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)。
| 生物活性 | Alsterpaullone (9-Nitropaullone) is a potentCDKinhibitor, withIC50s of 35 nM, 15 nM, 200 nM and 40 nM forCDK1/cyclin B,CDK2/cyclin A,CDK2/cyclin EandCDK5/p35, respectively. Alsterpaullone also competes with ATP for binding to GSK-3alpha/GSK-3beta withIC50s of both 4 nM. Alsterpaullone has antitumor activity, and possesses potential for the study in neurodegenerative and proliferative disorders[1]. Alsterpaullone inducesapoptosisin leukemia cell line[2]. |
| IC50& Target[1] | 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) |
|
体外研究
(In Vitro) | Alsterpaullone (0.3, 1, 3 μM; 8 hours) induces apoptosis in leukemia cell line[2].
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[3].
Alsterpaullone (20 μM) induces cell death depending on caspase activity[3].
Cell Viability Assay[3] | Cell Line: | HeLa cells | | Concentration: | 5, 10, 15, 20, 25, 30 μM | | Incubation Time: | 48 and 72 hours | | Result: | The growth of HeLa cells was inhibited in a dose-dependent manner for 48 h and 72 h ranging from 0 to 30 μM. |
Apoptosis Analysis[2] | Cell Line: | Jurkat cell line | | Concentration: | 0.3, 1, 3 μM | | Incubation Time: | 8 hours | | Result: | Induced dose-dependent apoptosis. 1 μM was sufficient to cause apoptosis, 3 μM demonstrated maximal apoptotic effects[2]. |
Western Blot Analysis[3] | Cell Line: | HeLa cells | | Concentration: | 2, 4, 6, 12, 24 hours | | Incubation Time: | 8 hours | | Result: | The cleavage of PARP started at 4 h, while the activation of caspase-3 occurred at 2 h. |
|
体内研究
(In Vivo) | Alsterpaullone (30 mg/kg, s.c., daily for 2 weeks) reduces tumor growth and increases survival in medulloblastoma xenografts[4].
| Animal Model: | 5-6 week old athymic nude mice[4] | | Dosage: | 30 mg/kg | | Administration: | Subcutaneous injections, daily for 2 weeks | | Result: | Antitumor effect in Group 3 medulloblastomas. |
|
| 分子量 | |
| 性状 | |
| Formula | |
| CAS 号 | |
| 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 | | In solvent | -80°C | 6 months | | -20°C | 1 month |
|
m.cnreagent.com