LY2090314

For research use only. Not for use in humans.

目录号:S7063

LY2090314 Chemical Structure

CAS No. 603288-22-8

LY2090314是一种有效的GSK-3抑制剂,作用于GSK-3α/βIC50为1.5 nM/0.9 nM;可提高以铂类为基础的化疗方案的疗效。LY2090314对GSK3具有高选择性,对其他大多数激酶的抑制活性低。

规格 价格 库存 购买数量  
RMB 1179.11 现货
RMB 3924.74 现货
RMB 8168.66 现货
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客户使用Selleck生产的LY2090314发表文献15篇:

客户使用该产品的5个实验数据:

  • Western blot of β-catenin, and p62 in FS5 and FS4 melanoma cells upon treatment with the GSK3 inhibitor (LY2090314)) for the indicated doses for 8 hours; loading control: HSP90.

    Cancer Res, 2017, 77(21):5873-5885. LY2090314 purchased from Selleck.

  • (D) GS87 leads to more effective AML differentiation than other clinically used GSK3 inhibitors. HL-60 cells were treated with GS87 (30 μM), Tideglusib (30 μM) or LY-2090314 (30 μM) for 72 hours and differentiation was measured by the NBT assay. * p<.05; **p<.01.

    Mol Cancer Ther, 2016, 15(7):1485-94.. LY2090314 purchased from Selleck.

  • LY2090314 was tested and exhibited similar synergistic apoptotic effect when co-administered with NAC. Error bar represents the standard deviation of 3 biological replicates.

    Stem Cell Res, 2017, 182-187. LY2090314 purchased from Selleck.

  • LY2090314 decreased GSK-3 phosphorylation and attenuate apoptosis inhibitor expression. a Western blots of all 3 cell lines (NGP, SK-N-AS, SH-SY-5Y), showing decreased phosphorylation of GSK-3α at Tyr279 compared to GSK-3β phosphorylation at Tyr216 as well as decrease in inactive phosphorylation ser 9 and 21. However, there is minimal to no decrease in phosphorylation of active Akt at ser 473. b Western blot analysis showed there is an increase in pro-apoptotic markers such as cleaved PARP and cleaved caspase-3, and a decrease in anti-apoptotic markers, cyclin D1, Mcl-1, and survivin. GAPDH was used as loading control. Experiments were repeated at least three times and the best pictures are shown here.

    BMC Cancer, 2018, 18(1):560. LY2090314 purchased from Selleck.

  • Expressions of p65 and c-Rel in NK cells treated with ILQ or LY-2090314 were detected by western blotting.

    Eur J Pharmacol, 2018, 838:11-22. LY2090314 purchased from Selleck.

产品安全说明书

GSK-3抑制剂选择性比较

生物活性

产品描述 LY2090314是一种有效的GSK-3抑制剂,作用于GSK-3α/βIC50为1.5 nM/0.9 nM;可提高以铂类为基础的化疗方案的疗效。LY2090314对GSK3具有高选择性,对其他大多数激酶的抑制活性低。
靶点
GSK-3β [1] GSK-3α [1]
0.9 nM 1.5 nM
体外研究

LY2090314通过阻断ATP结合选择性抑制GSK-3的活性。LY2090314能够稳定β-连环蛋白。LY2090314单药治疗,表现出有限的疗效。LY3090314增强顺铂和卡铂对体外实体肿瘤癌细胞系的疗效。[1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human SY5Y cells M1vDPGZ2dmO2aX;uJIF{e2G7 NFnC[I5KdmirYnn0bY9vKG:oIFfsfYNw\2WwIIP5cpRp[XOnIHvpcoF{\S1|IHLleIEh\GWyZX7k[Y51KFSjdTDwdo91\WmwIIPldolv\S1|OU[gdIhwe3Cqb4L5cIF1cW:wIHnuJIh2dWGwIGPZOXkh[2WubIOsJGlEPTB;MD63JI5O MXmxOVI3PzJ|Mh?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-GSK3 / GSK3 / p-AKT ; 

PubMed: 29751783     


Western blots of all 3 cell lines (NGP, SK-N-AS, SH-SY-5Y), showing decreased phosphorylation of GSK-3α at Tyr279 compared to GSK-3β phosphorylation at Tyr216 as well as decrease in inactive phosphorylation ser 9 and 21. However, there is minimal to no decrease in phosphorylation of active Akt at ser 473.

Cleaved PARP / Cleaved caspase-3 / Cyclin D1 / Survivin / Mcl-1 ; 

PubMed: 29751783     


Western blot analysis showed there is an increase in pro-apoptotic markers such as cleaved PARP and cleaved caspase-3, and a decrease in anti-apoptotic markers, cyclin D1, Mcl-1, and survivin. GAPDH was used as loading control.

LSD1 / Mono-methyl-Histone H3 (K4) ; 

PubMed: 29593255     


SKOV3 and ARK2 cells were treated for 24 h with different concentrations of the GSK3β inhibitor LY2090314. Protein levels of LSD1, mono-methylated H3K4, total histone 3, and actin were determined with Western blot.

29751783 29593255
Immunofluorescence
LSD1; 

PubMed: 29593255     


Confocal microscopy image indicated the intracellular localization of endogenous LSD1 (green) in cells treated with DMSO or LY2090314 (10 µM) for 24 h or LY2090314 (10 µM) with leptomycin B (10 nM) for 24 h.

29593255
Growth inhibition assay
Cell viability; 

PubMed: 29751783     


Growth inhibition of human NGP, SK-N-AS, SH-SY-5Y cell lines treated with LY2090314 or Tideglusib by MTT assay. NB cells a NGP b SK-N-AS and c SH-SY-5Y were plated in a 96 well plate and treated with LY2090314 or Tideglusib in increasing concentrations and assay data was collected at 48, 72, and 96 h. Percentage of cell growth seen decreasing in dose and time dependent manner. Tideglusib required μM concentrations compared to LY2090314 (nM) for similar growth reduction. Statistical analysis showed significant growth reduction with increasing concentrations of these drugs. NS, not significant; *, p = 0.05; ** P < 0.01; ***, p > 0.001; ****, p > 0.0001. Each experiment was repeated at least three times and the average of these experiments is shown here.

29751783
体内研究

LY2090314增强顺铂和卡铂对异种移植实体肿瘤的疗效。[1]

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)

溶解度 (25°C)

体外 DMSO 100 mg/mL (195.11 mM)
Ethanol 2 mg/mL warmed (3.9 mM)
Water Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
5% DMSO+45% PEG 300+ddH2O
17mg/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 512.53
化学式

C28H25FN6O3

CAS号 603288-22-8
储存条件 粉状
溶于溶剂
别名 N/A

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

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 (mg) = 浓度 (mM) x 体积 (mL) 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

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

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 use BI2536 in preclinical studies using mice with intracranial xenografts. How could I reconstitute the compound?

  • 回答:

    For in vivo study, DMSO should not be more than 5% because the toxicity. You can formulated BII2536 in hydrochloric acid (0.1 N), and diluted with 0.9% NaCl for animal study according to the reference: http://linkinghub.elsevier.com/retrieve/pii/S0960-9822(06)02671-6 (supplemental Data)

GSK-3 Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID