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U0126-EtOH

U0126-EtOH

产品编号 T6223   CAS 1173097-76-1
别名: U0126 Ethanol, U0126

U0126-EtOH (U0126 Ethanol) 是一种非 ATP 竞争性的选择性MEK1和MEK2抑制剂,IC50分别为 72 nM 和 58 nM。U0126-EtOH 可抑制自噬和线粒体自噬

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U0126-EtOH Chemical Structure
U0126-EtOH, CAS 1173097-76-1
规格 价格/CNY 货期 数量
1 mg ¥ 167 现货
5 mg ¥ 383 现货
10 mg ¥ 617 现货
25 mg ¥ 995 现货
50 mg ¥ 1,730 现货
100 mg ¥ 2,860 现货
200 mg ¥ 4,180 现货
500 mg ¥ 6,570 现货
1 mL * 10 mM (in DMSO) ¥ 417 现货
其他形式的 U0126-EtOH:
产品目录号及名称: U0126-EtOH (T6223)
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选择批次  
纯度: 99.82%
纯度: 99.72%
纯度: 98.65%
更多批次查询请联系客服
生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 U0126-EtOH (U0126 Ethanol) is a non-ATP competitive specific inhibitor of MEK1/2 (IC50: 0.07/0.06 μM).
靶点活性 MEK2:60 nM (cell free), MEK1:70 nM (cell free)
体外活性 U0126 antagonized AP-1 transcriptional activity via noncompetitive inhibition of the dual specificity kinase MEK with an IC50 of 0.07 microM for MEK 1 and 0.06 microM for MEK 2 [1]. In fibroblasts treated with TPA/serum, U0126 suppressed the up-regulation of c-Fos and c-Jun proteins by 50–80%. Treatment with 10 μM U0126 did not affect the protein levels of the constitutively expressed transcription factors SP-1 or JunD and Fra-1 [2]. U0126 caused phosphorylation and activation of AMPK) and increased phosphorylation of its downstream target acetyl-CoA carboxylase, in HEK293 cells. This effect only occurred in cells expressing the upstream kinase, LKB1 [3].
体内活性 Treatment of mice with U0126 via the aerosol route led to (i) inhibition of MEK activation in the lung (ii) reduction of progeny IAV titers compared to untreated controls (iii) protection of IAV infected mice against a 100× lethal viral challenge [4]. In all U0126 (10.5 mg/kg) experiments, engraftment and early tumor growth were significantly decreased. Furthermore, a 60–70% reduction in the volume of tumors treated with U0126 was obtained 9 days after injection and thereafter. Cdk1 expression was also strongly reduced in U0126-treated mice [5].
激酶实验 The amount of immunoprecipitated wild type MEK used in these assays was adjusted to give a similar amount of activity units as obtained with 10 nM recombinant MEK. All other assays were performed with a recombinant, constitutively activated mutant MEK-1 (ΔN3-S218E/S222D) or constitutively active MEK-2(S222E/S226D). Reaction velocities were measured using a 96-well nitrocellulose filter apparatus as described below. Unless otherwise noted, reactions were carried out at an enzyme concentration of 10 nM, in 20 mM Hepes, 10 mM MgCl2, 5 mM β-mercaptoethanol, 0.1 mg/ml BSA, pH 7.4, at room temperature. Reactions were initiated by the addition of [γ-33P]ATP into the premixed MEK/ERK/inhibitor reaction mixture, and an aliquot of 100 μl was taken every 6 min and transferred to the 96-well nitrocellulose membrane plate which had 50 mM EDTA to stop the reaction. The membrane plate was drawn and washed 4 times with buffer under vacuum. Wells were then filled with 30 μl of Microscint-20 scintillation fluid, and the radioactivity of33P-phosphorylated ERK was counted with a Top Count scintillation counter. Velocities were obtained from the slopes of radioactivity versus time plots. Concentrations of ERK and ATP were 400 nM and 40 μM, respectively, unless otherwise indicated [2].
细胞实验 HEK293 cells were maintained in Dulbecco's modification of Eagle's medium (low glucose) plus 10% foetal bovine serum. HeLa cells stably expressing wild type or kinase-dead LKB1 have been described. AMPK activity was determined by immunoprecipitate kinase assays using anti-AMPK-a1 and -a2 antibodies. Antibodies recognising AMPK phosphorylated on Thr-172 (anti-pT172), AMPK-α1 and -α2 and acetyl-CoA carboxylase-1 (ACC1) phosphorylated on Ser-80 [16] were described previously. Quantification of ratios of signals from phosphorylated and total protein using these antibodies was performed by dual labelling using the LI-COR Odyssey IR imager as described. Contents of ATP and ADP were determined for cells in 6 cm culture dishes by quickly pouring off the medium, adding 350 μl of ice-cold 5% perchloric acid, scraping the cells off with a plastic scraper, and centrifuging (14 000 · g; 3 min, 4 °C) to remove insoluble material. The perchloric acid was then extracted from the supernatant and nucleotides analysed by capillary electrophoresis of perchloric acid extracts as described previously. All incubations of cells were performed in triplicate and results are expressed as means ± S.E.M [3].
动物实验 Prior to injection, FI cells were labeled with a stable fluorescent dye molecule, DiA at 10 μg/ml for 5 h at 37 1C. After washing to remove free DiA, cells were trypsinized for inoculation (U0126 experiments) or transfection (RNAi experiments). Biliary epithelial cells were injected subcutaneously, at the indicated times, into the tibia of nude mice. In the chemical experiments, 3h after inoculation, mice were treated with U0126 (10.5 mg/kg) daily by intraperitoneal injection. The length and width of each tumor were measured every day by using a caliper. The following formula was used to calculate tumor volumes ? width2 length/2. Mice were killed at the end of experiment. Tumors were immediately frozen in liquid nitrogen [5].
别名 U0126 Ethanol, U0126
分子量 426.6
分子式 C18H16N6S2·C2H6O
CAS No. 1173097-76-1

