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CAS No.: 212844-54-7

Purvalanol B Catalog No. CSN16119

Synonyms: NG 95

Purvalanol B is a selective cyclin-dependent kinases (CDKs) inhibitor with IC50 values of 6, 6, 9, > 10,000, and 6 nM for cdc2/cyclin B, cdk2/cyclin A, cdk2/cyclin E, cdk4/cyclin D1 and cdk5-p35 respectively.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 cdk4/cyclin D1

IC50:10,000nM CDK1

IC50:6nM CDK2/cyclin A

IC50:6nM CDK5/p35

IC50:6nM CDK2/cyclin E

IC50:9nM
描述The cyclin-dependent kinases (CDKs) have a central role in coordinating the eukaryotic cell division cycle, and also serve to integrate diverse growth-regulatory signals^[3]. Purvalanol B has been recently optimized for activity against CDK1/cyclin B^[4]. While control cultures were composed of mostly multinucleated cells, the inhibitor-treated cultures contained predominantly parasites with only one nucleus, thus indicating parasites were unable to undergo schizogony after the 12-hour exposure to Purvalanol B in DMSO. Synchronized blood stage cultures of P. falciparum at 24 hours post-invasion were treated with 29.8 μM Purvalanol B for 12 hours. Transcript levels of proteasome component C8 were up-regulated in Purvalanol B-treated cultures compared to control cultures. Additionally, subunit of proteasome activator complex, proteasome subunit α type, and thioredoxin reductase 2, the protein levels of which were all up-regulated in treated group. These data indicated that Purvalanol B application decreased the ability of late-stage P. falciparum trophozoites to form multinucleated schizonts and up-regulates proteasome subunits and proteins that contribute to redox homeostasis^[5].
作用机制Purvalanol B reversibly inhibits CDKs, by competing with ATP for binding to the catalytic site of the kinase. The N6 position of its purine acts as a donor in an essential hydrogen bond between Purvalanol B and the kinase Leu83 residue.
动物研究
剂量
Mice: 20 mg/kg^[3] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	Mice: 20 mg/kg^[3] (i.p.)
给药途径	i.p.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.3100 mL
- 11.5499 mL
- 23.0998 mL
- 5 mM
- 0.4620 mL
- 2.3100 mL
- 4.6200 mL
- 10 mM
- 0.2310 mL
- 1.1550 mL
- 2.3100 mL

技术信息

CAS号

212844-54-7

储存条件

粉末: Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H25ClN6O3

运输

蓝冰

分子量

432.90

别名

NG 95

溶解度

DMSO	86.0 mg/mL (198.7 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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靶点	Description	IC50
cdk4/cyclin D1		IC50:10,000nM
CDK1		IC50:6nM
CDK2/cyclin A		IC50:6nM
CDK5/p35		IC50:6nM
CDK2/cyclin E		IC50:9nM

Purvalanol B Catalog No. CSN16119

靶点选择性

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