Purvalanol A.

Purvalanol A.用途

Purvalanol A 是一种有效的 CDK 抑制剂,对 cdc2-cyclin B,cdc2-cyclin B,cdk2-cyclin E,cdk4-cyclin D1 和 cdk5-p35 的 IC50 值分别为 4,70,35,850 和 75 nM。

Purvalanol A.名称

[ CAS 号 ]:
212844-53-6

[ 中文名 ]:
Purvalanol A.

[ 英文名 ]:
Purvalanol A

[英文别名 ]:

P01
NG-60
Purvalanol A
Purv

Purvalanol A.生物活性

[ 描述 ]:

Purvalanol A 是一种有效的 CDK 抑制剂,对 cdc2-cyclin B,cdc2-cyclin B,cdk2-cyclin E,cdk4-cyclin D1 和 cdk5-p35 的 IC50 值分别为 4,70,35,850 和 75 nM。

[ 相关类别 ]:

信号通路 >> 自噬 >> 自噬

研究领域 >> 癌症

[ 靶点 ]

cdc2-cyclin B:4 nM (IC50)

cdk2-cyclin E:35 nM (IC50)

cdk2-cyclin A:70 nM (IC50)

cdk4-cyclin D1:850 nM (IC50)

cdk5-p35:75 nM (IC50)

erk1:9000 nM (IC50)

[体外研究]

Purvalanol A抑制cdc28(酿酒酵母)和erk1,IC50为80和9000 nM。 Purvalanol A显示出针对60个人肿瘤细胞系的NCI组的抑制活性,平均GI50为2μM;两种细胞系对purvalanol A的敏感性增加~20倍：GI12为76 nM的KM12结肠癌细胞系和NCI-H522非小细胞肺癌细胞系,GI50为347 nM [1] 。 Purvalanol A是CDK2的2.5倍强效抑制剂,但在低微摩尔范围内也有效抑制DYRK1A和许多其他蛋白激酶。 Purvalanol A抑制MKK1,MAPK2/ERK2,JNK/SAPK1c,IC50分别为80,26,84μM[2]。 Purvalanol A选择性地抑制细胞蛋白的磷酸化。 Purvalanol A可防止血清诱导的G1期进展过程中细胞周期蛋白D和E含量的增加。 Purvalanol A在无细胞条件下不抑制转录[3]。

[参考文献]

[1]. Gray NS, et al. Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors. Science. 1998 Jul 24;281(5376):533-8.

[2]. Bain J, et al. The specificities of protein kinase inhibitors: an update. Biochem J. 2003 Apr 1;371(Pt 1):199-204.

[3]. Villerbu N, et al. Cellular effects of purvalanol A: a specific inhibitor of cyclin-dependent kinase activities. Int J Cancer. 2002 Feb 20;97(6):761-9.

[相关活性小分子]

Purvalanol A.物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
590.5±60.0 °C at 760 mmHg

[ 分子式 ]:
C₁₉H₂₅ClN₆O

[ 分子量 ]:
388.894

[ 闪点 ]:
310.9±32.9 °C

[ 精确质量 ]:
388.177826

[ PSA ]:
87.89000

[ LogP ]:
2.77

[ 外观性状 ]:
粉末

[ 蒸汽压 ]:
0.0±1.7 mmHg at 25°C

[ 折射率 ]:
1.654

[ 储存条件 ]:
−20°C

[ 水溶解性 ]:
methylene chloride: 50 mg/mL, clear, colorless

Purvalanol A.安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

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

[ WGK德国 ]:
3

[ 海关编码 ]:
2933990090

Purvalanol A.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%

Purvalanol A.文献

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Aberrant splicing of the cyclin-dependent kinase-associated phosphatase, KAP, promotes glioblastoma invasion in a Cdc2-dependent manner. However, the mechanism by which this occurs is unknown. Here we...

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