AR-A014418

产品编号: T1881 别名:

GSK-3beta Inhibitor VIII,AR 014418,AR 0133418,GSK 3β inhibitor VIII

AR-A014418 是选择性的，ATP 竞争性的GSK3β抑制剂，其 IC50=104 nM，Ki=38 nM。

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CAS：487021-52-3

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生物活性化学信息储存和溶解度信息参考文献引用文献

产品描述

AR-A014418 is an ATP-competitive, and selective GSK3β inhibitor.

体外活性

AR-A014418通过调节NMDA和代谢型受体信号传导以及在脊髓中的TNF-α和IL-1β传递,对乙酸和福尔马林诱导的小鼠伤害感受产生抑制作用.在具有G93A突变型人SOD1的ALS小鼠模型中,AR-A014418（0-4 mg/kg,i.p.）延迟症状的发作,改善运动行为,减缓疾病进展.

体内活性

AR-A014418在NGP细胞和SH-5Y-SY细胞中,抑制神经内分泌标志物,抑制神经瘤细胞的生长。AR-A014418抑制海马切片中由β样淀粉肽诱导的神经退化。AR-A014418抑制表达人类四重复tau蛋白的3T3成纤维细胞中的GSK3特异性位点（Ser-396）处的tau磷酸化,IC50为2.7 μM,并且保护培养的N2A细胞免于通过阻断PI3K/PKB途径诱导的死亡。

激酶实验

GSK3 Scintillation Proximity Assay: The competition experiments are carried out in duplicate with 10 concentrations of the inhibitor in clear-bottomed microtiter plates. The biotinylated peptide substrate, biotin-AAEELDSRAGS(PO3H2)PQL, is added at a final concentration of 2 μM in an assay buffer containing 6 milliunits of recombinant human GSK3 (equal mix of both α and β), 12 mM MOPS, pH 7.0, 0.3 mM EDTA, 0.01% β-mercaptoethanol, 0.004% Brij 35, 0.5% glycerol, and 0.5 μg of bovine serum albumin/25 μl and preincubated for 10-15 min. The reaction is initiated by the addition of 0.04 μCi of [γ-33P]ATP and unlabeled ATP in 50 mM Mg(Ac)2 to a final concentration of 1 μM ATP and assay volume of 25 μl. Blank controls without peptide substrate are used. After incubation for 20 min at room temperature, each reaction is terminated by the addition of 25 μl of stop solution containing 5 mM EDTA, 50 μM ATP, 0.1% Triton X-100, and 0.25 mg of streptavidin-coated SPA beads corresponding to ～35 pmol of binding capacity. After 6 h the radioactivity is determined in a liquid scintillation counter. Inhibition curves are analyzed by non-linear regression using GraphPad Prism.

细胞实验

Cell viability is assessed by calcein/propidium iodide uptake. Calcein AM is taken up and cleaved by esterases present within living cells, yielding yellowish-green fluorescence, whereas PI is only taken up by dead cells, which become orange-red fluorescent. In brief, N2A cells are cultured for 2 days in vitro and then treated with 50 μM LY-294002 in the presence of AR-A014418 or vehicle (DMSO) for 24 h. Subsequently, N2A cells are incubated for 30 min with 2 μM PI and 1 μM calcein-AM. The cultures are then rinsed three times with Hanks' buffered saline solution containing 2 mM CaCl2, and the cells are visualized by fluorescence microscopy using a Zeiss Axiovert 135 microscope. Three fields (selected at random) are analyzed per well (∼300 cells/field) in at least three different experiments. Cell death is expressed as percentage of PI-positive cells from the total number of cells. In every experiment, specific cell death is obtained after subtracting the number of dead cells present in vehicle-treated cultures. (Only for Reference)

Cas No.

