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品質等級
化驗
≥98% (HPLC)
形狀
powder
儲存條件
protect from light
顏色
white to off-white
溶解度
DMSO: >10 mg/mL (Stock solutions in DMSO should be used within a month. Acidic solutions exhibit weaker inhibition)
儲存溫度
2-8°C
SMILES 字串
N#CC(C(C#N)=C(N)SC1=C(N)C=CC=C1)=C(N)SC2=C(N)C=CC=C2.CCO
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
InChI 密鑰
CFQULUVMLGZVAF-UHFFFAOYSA-N
基因資訊
human ... MAP2K1(5604) , MAP2K2(5605)
應用
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。
生化/生理作用
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。
特點和優勢
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。
注意
光敏感的
準備報告
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。
儲存類別代碼
11 - Combustible Solids
水污染物質分類(WGK)
WGK 3
閃點(°F)
Not applicable
閃點(°C)
Not applicable
個人防護裝備
Eyeshields, Gloves, type N95 (US)
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