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。

点击显示

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

Phosphoproteomic Analysis of Aurora Kinase Inhibition in Monopolar Cytokinesis.

J. Proteome Res. 14 , 4087-98, (2015)

Cytokinesis is the last step of the cell cycle that requires coordinated activities of the microtubule cytoskeleton, actin cytoskeleton, and membrane compartments. Aurora B kinase is one of the master...

Involvement of atypical transcription factor E2F8 in the polyploidization during mouse and human decidualization.

Cell Cycle 14 , 1842-58, (2015)

Polyploid decidual cells are specifically differentiated cells during mouse uterine decidualization. However, little is known about the regulatory mechanism and physiological significance of polyploid...

KAP regulates ROCK2 and Cdk2 in an RNA-activated glioblastoma invasion pathway.

Oncogene 34(11) , 1432-41, (2015)

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...

更多文献