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产品总数：60950
| 中文名称 |
Alsterpaullone
|
|---|---|
| 中文别名 |
9-硝基-7,12-二氢吲哚o[3,2-d][1]苯并氮杂卓-6(5H)-酮
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| 英文名称 |
Alsterpaullone
|
| 英文别名 |
Indolo[3,2-d][1]benzazepin-6(5H)-one,7,12-dihydro-9-nitro-;Alsterpaullone;9-nitro-7,12-dihydro-5H-indolo[3,2-d][1]benzazepin-6-one;9-Nitro-7,12-dihydroindolo-[3,2-d][1]benzazepin-6(5)-one;9-Nitropaullone;NSC 705701
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| Cas No. |
237430-03-4
|
| 分子式 |
C16H11N3O3
|
| 分子量 |
293.28
|
| 包装储存 |
Powder -20°C 3 years；4°C 2 years
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| 产品详情 |
Alsterpaullone (9-Nitropaullone) 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 是 ATP 竞争性的 GSK-3alpha/GSK-3beta 抑制剂，且作用的 IC50 值都为 4 nM。Alsterpaullone 具有抗肿瘤活性，有用于神经退行性和增生性疾病研究的潜力。Alsterpaullon 诱导白血病细胞凋亡 (apoptosis)。
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|---|---|
| 生物活性 |
Alsterpaullone (9-Nitropaullone) is a potent CDK inhibitor, with IC 50 s of 35 nM, 15 nM, 200 nM and 40 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E and CDK5/p35, respectively. Alsterpaullone also competes with ATP for binding to GSK-3alpha/GSK-3beta with IC 50 s of both 4 nM. Alsterpaullone has antitumor activity, and possesses potential for the study in neurodegenerative and proliferative disorders. Alsterpaullone induces apoptosis in leukemia cell line.
|
| 性状 |
Solid
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| IC50 & Target[1][2] |
Cdk1/cyclin B 35 nM (IC50) cdk2/cyclin A 1
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| 体外研究(In Vitro) |
Alsterpaullone (0.3, 1, 3 μM; 8 hours) induces apoptosis in leukemia cell line.Alsterpaullone (5, 10, 15, 20, 25, 30 μM; 48 and 72 hours) inhibits the growth of HeLa cells in dose-and time-dependent manner. Treatment with Alsterpaullone causes a time-dependent inhibition of cell growth too. Alsterpaullone (20?μM) induces cell death depending on caspase activity. has not independently confirmed the accuracy of these methods. They are for reference only.
Alsterpaullone (30 mg/kg, s.c., daily for 2 weeks) reduces tumor growth and increases survival in medulloblastoma xenografts. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: 5-6 week |
| 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]. 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.
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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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