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AR-A014418

AR-A014418

产品编号 T1881   CAS 487021-52-3
别名: AR 0133418, GSK-3beta Inhibitor VIII, AR 014418, GSK 3β inhibitor VIII

AR-A014418 (GSK 3β inhibitor VIII) 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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AR-A014418 Chemical Structure
AR-A014418, CAS 487021-52-3
规格 价格/CNY 货期 数量
5 mg ¥ 415 现货
10 mg ¥ 498 现货
25 mg ¥ 989 现货
50 mg ¥ 1,690 现货
100 mg ¥ 2,690 现货
200 mg ¥ 3,830 现货
1 mL * 10 mM (in DMSO) ¥ 456 现货
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
Venetoclax限时半价
MG-132限时半价
产品目录号及名称: AR-A014418 (T1881)
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纯度: 99.94%
纯度: 98%
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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 AR-A014418 (GSK 3β inhibitor VIII) is an ATP-competitive, and selective GSK3β inhibitor.
靶点活性 GSK-3β:38 nM(Ki)
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)
别名 AR 0133418, GSK-3beta Inhibitor VIII, AR 014418, GSK 3β inhibitor VIII
分子量 308.31
分子式 C12H12N4O4S
CAS No. 487021-52-3

存储

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

溶解度

Ethanol: 1.5 mg/mL (5 mM)

DMSO: 30.8 mg/mL (100 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO 1 mM 3.2435 mL 16.2174 mL 32.4349 mL 81.0872 mL
5 mM 0.6487 mL 3.2435 mL 6.487 mL 16.2174 mL
DMSO 10 mM 0.3243 mL 1.6217 mL 3.2435 mL 8.1087 mL
20 mM 0.1622 mL 0.8109 mL 1.6217 mL 4.0544 mL
50 mM 0.0649 mL 0.3243 mL 0.6487 mL 1.6217 mL
100 mM 0.0324 mL 0.1622 mL 0.3243 mL 0.8109 mL

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TargetMol Library Books参考文献

1. Bhat R, et al. J Biol Chem. 2003, 278(46), 45937-45945. 2. Carter YM, et al. Cancer Biol Ther. 2014, 15(5). 3. Koh SH, et al. Exp Neurol. 2007, 205(2), 336-346. 4. Martins DF, et al. J Pain. 2011, 12(3), 315-322. 5. 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. 6. Tian J, Li X, Zhao L, et al. Glycyrrhizic Acid Promotes Neural Repair by Directly Driving Functional Remyelination[J]. Food & Function. 2019. 7. 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. 8. 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.

TargetMol Library Books文献引用

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.
Tideglusib TBB GSK3-IN-4 GS87 GSK-3 Inhibitor XIII Citric acid trilithium salt tetrahydrate RGB-286638 free base SNS-032

相关化合物库

该产品包含在如下化合物库中:
抑制剂库 高选择性抑制剂库 神经退行性疾病化合物库 激酶抑制剂库 自噬库 Wnt/Hedgehog/Notch 通路化合物库 糖酵解化合物库 代谢化合物库 癌细胞分化化合物库 抗糖尿病库

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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。

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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

AR-A014418 487021-52-3 PI3K/Akt/mTOR signaling Stem Cells GSK-3 AR-A-014418 AR A014418 GSK-3b Inhibitor VIII Glycogen synthase kinase 3 Inhibitor GSK-3β Inhibitor VIII GSK 3beta inhibitor VIII AR-0133418 inhibit AR0133418 Glycogen synthase kinase-3 AR-014418 AR 0133418 AR-A 014418 AR014418 GSK-3beta Inhibitor VIII AR 014418 GSK 3β inhibitor VIII ARA014418 GSK 3b inhibitor VIII inhibitor

 

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