AR-A014418|487021-52-3|(AR 0133418; GSK 3β inhibitor VIII; AR 014418)-陌孚医药/Medlife

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AR-A014418 (Synonyms: AR 0133418; GSK 3β inhibitor VIII; AR 014418)

目录号: PL01509 纯度: ≥99%

CAS No. :487021-52-3

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中文名称	AR-A014418
中文别名	AR-A014418 抑制剂;N-(4-甲氧基苄基)-N'-(5-硝基-1,3-噻唑-2-基)脲;N-(4-甲氧基苄基)-N-(5-硝基-1,3-噻唑-2-基)脲;茚草酮;GSK-3BETA 抑制剂 VIII
英文名称	AR-A014418
英文别名	AR-A014418;GSK-3β Inhibitor VIII;N-[(4-Methoxyphenyl)methyl]-N'-(5-nitro-2-thiazolyl)urea;N-[(4-Methoxyphenyl)Methyl]-N'-(5-nitro-thiazol-2-yl)urea;AR-AO 14418;1-[(4-methoxyphenyl)methyl]-3-(5-nitro-1,3-thiazol-2-yl)urea;GSK3β Inhibitor VIII;SN 4521;1q5k;AR 0133418;AR 014418;GSK 3β inhibitor;GSK-3 Inhibitor VIII;GSK-3beta Inhibitor VIII;Kinome_1268;N-(4-Methoxybenzyl)-N'-(5-nitro-1,3-thiazol-2-yl)urea;N-(4-Methoxybenzyl)-N′-(5-nitro-1,3-thiazol-2-yl)urea;GSK 3B Inhibitor VIII;GSK 3beta inhibitor VIII;1-(4-methoxybenzyl)-3-(5-nitrothiazol-2-yl)urea;GSK-3;A Inhibitor VIII;87KSH90Q6D;AK175829;InSolution™ GSK-3beta Inhibitor VIII;C12H12N4O4S;N-(4-Methoxybenzyl)-N′-(5-nitro-1,3-thiazol-2-yl)urea
Cas No.	487021-52-3
分子式	C₁₂H₁₂N₄O₄S
分子量	308.31
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	AR-A014418 是一种有效，选择性，ATP 竞争性的 GSK3β 抑制剂 (IC₅₀=104 nM; K_i=38 nM)。
生物活性	AR-A014418 is a potent, selective and ATP-competitive GSK3β inhibitor (IC 50 =104 nM; K i =38 nM).
性状	Solid
IC50 & Target[1][2]	GSK-3β 104 nM (IC50)
体外研究(In Vitro)	AR-A014418 blocks the phosphorylation of tau at a GSK3-specific site (Ser-396) in 3T3 fibroblasts expressing human four-repeat tau protein, with an IC50 of 2.7 μM, and protects cultured N2A cells from death cuased by PI3K/PKB pathway blockage. AR-A014418 also shows inhibitory effect on neurodegeneration mediated by beta-amyloid peptide in hippocampal slices. AR-A014418 decreases neuroendocrine markers and suppresses neuroblastoma cell growth in NGP and SH-5Y-SY cells. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	AR-A014418 (0-4 mg/kg, i.p.) delays the onset of symptoms, enhances motor activity, blocks disease progression, and postpons the endpoint of the disease in ALS mouse model with the G93A mutant human SOD1. Furthermore, AR-A014418 suppresses acetic acid- and formalin-induced nociception in mice via modulating NMDA and metabotropic receptor signaling as well as TNF-α and IL-1β transmission in the spinal cord. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[1]. Bhat R, Xue Y, Berg S, Structural insights and biological effects of glycogen synthase kinase 3-specific inhibitor AR-A014418. J Biol Chem. 2003 Nov 14;278(46):45937-45. [2]. Carter YM, et al. Specific glycogen synthase kinase-3 inhibition reduces neuroendocrine markers and suppresses neuroblastoma cell growth. Cancer Biol Ther. 2014 May;15(5):510-5.

溶解度数据	In Vitro: DMSO : ≥ 100 mg/mL (324.35 mM)配制储备液

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1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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