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U-0126
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
U-0126图片
CAS NO:109511-58-2
包装与价格：
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议

产品介绍
U-0126 是一种有效的、非 ATP 竞争性和选择性的 MEK1 和 MEK2 抑制剂，IC50 分别为 72 nM 和 58 nM。 U-0126 是一种自噬和线粒体自噬抑制剂。
Cas No.109511-58-2
别名1,4-二氨基-2,3-二氰基-1,4-双(邻氨基苯巯基)丁二烯
化学名2,3-bis[amino[(2-aminophenyl)thio]methylene]-butanedinitrile
Canonical SMILESN/C(SC1=CC=CC=C1N)=C(C#N)\C(C#N)=C(N)\SC2=C(N)C=CC=C2
分子式C18H16N6S2
分子量380.5
溶解度0.5mg/mL in ethanol, 25mg/mL in DMSO, 30mg/mL in DMF
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
文献引用
产品描述

U-0126 is a MEK inhibitor with IC50 values of 72 nM and 58 nM for MEK1 and MEK2, respectively. [1] It is noncompetitive with respect adenosine triphosphate (ATP) and its phosphorylation target ERK and it shows little to no inhibition against a number of other kinases including PKC, Ab1, Raf, MEKK, ERK, JNK, MKK-3, MKK-4, MKK-6, Cdk2, and Cdk4. However, U-0126 does phosphorylate and activate AMP-activated protein kinase (AMPK) in a dose-dependent manner (EC50 = 15 &#181M in HEK293 cells).[2] It increases the ratios of ADP to ATP and AMP to ATP and increases phosphorylation of the AMPK target acetyl-CoA carboxylase (ACC).

Reference:
[1]. Favata, M.F., Horiuchi, K.Y., Manos, E.J., et al. Identification of a novel inhibitor of mitogen-activated protein kinase kinase. J. Biol. Chem. 273(29), 18623-18632 (1998).
[2]. Dokladda, K., Green, K.A., Pan, D.A., et al. PD98059 and U0126 activate AMP-activated protein kinase by increasing the cellular AMP:ATP ratio and not via inhibition of the MAP kinase pathway. FEBS Lett. 579(1), 236-240 (2005).