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AR-A014418

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。

CAS号

487021-52-3

分子式

C12H12N4O4S

主要靶点

GSK-3

仅限科研使用

Cat No : CM04320

Print datasheet

Synonyms

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

验证数据展示

  • CAS No.: 487021-52-3

    AR-A014418
    CAS#: 487021-52-3

产品信息

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

CAS号 487021-52-3
分子式 C12H12N4O4S
主要靶点 GSK-3
主要通路 PI3K/Akt/mTOR信号通路|干细胞
分子量 308.31
纯度 99.94%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 GSK-3beta Inhibitor VIII|AR 014418|GSK 3β inhibitor VIII|AR 0133418

靶点活性

GSK-3β:38 nM(Ki)

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。

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.

溶解度

Ethanol:1.5 mg/mL (5 mM),DMSO:30.8 mg/mL (100 mM)

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)

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.

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