阿特波龙

阿特波龙用途

Alsterpaullone (9-Nitropaullone;NSC 705701) 是一种高效的 CDK 抑制剂,作用于 CDK1/cyclin B、CDK2/cyclin A、CDK2/cyclin E 和 CDK5/p35 的 IC50 值分别为 35 nM、15 nM、200 nM 和 40 nM。Alsterpaullone 还是 ATP 竞争性 GSK-3alpha/GSK-3beta 抑制剂,IC50 值为 4 nM,具有抗肿瘤活性,有治疗神经退行性和增生性疾病的潜力。

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阿特波龙名称

[ CAS 号 ]:
237430-03-4

[ 中文名 ]:
阿特波龙

[ 英文名 ]:
Alsterpaullone

[英文别名 ]:

阿特波龙生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 干细胞及 Wnt 通路 >> GSK-3

研究领域 >> 癌症

信号通路 >> 细胞周期/DNA损伤 >> CDK

信号通路 >> PI3K/Akt/mTOR 信号通路 >> GSK-3

[ 靶点 ]

Cdk1/cyclin B:35 nM (IC50)

cdk2/cyclin A:15 nM (IC50)

CDK2/Cyc E:200 nM (IC50)

CDK5/p35:40 nM (IC50)

GSK-3α:4 (IC50)

GSK-3β:4 nM (IC50)

[参考文献]

[1]. Leost M, et al. Paullones are potent inhibitors of glycogen synthase kinase-3beta and cyclin-dependent kinase 5/p25. Eur J Biochem. 2000 Oct;267(19):5983-94.

[2]. Lahusen T, et al. Alsterpaullone, a novel cyclin-dependent kinase inhibitor, induces apoptosis by activation of caspase-9 due to perturbation in mitochondrial membrane potential. Mol Carcinog. 2003 Apr;36(4):183-94.

阿特波龙物理化学性质

[ 密度 ]:
1.5±0.1 g/cm3

[ 沸点 ]:
651.5±45.0 °C at 760 mmHg

[ 分子式 ]:
C₁₆H₁₁N₃O₃

[ 分子量 ]:
293.277

[ 闪点 ]:
347.8±28.7 °C

[ 精确质量 ]:
293.080048

[ PSA ]:
90.71000

[ LogP ]:
3.55

[ 蒸汽压 ]:
0.0±2.0 mmHg at 25°C

[ 折射率 ]:
1.738

[ 储存条件 ]:
-20°C，密闭，干燥

阿特波龙MSDS

详细MSDS(安全技术说明书)

阿特波龙安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H315-H319-H335

[ 警示性声明 ]:
P261-P305 + P351 + P338

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xi: Irritant;

[ 风险声明 (欧洲) ]:
R36/37/38

[ 安全声明 (欧洲) ]:
26-36

[ 危险品运输编码 ]:
NONH for all modes of transport

[ 海关编码 ]:
2933990090

阿特波龙合成路线

详细合成路线

阿特波龙上下游产品

阿特波龙上游产品

阿特波龙下游产品

阿特波龙海关

[ 海关编码 ]: 2933990090

[ 中文概述 ]:
2933990090. 其他仅含氮杂原子的杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

阿特波龙文献

Paullones, a series of cyclin-dependent kinase inhibitors: synthesis, evaluation of CDK1/cyclin B inhibition, and in vitro antitumor activity.

J. Med. Chem. 42 , 2909, (1999)

The paullones represent a novel class of small molecule cyclin-dependent kinase (CDK) inhibitors. To investigate structure-activity relationships and to develop paullones with antitumor activity, deri...

Evidence for antimanic efficacy of glycogen synthase kinase-3 (GSK3) inhibitors in a strain-specific model of acute mania.

Int. J. Neuropsychopharmacol. 14 , 1051-67, (2011)

There is a growing body of evidence suggesting that animal models can be developed to probe the specific domains of bipolar disorder (BD) using the endophenotype approach. Here we tested clinically ac...

Induction of canonical Wnt signaling by alsterpaullone is sufficient for oral tissue fate during regeneration and embryogenesis in Nematostella vectensis.

Dev. Dyn. 240 , 2673-9, (2011)

Although regeneration is widespread among metazoa, the molecular mechanisms have been studied in only a handful of taxa. Of these taxa, fewer still are amenable to studies of embryogenesis. Our unders...

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