Alsterpaullone - CAS:237430-03-4

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Alsterpaullone (Synonyms:9-Nitropaullone; NSC 705701)

目录号 : KM7391 CAS No. : 237430-03-4 纯度 : ≥98%

Data Sheet 产品使用指南

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 IC₅₀s 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 IC₅₀s 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.

体外研究

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.

Cell Viability Assay

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

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.

Western Blot Analysis

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

Alsterpaullone (30 mg/kg, s.c., daily for 2 weeks) reduces tumor growth and increases survival in medulloblastoma xenografts.

Animal Model:	5-6 week old athymic nude mice
Dosage:	30 mg/kg
Administration:	Subcutaneous injections, daily for 2 weeks
Result:	Antitumor effect in Group 3 medulloblastomas.

分子式

C₁₆H₁₁N₃O₃

分子量

293.28

CAS号

237430-03-4

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

纯度： ≥98%

Data Sheet

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