2. Apoptosis
  3. RIP kinase
  4. GSK583

GSK583 是一种高效、口服有效的、高选择性的 RIP2 Kinase 抑制剂，其 IC50 值为 5 nM。GSK583 可同时抑制TNF-α 和IL-6 的产生，IC50 值为 200 nM。

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GSK583 Chemical Structure

GSK583 Chemical Structure

CAS No. : 1346547-00-9

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1227
In-stock
2 mg ￥750
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5 mg ￥1400
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10 mg ￥1960
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25 mg ￥3435
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50 mg ￥5153
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100 mg 现货 询价
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

GSK583 相关抗体

Top Publications Citing Use of Products

    GSK583 purchased from MCE. Usage Cited in: J Immunol. 2017 May 1;198(9):3729-3736.  [Abstract]

    Confocal images of lysozyme and procryptdin in cultured WT crypt organoids treated with GSK583 (5 μM) or mock-treated (A), or WEHI-345 (2.5 μM) or mock-treated (B) for 16 hours.

    查看 RIP kinase 亚型特异性产品:

    查看所有亚型
    RIPK1 RIPK2 RIPK3

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    GSK583 is a highly potent, orally active and selective inhibitor of RIP2 Kinase, with IC50 of 5 nM. GSK583 inhibits both TNF-α and IL-6 production with an IC50 value of 200 nM.

    IC50 & Target

    IC50: 5 nM (RIP2K)[1]
    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    Monocyte IC50
    8 nM
    Compound: 27
    Inhibition of MDP-stimulated TNF-alpha release in human monocytes preincubated for 30 mins prior to MDP stimulation measured after 6 hrs by immunoassay
    Inhibition of MDP-stimulated TNF-alpha release in human monocytes preincubated for 30 mins prior to MDP stimulation measured after 6 hrs by immunoassay
    		[PMID: 27109867]
    体外研究
    (In Vitro)

    GSK583 (1 μM) 在 300 种激酶 (包括 p38α 和 VEGFR2) 中表现出良好的选择性。GSK583 有效且剂量依赖地抑制 MDP 刺激的肿瘤坏死因子 α (TNFα) 的产生，IC50 为 8 nM。在类似的 MDP 诱导的人全血 (IC50=237 nM) 和大鼠全血 (IC50=133 nM) 中，GSK583 仅 显示出适度的降低效力[1]。

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

    GSK583 相关抗体:
    体内研究
    (In Vivo)

    GSK583 (0.1、1 和 10 mg/kg，口服) 以剂量依赖性方式抑制大鼠血清 KC (IL-8 的啮齿动物直系同源物) 水平，IC50 浓度为 50 nM (或 20 ng/mL) (来自大鼠血液)。同样，GSK583 以剂量依赖性方式抑制小鼠血清 KC 水平和中性粒细胞向腹膜腔募集，IC50 为 37 nM (15 ng/mL)，源自小鼠血液[1]。

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

    398.45

    Formula

    C20H19FN4O2S
    CAS 号
    性状

    固体

    颜色

    Light yellow 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 1 year
    -20°C 6 months
    溶解性数据
    细胞实验： 

    DMSO 中的溶解度 : ≥ 100 mg/mL (250.97 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.5097 mL 12.5486 mL 25.0972 mL
    5 mM 0.5019 mL 2.5097 mL 5.0195 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, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

    • 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

    动物实验：

    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: ≥ 2.5 mg/mL (6.27 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 25.0 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: ≥ 2.5 mg/mL (6.27 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 25.0 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。

      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

    只
    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: 98.74%

    COA (291 KB) LCMS (96 KB)

    产品使用指南 (1538 KB)
    参考文献
    Kinase Assay
    [1]

    A fluorescent polarization based binding assay is developed to quantitate interaction of novel test compounds at the ATP binding pocket of RIP2K by competition with a fluorescently labeled ATP competitive ligand. Full length FLAG His tagged RIP2K is purified from a baculovirus expression system and is used at a final assay concentration of twice the KD apparent. A fluorescent labeled ligand that is reversible and competitive with the inhibitors is used at a final assay concentration of 5 nM. Both the enzyme and ligand are prepared in solutions in 50 mM HEPES pH 7.5, 150 mM NaCl, 10 mM MgCl2, 1 mM DTT, and 1 mM CHAPS. Test compounds are prepared in 100% DMSO, and 100 nL is dispensed to individual wells of a multiwell plate. Next, 5 μL of RIP2K is added to the test compounds at twice the final assay concentration and incubated at room temperature for 10 min. Following the incubation, 5 μL of the fluorescent labeled ligand solution is added to each reaction at twice the final assay concentration and incubated at room temperature for at least 10 min. Finally, samples are read on an instrument capable of measuring fluorescent polarization. Test compound inhibition is expressed as percent (%) inhibition of internal assay controls. For concentration response experiments, normalized data are fit using the following four parameter logistic equation: y = A + ((B-C))/(1+(10x)/(10C)D), where y is the % activity (% inhibition) at a specified compound concentration, A is the minimum % activity, B is the maximum % activity, C = log10(IC50), D = Hill slope, x = log10(compound concentration [M]), and pIC50 = (−C).

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    Mice[1]
    Female C57Bl/6 mice (for cytokine analyses) or male Balb/c mice (for peritoneal neutrophil analyses) (n=10/treatment group) are dosed orally 15 min prior to MDP challenge with vehicle or GSK583 (0.1, 1, or 10 mg/kg). For peritoneal neutrophil analysis, mice are sacrificed at 4 h post-MDP challenge (30 μg, i.p.) and peritoneal fluid is collected by lavage. Peritoneal neutrophils are quantified by FACS analysis.
    Rats[1]
    Female Crl:CD(SD) rats (n=8/treatment group) are dosed orally with vehicle or GSK583 15 min prior to MDP challenge (150 μg/rat, IV). At 2 h post MDP challenge, rats are sacrificed and terminal serum is prepared from blood collected via cardiac stick. Serum cytokine levels (IL-6, IL-8 or KC, IL-1β, and TNFα) are quantified by the MSD platform.

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

    GSK583 相关分类

    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, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.5097 mL 12.5486 mL 25.0973 mL 62.7431 mL
    5 mM 0.5019 mL 2.5097 mL 5.0195 mL 12.5486 mL
    10 mM 0.2510 mL 1.2549 mL 2.5097 mL 6.2743 mL
    15 mM 0.1673 mL 0.8366 mL 1.6732 mL 4.1829 mL
    20 mM 0.1255 mL 0.6274 mL 1.2549 mL 3.1372 mL
    25 mM 0.1004 mL 0.5019 mL 1.0039 mL 2.5097 mL
    30 mM 0.0837 mL 0.4183 mL 0.8366 mL 2.0914 mL
    40 mM 0.0627 mL 0.3137 mL 0.6274 mL 1.5686 mL
    50 mM 0.0502 mL 0.2510 mL 0.5019 mL 1.2549 mL
    60 mM 0.0418 mL 0.2091 mL 0.4183 mL 1.0457 mL
    80 mM 0.0314 mL 0.1569 mL 0.3137 mL 0.7843 mL
    100 mM 0.0251 mL 0.1255 mL 0.2510 mL 0.6274 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.

    Keywords:

    GSK5831346547-00-9GSK 583GSK-583RIP kinaseReceptor-interacting protein kinasesRIPKInhibitorinhibitorinhibit

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