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GSK583

GSK583

产品编号 T3537   CAS 1346547-00-9

GSK583 是一种高效且特异性的 RIP2 激酶抑制剂,IC50值为 5 nM。它抑制 TNF-α 和 IL-6 的产生,IC50值为 200 nM。

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GSK583 Chemical Structure
GSK583, CAS 1346547-00-9
规格 价格/CNY 货期 数量
1 mg ¥ 428 现货
2 mg ¥ 622 现货
5 mg ¥ 1,160 现货
10 mg ¥ 1,630 现货
25 mg ¥ 2,970 现货
50 mg ¥ 4,380 现货
100 mg ¥ 6,230 现货
500 mg ¥ 12,700 现货
1 mL * 10 mM (in DMSO) ¥ 973 现货
产品目录号及名称: GSK583 (T3537)
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纯度: 99.06%
纯度: 98.68%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 GSK583 is a highly effective and specific RIP2 kinase inhibitor (IC50: 5 nM).
靶点活性 RIP2:5 nM
体外活性 GSK583 possesses a comparable binding affinity for RIP3 kinase similarly to the RIP2 (RIP2/3 FP IC50: 5/16 nM) by an in-house FP binding assay configured. But GSK583 (10 μM) shows little or no inhibition of RIP3-dependent necroptotic cell death in a cellular assay. GSK583 effectively and dose-dependently inhibits MDP-stimulated TNFα production (IC50: 8 nM) in primary human monocytes. Following treatment with GSK583 at 1 μM, little inhibition of pro-inflammatory signaling is observed upon activation of cytokine receptors (IL-1R, TNFR) or Toll-like receptors (TLR2, TLR4, TLR7) but complete inhibition is observed upon activation of NOD1/2 receptors, which signal in a RIP2-dependent manner. Although it has excellent kinase selectivity, GSK583 does inhibit both the hERG channel and CYP3A4.
体内活性 GSK583 has moderate volumes of distribution, low clearance, and moderate oral bioavailability (in rat and mouse). Although GSK583 would not produce a human pharmacodynamic response within an acceptable dose range, the oral PK in mouse and rat supplies enough systemic exposure for use as a preclinical in vivo tool molecule in an acute inflammation challenge model.
激酶实验 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).
细胞实验 To assess cellular selectivity, monocytes are pretreated with inhibitor for 30 min, then stimulated for 6 h with ligands which selectively agonize NLRs NOD1, NOD2; Toll-like receptors TLR, TLR4, TLR7, or cytokine receptors IL-1R, TNFR. Release of pro-inflammatory cytokines, either TNFα (NOD2, TLR2, TLR4, IL1R) or IL-8 (NOD1, TLR7, TNFR), is measured by immunoassay. Percent inhibition and/or IC50 values are calculated. (Only for Reference)
分子量 398.45
分子式 C20H19FN4O2S
CAS No. 1346547-00-9

存储

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

溶解度

DMSO: 73 mg/mL (183.2 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 27 mg/mL (67.8 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 / Ethanol 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 0.251 mL 1.2549 mL 2.5097 mL 6.2743 mL
20 mM 0.1255 mL 0.6274 mL 1.2549 mL 3.1372 mL
50 mM 0.0502 mL 0.251 mL 0.5019 mL 1.2549 mL
DMSO 100 mM 0.0251 mL 0.1255 mL 0.251 mL 0.6274 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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参考文献

1. Haile PA, et al. J Med Chem. 2016, 59(10):4867-80.
RIPK1-IN-17 RIPK3-IN-4 SZM679 GSK872 HCl(1346546-69-7 free base) RIP1 kinase inhibitor 4 RIP1 kinase inhibitor 5 GSK963 RIP1 kinase inhibitor 6

相关化合物库

该产品包含在如下化合物库中:
抗前列腺癌化合物库 激酶抑制剂库 抑制剂库 经典已知活性库 抗卵巢癌化合物库 抗癌化合物库 抗肝癌化合物库 NO PAINS 化合物库 抗抑郁症化合物库 含氟化合物库

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
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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

GSK583 1346547-00-9 Apoptosis NF-Κb RIP kinase RIPK Inhibitor Receptor-interacting protein kinases GSK-583 GSK 583 inhibit inhibitor

 

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