U0126-EtOH

目录号:S1102

U0126-EtOH Chemical Structure

Molecular Weight(MW): 426.56

U0126-EtOH是一种高度选择性的MEK1/2抑制剂,无细胞试验中IC50为0.07 μM/0.06 μM,作用于ΔN3-S218E/S222D MEK的亲和力比PD098059强100倍。

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客户购买Selleck的此次产品后发表的文献61篇:

客户使用该产品的12个实验数据:

  •  

    Melanoma cell viability and in vivo growth by cyclindependent kinase 2/4 inhibition. Western blot analysis for c-Jun, phosphorylated-ERK1/2 (Thr202/Tyr204) (p-ERK1/2), and total ERK1/2 protein levels was done for human melanoma cell lines treated with the BRAFV600E inhibitor GDC-0879 (1 μM), or MEK inhibitors CI-1040 (1 μM), U0126 (1 μM), and PD98059 (10 μM) for 18 hours.

    J Natl Cancer Inst 2012 104(21), 1673-9. U0126-EtOH purchased from Selleck.

    Cells were stimulated with TPA (10 nM) for 15 min in the presence of the indicated concentrations of U0126. Samples were collected and analyzed by Western blot to detect phosphorylated p42/p44 MAPK.

    Proc Natl Acad Sci U S A 2014 111(15):E1528-37. U0126-EtOH purchased from Selleck.

  • Successful test of decision tree model prediction that reducing ERK signal on Cn/tEGF substrates will enhance MSC migration persistence and mean free path. (A) mean free path, (B) persistence time, and (C) speed under partial and total ERK inhibition with MEK inhibitor U0126

    Biomaterials 2011 32, 7524-7531. U0126-EtOH purchased from Selleck.

    Inhibition of the ERK1/2 pathway prevents FLIPL downregulation and sensitivity to TRAIL induced by EGF. MCF10A cells were preincubated in the absence of EGF for 48 h before re-addition of EGF ( -/+ ) and incubated in the presence or absence of ( a) the PI3K inhibitor LY294002 (LY, 10 μM), or (b) the MEK1 inhibitor U0126 (10 μM), for 15 h. Other cultures were incubated in parallel with (+/+ ) or without ( -/- ) EGF for the entire experimental period (preincubation/incubation). FLIPL , p-AKT, AKT, p-ERK1/2, ERK1/2 and BimEL levels were assessed by western blotting. GAPDH and tubulin levels were used as protein loading controls. FLIPL mRNA levels were measured by quantitative PCR (b , lower panel). Results are representative of two independent experiments. (c ) Cells were preincubated/incubated as in (b) and then TRAIL (500 ng/ml) was added to some cultures for 6 h. Apoptosis was determined as described in Materials and Methods. Error bars represent S.D. from three independent experiments.

    Cell Death Differ 2012 19, 1908-16. U0126-EtOH purchased from Selleck.

  • UACC62 cells were treated for 6 hours as indicated, followed by assessment of phospho-p90RSK1 and p90RSK1 levels by western blotting.

    J Invest Dermatol 2012 132, 2780-90. U0126-EtOH purchased from Selleck.

    SB431542(10 μM) and U0126EtOH (8 μM), which can inhibit of EMT were used to treat HCT-116 and HCT-8 in these experiments. (A) Protein expression levels of EMT markers E-cd, Claudin-4 and Vim in CRC cells. *P < 0.05.

    Sci Rep, 2016, 6:37534. U0126-EtOH purchased from Selleck.

  • ERK activation is increased in Il6ra2/2 mice compared with WT mice. A, Total and phosphorylated (p) Stat3 and ERK were assessed in small punch biopsy wounds collected after 30 min (Stat3) or 1 d (ERK) by Western blotting. Densitometry results for the blots are provided to the right. pp , 0.05. B, Total and p-ERKs were assessed in small wounds generated in WTand Il6ra2/2 mice treated topically with vehicle (DMSO) or with the MEK inhibitor U0126.Wounds were harvested after 1 d, and western blotting was performed on lysates. C, Wound contraction was assessed macroscopically in large wounds of WT (left panel) and Il6ra2/2 mice treated daily with vehicle (DMSO) or U0126. pp , 0.05.

    J Immunol 2010 184, 7219-7228. U0126-EtOH purchased from Selleck.

    Dose response curves and cytotoxic CI plots for A549 in 72 h combined treatment of gemcitacine, AG1478 and U0126 are shown in (A) and (B), respectively. These are also shown for H322 in (C) and (D). Gemcitabine concentration was set constant at 10 nM for A549 and 500 nM for H322. U0126 concentration was 2.5 μM and AG1478.

    Lung Cancer 2011 73, 274-82. U0126-EtOH purchased from Selleck.

  • Breast cancer cells were pretreated with 100ng/ml EGF for 15 min and then treated with the indicated concentrations of U0126 for 24 hours.

