1. Epigenetics Autophagy
  2. Histone Methyltransferase Autophagy
  3. GSK343

GSK343 是一种高效,选择性的 EZH2 抑制剂,IC50 为 4 nM。

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GSK343 Chemical Structure

GSK343 Chemical Structure

CAS No. : 1346704-33-3

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥596
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5 mg ¥495
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10 mg ¥800
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25 mg ¥1560
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50 mg ¥2420
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100 mg ¥3800
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Top Publications Citing Use of Products

    GSK343 purchased from MCE. Usage Cited in: Nat Chem Biol. 2023 Mar 27.  [Abstract]

    GSK343 (1, 2.5, 5, 10 μM; 72 h) reduces the level of H3K27me3 in wild-type and CXCdel+/− Karpas-422 cells.

    GSK343 purchased from MCE. Usage Cited in: Int Immunopharmacol. 2023 Apr 10;119:110155.  [Abstract]

    GSK343 (2.5 mg/kg; i.p.; 32 weeks) reduces extensive IgG deposition in the kidneys of lupus mice.(once every other day for the first 16 weeks, then twice a week for 8 weeks, and finally once a week for 8 weeks)

    GSK343 purchased from MCE. Usage Cited in: Theranostics. 2019 Jan 24;9(3):761-777.  [Abstract]

    Immunoblot analysis of the indicated proteins in lysates from cells as in G with α-Tubulin as loading control with or without the treatment of GSK343.

    GSK343 purchased from MCE. Usage Cited in: Oncol Lett. 2018 Jul;16(1):1231-1236.  [Abstract]

    EZH2 protein expression in T24 cells treated with methyl jasmonate alone or in combination with GSK343 is analyzed using western blot analysis.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    GSK343 is a highly potent and selective EZH2 inhibitor with an IC50 of 4 nM.

    IC50 & Target

    EZH2

     

    体外研究
    (In Vitro)

    GSK343 在吡啶酮的4位含有正丙基,EZH2 Kiapp=1.2±0.2 nM。在这项为期 6 天的增殖试验中,在本研究评估的细胞系中,前列腺癌细胞系 LNCaP 对 EZH2 抑制最敏感,GSK343 的生长 IC50 值为 2.9 μM >[1]。发现 GSK343 在 HeLa 细胞中的半数最大抑制浓度值为 13 μM,在 SiHa 细胞中为 15 μM[2]

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    体内研究
    (In Vivo)

    与对照组相比,GSK343 (5 mg/kg) 处理的小鼠表现出显著肿瘤生长抑制。GSK343 处理组的平均肿瘤体积和重量显著降低。早在植入后 20 天,与对照组相比,在 GSK343 处理组中观察到肿瘤生长显著减少;这种差异在其他研究中一直存在。此外,与对照组相比,异种移植模型中 GSK343 处理的动物显示 E-cadherin 信使 RNA 水平显著增加,但波形蛋白信使 RNA 水平显著降低[2]

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    分子量

    541.69

    Formula

    C31H39N7O2

    CAS 号
    性状

    固体

    颜色

    White to yellow

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : 15.62 mg/mL (28.84 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.8461 mL 9.2304 mL 18.4607 mL
    5 mM 0.3692 mL 1.8461 mL 3.6921 mL
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    In Vivo:

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 1.56 mg/mL (2.88 mM); 澄清溶液

      此方案可获得 ≥ 1.56 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 15.6 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

      生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 1.56 mg/mL (2.88 mM); 澄清溶液

      此方案可获得 ≥ 1.56 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 15.6 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

      20% SBE-β-CD in Saline 的配制(4°C,储存一周):2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
    动物溶解方案计算器
    请输入动物实验的基本信息:

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    由于实验过程有损耗,建议您多配一只动物的量
    请输入您的动物体内配方组成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
    您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
    连续给药周期超过半月以上,请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.88%

    参考文献
    Kinase Assay
    [1]

