Home>>U0126-EtOH

U0126-EtOH

(Synonyms: 2,3-双[氨基[(2-氨基苯基)硫]亚甲基]丁二腈乙醇盐) 目录号 : GC12807

U0126 (U0126-EtOH) 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。 U0126 是一种自噬和线粒体自噬抑制剂。

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥431.00
现货
5mg
¥378.00
现货
25mg
¥809.00
现货
100mg
¥2,300.00
现货

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Sample solution is provided at 25 µL, 10mM.

文献引用

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Quality Control & SDS

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实验参考方法

Cell experiment [1]:

Cell lines

Fibroblast-like synoviocytes(FLSs)

Preparation Method

FLSs were plated at a density of 5 × 104 mL−1 in 6-well plates for 24 h. FLSs were serum starved for 24 h before incubation with Cyclopamine (10 μM) or Purmorphamine (1 μM), or co-treated with U0126-EtOH-EtOH (10 μM) Purmorphamine (1 μM). Cell counting kit-8 assay was performed to examine the cell viability.

Reaction Conditions

10 μM; 48 h

Applications

U0126-EtOH-EtOH inhibit cell viability and regulate cell cycle distribution of RA-FLSs induced by SHH signaling.

Animal experiment [2]:

Animal models

Rats

Preparation Method

Rats were subjected to 120 minutes tMCAO and thereafter treated with the MEK1/2 inhibitor U0126-EtOH (30 mg/kg intraperitoneally) at 0 and 24 hours of reperfusion.

Dosage form

30 mg/kg; i.p.

Applications

After treatment with U0126-EtOH, the vasoconstriction to S6c was markedly reduced. ET-1-induced vasoconstriction was not significantly different in non-occluded and occluded MCAs, and not affected by U0126-EtOH.

References:

[1]. Liu F, et al. Sonic Hedgehog Signaling Pathway Mediates Proliferation and Migration of Fibroblast-Like Synoviocytes in Rheumatoid Arthritis via MAPK/ERK Signaling Pathway. Front Immunol. 2018 Dec 5;9:2847.

[2]. Ahnstedt H, et al. U0126-EtOH attenuates cerebral vasoconstriction and improves long-term neurologic outcome after stroke in female rats. J Cereb Blood Flow Metab. 2015 Mar;35(3):454-60.

产品描述

U0126-EtOH-EtOH (U0126), as a non-ATP competitive and selective inhibitor, a has potent inhibition on MEK1 and MEK2 with IC50s of 72 nM and 58 nM, respectively.[1][6]

In vitro experiment it shown that treatment with 10 μM of U0126-EtOH-EtOH decreased the numbers of migration RA-FLSs induced by Sonic Hedgehog signaling. [2] In vitro, pretreatment with 50 μM SB203580 (the p38 inhibitor) and 50 μM U0126-EtOH-EtOH (ERK1/2 inhibitor) in the microglial cells obviously brogated the effects of isotalatizidine.[3] In addition, H9C2 cells pretreated with 10μM U0126-EtOH reduced ischemia/reperfusion-induced apoptosis and autophagy in myocardium and reduced cisplatin-induced renal injury by decreasing inflammation and apoptosis by inhibition of ERK1/2 phosphorylation.[4] Pretreatment with 10 μM of U0126-EtOH protected PC-12 Cells against hydrogen peroxide-induced cell death independent of MEK inhibition.[6] Moreover, at 1 μM to 20 μM of U0126-EtOH increased the half-width and decay time of action potential in a dose-dependent manner in primary hippocampal neurons. Bath application of 40 μM U0126-EtOH is more potent than 4-AP and TEA in suppressing maximal firing rate of pyramidal neurons in hippocampal slices.[5]

In vivo efficacy test it demonstrated that pretreatment with 1mg/kg U0126-EtOH in in STZ-induced diabetic mice improved cardiac function and ameliorated cardiac hypertrophy.[4] In the acute phase of experimental stroke, 30 mg/kg U0126-EtOH prevent activation of MMP-9, additionly, by adding U0126-EtOH in combination with rt-PA prevent activation of MMP-9 expression leading to BBB leakage and hemorrhagic transformation.[6]

References:
[1]. Favata MF, et al. Identification of a novel inhibitor of mitogen-activated protein kinase kinase. J Biol Chem. 1998 Jul 17;273(29):18623-32.
[2]. Liu F, et al. Sonic Hedgehog Signaling Pathway Mediates Proliferation and Migration of Fibroblast-Like Synoviocytes in Rheumatoid Arthritis via MAPK/ERK Signaling Pathway. Front Immunol. 2018 Dec 5;9:2847.
[3]. Shao S, et al. Isotalatizidine, a C19-diterpenoid alkaloid, attenuates chronic neuropathic pain through stimulating ERK/CREB signaling pathway-mediated microglial dynorphin A expression. J Neuroinflammation. 2020 Jan 10;17(1):13.
[4]. Wang T, et al. The MEK inhibitor U0126-EtOH ameliorates diabetic cardiomyopathy by restricting XBP1's phosphorylation dependent SUMOylation. Int J Biol Sci. 2021 Jul 13;17(12):2984-2999.
[5]. Orset C, et al. Combination treatment with U0126-EtOH and rt-PA prevents adverse effects of the delayed rt-PA treatment after acute ischemic stroke. Sci Rep. 2021 Jun 7;11(1):11993.
[6]. Ong Q, et al. U0126-EtOH protects cells against oxidative stress independent of its function as a MEK inhibitor. ACS Chem Neurosci. 2015 Jan 21;6(1):130-7.
[7]. Wang JZ, et al. Potent block of potassium channels by MEK inhibitor U0126-EtOH in primary cultures and brain slices. Sci Rep. 2018 Jun 11;8(1):8808.

Chemical Properties

Cas No. 1173097-76-1 SDF
别名 2,3-双[氨基[(2-氨基苯基)硫]亚甲基]丁二腈乙醇盐
化学名 (2Z,3Z)-2,3-bis[amino-(2-aminophenyl)sulfanylmethylidene]butanedinitrile;ethanol
Canonical SMILES CCO.C1=CC=C(C(=C1)N)SC(=C(C#N)C(=C(N)SC2=CC=CC=C2N)C#N)N
分子式 C18H16N6S2.C2H6O 分子量 426.56
溶解度 DMSO :(warmed with 50ºC water bath)85 mg/mL (199.27 mM) 储存条件 Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

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