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 79 mg/mL (185.2 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3441 mL 11.7206 mL 23.4412 mL 58.6029 mL
5 mM 0.4688 mL 2.3441 mL 4.6882 mL 11.7206 mL
10 mM 0.2344 mL 1.1721 mL 2.3441 mL 5.8603 mL
20 mM 0.1172 mL 0.586 mL 1.1721 mL 2.9301 mL
50 mM 0.0469 mL 0.2344 mL 0.4688 mL 1.1721 mL
100 mM 0.0234 mL 0.1172 mL 0.2344 mL 0.586 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Duncia JV, et al. MEK inhibitors: the chemistry and biological activity of U0126, its analogs, and cyclization products. Bioorg Med Chem Lett. 1998, 8(20), 2839-2844. 2. 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. 3. Dokladda K, 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. 2005 Jan 3;579(1):236-40. 4. Droebner K, et al. Antiviral activity of the MEK-inhibitor U0126 against pandemic H1N1v and highly pathogenic avian influenza virus in vitro and in vivo. Antiviral Res. 2011 Nov;92(2):195-203. 5. Bessard A, et al. RNAi-mediated ERK2 knockdown inhibits growth of tumor cells in vitro and in vivo. Oncogene. 2008 Sep 11;27(40):5315-25. 6. Ahnstedt H, et al. U0126 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. 7. Zeng H, Pathak J L, Shi Y, et al. Indirect selective laser sintering-printed microporous biphasic calcium phosphate scaffold promotes endogenous bone regeneration via activation of ERK1/2 signaling[J]. Biofabrication. 2020, 12(2): 025032. 8. Shao S, Xia H, Hu M, et al. Isotalatizidine, a C 19-diterpenoid alkaloid, attenuates chronic neuropathic pain through stimulating ERK/CREB signaling pathway-mediated microglial dynorphin A expression[J]. Journal of Neuroinflammation. 2020, 17(1): 1-11. 9. Zeng H, Pathak J L, Shi Y, et al. Indirect selective laser sintering printed microporous biphasic calcium phosphate scaffold promotes endogenous bone regeneration via activation of ERK1/2 signaling[J]. Biofabrication. 2020. 10. Zhou B, Yan J, Guo L, et al. Hepatoma cell-intrinsic TLR9 activation induces immune escape through PD-L1 upregulation in hepatocellular carcinoma[J]. Theranostics. 2020, 10(14): 6530.

文献引用

1. Shao S, Xia H, Hu M, et al. Isotalatizidine, a C19-diterpenoid alkaloid, attenuates chronic neuropathic pain through stimulating ERK/CREB signaling pathway-mediated microglial dynorphin A expression. Journal of Neuroinflammation. 2020, 17(1): 1-11 2. Zeng H, Pathak J L, Shi Y, et al. Indirect selective laser sintering-printed microporous biphasic calcium phosphate scaffold promotes endogenous bone regeneration via activation of ERK1/2 signaling. Biofabrication. 2020, 12(2): 025032. 3. Zhou B, Yan J, Guo L, et al. Hepatoma cell-intrinsic TLR9 activation induces immune escape through PD-L1 upregulation in hepatocellular carcinoma. Theranostics. 2020, 10(14): 6530. 4. Zeng H, Pathak J L, Shi Y, et al. Indirect selective laser sintering printed microporous biphasic calcium phosphate scaffold promotes endogenous bone regeneration via activation of ERK1/2 signaling. Biofabrication. 2020 5. Xiao Q, Lei L, Ren J, et al. Mutant NPM1-Regulated FTO-Mediated m6A Demethylation Promotes Leukemic Cell Survival via PDGFRB/ERK Signaling Axis. Frontiers in Oncology. 2022.12 6. Zhu Y, Xiao Y, Kong D, et al. Down-Regulation of miR-378d Increased Rab10 Expression to Help Clearance of Mycobacterium tuberculosis in Macrophages. Frontiers in cellular and infection microbiology. 2020, 10: 108. 7. Meng Y, Lv T, Zhang J, et al.Temporospatial inhibition of Erk signaling is required for lymphatic valve formation.Signal Transduction and Targeted Therapy.2023, 8(1): 342.
5-Aminolevulinic acid hydrochloride Aspirin Hemin Adezmapimod Deferoxamine Mesylate Simvastatin Oxidopamine hydrochloride Dexamethasone acetate

相关化合物库

该产品包含在如下化合物库中:
高选择性抑制剂库 酪氨酸激酶分子库 抗卵巢癌化合物库 抑制剂库 经典已知活性库 HIF-1化合物库 抗胰腺癌化合物库 抗肥胖化合物库 自噬库 抗心血管疾病化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
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% Tween 80
% ddH2O
计算 重置

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

U0126-EtOH 1173097-76-1 Autophagy MAPK Microbiology/Virology Mitophagy Influenza Virus MEK Mitogen-activated protein kinase kinase MAP2K U-0126-EtOH inhibit competitive virus U0126 Ethanol U0126EtOH MAPKK Mitochondrial Autophagy U 0126 Inhibitor progeny non-ATP U0126 EtOH U-0126 U0126 inhibitor

 

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