    Activity against EZH2 is assessed using 5 member PRC2 complex (Flag-EZH2, EED, SUZ12, AEBP2, RbAp48). The assay protocol may be summarized as follows: 10 mM stocks of GSK343 are prepared from solid in 100% DMSO. An 11 point serial dilution master plate is prepared in 384 well format (1:3 dilution, columns 6 and 18 are equal volume DMSO controls) and dispensed to assay ready plates using acoustic dispensing technology to create a 100 nL stamp of GSK343 and DMSO controls. The assay additions consisted of equal volume additions of 10 nM EZH2 and the substrate solution (5 μg/mL HeLa nucleosomes and 0.25 μM [3H]-SAM) dispensed into assay plates using a multi-drop combi dispense. Reaction plates are incubated for 1 hr and quenched with an equal volume addition of 0.5 mg/mL PS-PEI Imaging Beads (RPNQ0098) containing 0.1 mM unlabeled SAM. The plates are sealed, dark adapted for 30 minutes, and a 5 minute endpoint luminescence image is acquired using a Viewlux imager. Plate statistics such as Z’ and signal to background as well as dose response curves are analyzed using ActivityBaseXE. The in vitro biochemical activity of EZH1 is assessed as part of a 5 member PRC2 complex using a 384 well SPA assay identical to EZH2. Buffer components, reagent dispensing, GSK343 plate preparation, quench conditions and data analysis are identical for EZH1 and EZH2 with final assay concentrations of 20 nM EZH1, 5 μg/mL HeLa nucleosomes and 0.25 μM [3H]-SAM. Further data analysis, pIC50 pivots and visualizations are enabled by TIBCO Spotfire[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [1]

    To account for varying doubling rates among cancer cell lines, the optimal cell seeding is determined empirically for all cell lines by examining their growth in a 384-well plate over 6 days with a wide range of seeding densities. Cells are then plated at the optimal seeding density and allowed to adhere overnight. Cells are treated in duplicate with a 20-point 2-fold dilution series of GSK343 or 0.147% DMSO (vehicle control) and incubated for 6 days at 37°C in 5% CO2. Cells are then lysed with 25 μL CellTiter-Glo per well and chemiluminescence is quantified with a TECAN Safire2 microplate reader. In addition, an untreated plate of cells is harvested at the time of GSK343 addition (T0) to quantify the starting number of cells. CTG values after 6 days of treatment are expressed as a percent of the T0 value and plotted against GSK343 concentration. Data are fit with a 4-parameter equation to generate a concentration response curve and the concentration of GSK343 required to inhibit 50% of growth (gIC50) is determined[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [2]

    Mice[2]
    Six-week-old female nude BALB/c mice are used. To study the effect of the EZH2 inhibitor GSK343, 5 mg/kg in 100-μL phosphate-buffered saline is injected intraperitoneally every other day into BALB/c nude mice (n=6) after the tumor volume reaches 100 mm3. In this analysis, the negative control group (n=6) received saline. After 40 days, the mice are killed, and the subcutaneous tumors are surgically excised, weighed, photographed, sectioned, and fixed in 10% formalin. The expression levels of E-cadherin, N-cadherin, and vimentin in the tumours are measured by real-time reverse transcription polymerase chain reaction.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    参考文献

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.8461 mL 9.2304 mL 18.4607 mL 46.1519 mL
    5 mM 0.3692 mL 1.8461 mL 3.6921 mL 9.2304 mL
    10 mM 0.1846 mL 0.9230 mL 1.8461 mL 4.6152 mL
    15 mM 0.1231 mL 0.6154 mL 1.2307 mL 3.0768 mL
    20 mM 0.0923 mL 0.4615 mL 0.9230 mL 2.3076 mL
    25 mM 0.0738 mL 0.3692 mL 0.7384 mL 1.8461 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    产品名称:
    GSK343
    目录号:
    HY-13500
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