（KO）小鼠神经元中的 ERK2 功能。
Biochem/physiol Actions
U0126 是 MEK1 和 MEK2（MAP 激酶激酶；MAPKK）的特异性抑制剂；还抑制 MEK 的组成型活性突变形式。
U0126，1，4-二氨基-2，3-二氰基-1，4-双[2-氨基苯硫基]丁二烯是 MEK1 和 MEK2 的高选择性抑制剂。 U0126 通过非竞争性抑制双特异性激酶 MEK，在功能上拮抗 AP-1 转录活性，MEK1的 IC50 为 72nM，MEK2 的 IC50 为 58nM。 U0126 通过同时阻断细胞外信号调节激酶（ERK）和哺乳动物雷帕霉素靶蛋白（mTOR）-p70（S6K）途径，抑制 Ki-ras 转化的大鼠成纤维细胞的贴壁依赖性生长。U0126 对 8 种人乳腺癌细胞系生长的影响表明，U0126 选择性地抑制 MDA-MB231 和HBC4 细胞的锚定非依赖性生长，这两种细胞具有组成型激活的 ERK。在许多正常细胞类型中，与基质失去接触会引发细胞凋亡，这种现象称为失巢凋亡。U0126 使得 MDA-MB231 和 HBC4 对失巢凋亡敏感，即在用 U0126 处理后，失去锚定的细胞将进入凋亡。
Disclaimer
光敏感的
Features and Benefits
该化合物是激酶磷酸酶生物学研究的特色产品。点击此处 ，查看更多激酶磷酸酶生物学精选产品。了解更多有关用于其他研究领域的生物活性小分子的信息，请访问 sigma.com/discover-bsm。
Preparation Note
U0126乙醇盐可以>10 mg/ml的浓度溶于DMSO。本产品在 DMSO 中的储备溶液应在一个月内使用。本产品的酸性溶液表现出较弱的 MEK 抑制功能。
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
Eyeshields, Gloves, type N95 (US)
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