    2010 Dr. Zhang of Tianjin Medical University. U0126-EtOH purchased from Selleck.

    Some of the mice received intra-peritoneal administration of U0126 (10 mg/kg BW) or vehicle beginning at 24 h after I/R or sham until 24 h prior to harvest daily. Antibodies used was: Na,K-ATPase.

    Biochim Biophys Acta 2013 1832(12):1998-2008. U0126-EtOH purchased from Selleck.

  • Some of the mice received intra-peritoneal administration of U0126 (10 mg/kg BW) or vehicle beginning at 24 h after I/R or sham until 24 h prior to harvest daily. kidneys were snap-frozen in liquid nitrogen and perfusion-fixed with 30 mL of phosphate buffered saline (PBS) for 2 min and then PLP (4% paraformaldehyde, 75 mM l-lysine, 10 mM sodium periodate) solution, respectively.

    Biochim Biophys Acta 2013 1832(12):1998-2008. U0126-EtOH purchased from Selleck.

    U0126-EtOH purchased from Selleck.

产品安全说明书

MEK抑制剂选择性比较

生物活性

产品描述 U0126-EtOH是一种高度选择性的MEK1/2抑制剂,无细胞试验中IC50为0.07 μM/0.06 μM,作用于ΔN3-S218E/S222D MEK的亲和力比PD098059强100倍。
特性 A chemically synthesized and highly selective inhibitor of both MEK1 and MEK2.
靶点
MEK2 [1]
(Cell-free assay)
MEK1 [1]
(Cell-free assay)
0.06 μM 0.07 μM
体外研究

与MEK抑制剂PD098059(IC50为10 μM)相比,U0126高亲和力(高100多倍)作用于重组组成型激活的突变MEK1 (DN3-S218E/S222D),IC50为72 nM。与PD98059类似, U0126 非竞争性抑制MEK,说明 U0126结合在MEK的特定位点上。与作用于多种其他激酶,如PKC, Abl, Raf, MEKK, ERK, JNK, MKK-3, MKK-4/SEK, MKK-6, Cdk2, 和Cdk4相比,U0126 更显著高选择性作用于MEK1和MKE2。U0126 作用于TPA刺激的细胞,通过阻断 MAPK信号传递,显著抑制c-Fos和c-Jun mRNA的上调及蛋白水平,抑制达50-80%,导致AP-1转录活性受抑制,IC50为0.96 μM。[1]10 μM U0126通过抑制 ERK2而不是ERK1磷酸化,显著抑制细胞死亡。[2] 根据对ERK 和mTOR-p70S6K通路的同时抑制,U0126选择性抑制贴壁非依赖性Ki-ras-转化的大鼠成纤维细胞生长,也抑制组成型激活ERK, MDA-MB231和HBC4的肿瘤细胞系生长。[3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HeLa cells M3jiWGZ2dmO2aX;uJIF{e2G7 NWrZfllyUW6qaXLpeIlwdiCxZjDFS2Yue3SrbYXsZZRm\CCHbHuxMYx2[2moZYLhd4UhemWyb4L0[ZIh[XO|YYmgbY4hUGWOYTDj[YxteyxiSVO1NF0xNjJ7IN88UU4> NVrB[INMOTV{MkW3NFY>
COS-7 cells MmfBSpVv[3Srb36gZZN{[Xl? NEeycVlKdmirYnn0c5J6KGOxbnPlcpRz[XSrb36gZYdicW6|dDDBVE0yKHS{YX7zZ5JqeHSrb36gbY4hS0:VLUegZ4VtdHQxvJygTWM2OD1zIN88UU4> NUfSdIhJOTVyME[zPFY>
HCT116 cells MorHSpVv[3Srb36gZZN{[Xl? M17XS2FjcWyrdImgc4Yh[2:vcH;1coQhfG9iaX7obYJqfCCjbnPoc5Ji\2ViaX7k[ZBmdmSnboSgZ49td267IH\vdo1ifGmxbjCod49nfCCjZ3HyJIdzd3e2aDDhd5NigSliaX6gTGNVOTF4IHPlcIx{NCCLQ{WwQVE6NjRizszNMi=> NFPpVnYyPTJ{NUewOi=>
mouse RAS-3T3 cells NX3LPJFtTnWwY4Tpc44h[XO|YYm= NYLFdVIzOTBvNECg{txO Mnf3TY5pcWKrdHnvckBw\iCPRVutcYVlcWG2ZXSgSXJMOS9{IIDoc5NxcG:{eXzheIlwdiCrbjDtc5V{\SCUQWOtN3Q{KGOnbHzzJIF1KDFyIITvJFQxKHWPIHL5JGVNUVODLh?= M1zLfVI1PTB5OEK2
rat PC12 cells M4rwTmZ2dmO2aX;uJIF{e2G7 M1LsS|ExKM7:TR?= NV7MbJY3OSCq MnTiRYN1cX[jdHnvckBw\iCQcn[yM2FTTSCrbjDyZZQhWENzMjDj[YxteyCjc4Pld5Nm\CCjczDIU{0yKHC{b4TlbY4hcW6mdXP0bY9vKGG2IEGwJJVOKGGodHXyJFUhcHK|IIDy[ZRz\WG2ZXSge4l1cCCMTlugbY5pcWKrdH;yJHNRPjByMUK1JIZweiBzIHjyJIJm\m:{ZTDjc41xd3WwZDDh[IRqfGmxbjDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN? MmezNlE{PDV4OEW=