487021-52-3

分子式

C12H12N4O4S

分子量

308.31

别名

GSK-3beta Inhibitor VIII;AR 014418;AR 0133418;GSK 3β inhibitor VIII;AR-A014418

参考文献

[1]Zhang Y, Zhang J, Wang E, et al. Microcystin-LR induces tau pathology through Bα degradation via PP2A demethylation and associated GSK-3β phosphorylation[J]. Toxicological Sciences. 2018 Apr 1;162(2):475-487.[2]Carter YM, et al. Cancer Biol Ther. 2014, 15(5).[3]Mai C L, Wei X, Gui W S, et al. Differential regulation of GSK-3β in spinal dorsal horn and in hippocampus mediated by interleukin-1beta contributes to pain hypersensitivity and memory deficits following peripheral nerve injury[J]. Molecular pain. 2019, 15: 1744806919826789.[4]Bhat R, et al. J Biol Chem. 2003, 278(46), 45937-45945.[5]Martins DF, et al. J Pain. 2011, 12(3), 315-322.[6]Koh SH, et al. Exp Neurol. 2007, 205(2), 336-346.[7]Tian J, Li X, Zhao L, et al. Glycyrrhizic Acid Promotes Neural Repair by Directly Driving Functional Remyelination[J]. Food & Function. 2019.[8]Zhang Y, Zhang J, Wang E, et al. Microcystin-Leucine-Arginine Induces Tau Pathology Through Bα Degradation via Protein Phosphatase 2A Demethylation and Associated Glycogen Synthase Kinase-3β Phosphorylation. Toxicological Sciences. 2018, 162(2): 475-487.

引用文献

[1]Zhang Y, Zhang J, Wang E, et al. Microcystin-LR induces tau pathology through Bα degradation via PP2A demethylation and associated GSK-3β phosphorylation. Toxicological Sciences. 2018 Apr 1;162(2):475-487 [2]Zhang Y, Zhang J, Wang E, et al. Microcystin-Leucine-Arginine Induces Tau Pathology Through Bα Degradation via Protein Phosphatase 2A Demethylation and Associated Glycogen Synthase Kinase-3β Phosphorylation. Toxicological Sciences. 2018, 162(2): 475-487 [3]Tian J, Li X, Zhao L, et al. Glycyrrhizic Acid Promotes Neural Repair by Directly Driving Functional Remyelination. Food & Function. 2019 [4]Mai C L, Wei X, Gui W S, et al. Differential regulation of GSK-3β in spinal dorsal horn and in hippocampus mediated by interleukin-1beta contributes to pain hypersensitivity and memory deficits following peripheral nerve injury. Molecular pain. 2019, 15: 1744806919826789.

储存和溶解度

Ethanol:1.5 mg/mL (5 mM)
DMSO:30.8 mg/mL (100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years

剂量换算 AR-A014418 487021-52-3

对于各种应用，安全且有效的用药剂量是很有必要的了解更多

体内实验配液计算器

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 ul

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 +

% +

% Tween 80 +

% ddH₂O

% DMSO +

重置计算

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 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 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

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将已知质量的化合物溶解到所需浓度所需的溶液体积
已知质量的化合物在一定体积内形成的溶液的浓度

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技术支持

在抑制剂处理说明中可以找到您可能遇到的问题的答案。主题包括如何准备储备溶液，如何存储产品以及基于细胞的测定和动物实验需要特别注意的问题。

Keywords

AR014418 AR A014418 GSK-3beta Inhibitor VIII Glycogen synthase kinase 3 AR 014418 Inhibitor inhibit AR-014418 AR 0133418 Glycogen synthase kinase-3 AR-A-014418 AR-0133418 AR0133418 GSK 3β inhibitor VIII GSK-3 AR-A014418 ARA014418 487021-52-3

AR-A014418 相关推荐

相关化合物库推荐该产品包含在如下化合物库中：

注册成功

AR-A014418

GSK-3beta Inhibitor VIII,AR 014418,AR 0133418,GSK 3β inhibitor VIII

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