化合物 AR-A014418|T1881|TargetMol

AR-A014418
487021-52-3

￥415 5mg 起订

￥498 10mg 起订

￥989 25mg 起订

上海更新日期：2024-09-29

TargetMol中国（陶术生物）

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联系人：邵小姐

手机：4008200310 拨打

邮箱：marketing@tsbiochem.com

产品详情:

中文名称：: 化合物 AR-A014418

英文名称：: AR-A014418

CAS号：: 487021-52-3

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: ≥95%

产品类别：: 抑制剂

货号：: T1881

Product Introduction

Bioactivity

Name	AR-A014418
Description	AR-A014418 (GSK 3β inhibitor VIII) is an ATP-competitive, and selective GSK3β inhibitor.
Cell Research	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)
Kinase Assay	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.
In vitro	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.
In vivo	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。
Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
Solubility Information	Ethanol : 1.5 mg/mL (5 mM) DMSO : 30.8 mg/mL (100 mM)
Keywords	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-A 014418 \| AR014418 \| AR-A014418 \| GSK-3 \| ARA014418 \| GSK 3b inhibitor VIII
Inhibitors Related	Cromolyn sodium \| Ginsenoside Rg2 \| 4-Chloro-2'-bromoacetophenone \| CHIR-99021 HCl \| AT7519 \| 5-Bromoindole \| GSK-3 Inhibitor 5 \| GSK 3 Inhibitor IX \| SNS-032 \| Cyanoacetohydrazide \| CHIR-99021 \| 1-Azakenpaullone
Related Compound Libraries	Neuroprotective Compound Library \| Inhibitor Library \| Anti-Breast Cancer Compound Library \| Bioactive Compound Library \| Bioactive Compounds Library Max \| Kinase Inhibitor Library \| Anti-Aging Compound Library \| Highly Selective Inhibitor Library \| Stem Cell Differentiation Compound Library \| Anti-Neurodegenerative Disease Compound Library

GSK-3beta Inhibitor VIII|||GSK 3β inhibitor VIII|||AR 014418|||AR 0133418|TargetMol

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

成立日期	(12年)
注册资本	566.265100万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,工厂,试剂,定制,服务
主营行业	天然产物,生化试剂,分子生物学,分子砌块,生物技术服务