... Click to View More Cell Line Experimental Data

体内研究 U0126 作用于携带脑贫血-再灌注的CA1 锥体细胞的沙鼠,降低ERK1/2磷酸化,和随后的神经元死亡,这种作用存在剂量依赖性。U0126 按200 μg/kg剂量作用于局灶性脑缺血小鼠,显著降低 42%梗塞体积,也降低 41% 脑萎缩。[2]U0126按~30 mg/kg剂量腹腔注射给药患过敏性哮喘的小鼠,具有显著的抗炎效果,这种作用存在剂量依赖性,通过抑制 IL-4, IL-5, IL-13, eotaxin, VCAM-1, 全部IgE和OVA特定的IgE和IgG1。[4]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:[1]
+ 展开

体外激酶实验:

使用重组组成型激活的突变MEK-1 (DN3-S218E/S222D) 或组成型激活的 MEK-2(S222E/S226D)进行实验。使用 96孔 硝化纤维素过滤装置测量反应速度。在酶浓度为 10 nM时,在20 mM Hepes, 10 mM MgCl2, 5 mM β-巯基乙醇, 0.1 mg/mL BSA, pH 7.4, 中室温下进行反应。加入[γ-33P]ATP到预混合的U0126反应混合物中开始反应,每6分钟采集100 μL等分样,然后转移到含50 mM EDTA 的96孔硝化纤维模板上,阻止反应进行。提取模板,使用buffer 在真空下冲洗4次。使用30 μL Microscint-20 闪烁液填满每孔,使用Top Count 闪烁计数器测定33P-磷酸化的ERK的放射性。从放射性对时间曲线获得反应速度。ERK和 ATP浓度分别为400 nM和40 μM。数据绘制成抑制百分数,通过非线性最小二乘回归,根据 Langmuir 等温方程测定IC50值。
细胞实验:[3]
+ 展开
  • Cell lines: MCF-7, MDAMB453, SKBR3, ZR75-1, BSY1, HBC4, HBC5, 和 MDA-MB231
  • Concentrations: 溶于DMSO,终浓度为~50 μM
  • Incubation Time: 24, 48, 或96小时
  • Method: 为了测量贴壁非依赖性生长,细胞按每孔 5000 个细胞接种在聚HEMA包被的96孔板上,体积为135 μL。加入培养基稀释的15 μL 不同浓度U0126,然后细胞培养96小时。加入15 μL MTT 溶液(5 mg/mL,溶于 PBS),再温育4小时。加入 100 μL SDS溶液 (20% ,溶于10 mM HCl), MTT甲臜被溶解,24小时后,在570 nm 处测量吸光值,然后使用酶标仪在 690 nm处测定参考波长。为了测定DNA 片段,细胞接种在聚HEMA包被或未包被的组织培养塑料 35-mm盘上,然后温育24小时。使用U0126处理细胞24-48小时,使用PBS冲洗,然后使用10 mM Tris-HCl (pH 7.4), 10 mM EDTA,和0.5% Triton X-100溶解。在10,000 g转速下离心10分钟,分离低分子量DNA片段。使用20 μg/mL RNase A处理含等量蛋白的上清液1小时,然后使用 20 μg/mL蛋白酶 K在37oC下处理30分钟。使用2-丙醇沉淀DNA,在2%琼脂糖凝胶上跑胶,然后通过SYBR Green I 染色观察。
    (Only for Reference)
动物实验:[2]
+ 展开
  • Animal Models: 携带双侧颈总动脉闭塞(BCAO)诱导脑部缺血的雄性沙土鼠,携带大脑中动脉闭塞(MCAO) 诱导局灶性脑缺血的雄性ICR或ddY小鼠
  • Formulation: 溶于DMSO,然后在0.1 M PBS中稀释
  • Dosages: ~400 μg/kg
  • Administration: 静脉注射
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 85 mg/mL warmed (199.26 mM)
Water Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品:
10% DMSO+50% PEG 300+ddH2O
28mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 426.56
化学式

C18H16N6S2.C2H6O

CAS号 1173097-76-1
稳定性 powder
别名 N/A

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

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操作手册

如果有其他问题,请给我们留言。

  • * 必填项

常见问题及建议解决方法

  • 问题 1:

    I want to know whether the compound is light-sensitive?

  • 回答:

    S1102 U0126-EtOH is not stable. It should be stored as powder at -20°C, and prepared the solution just before use.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID