Purvalanol B

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Chemical Structure| 212844-54-7 同义名 : NG 95
CAS号 : 212844-54-7
货号 : A176253
分子式 : C20H25ClN6O3
纯度 : 99%+
分子量 : 432.904
MDL号 : N/A
存储条件：

Pure form Keep in dark place,Sealed in dry,Store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 40 mg/mL(92.4 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
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.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.31mL

0.46mL

0.23mL

11.55mL

2.31mL

1.15mL

23.10mL

4.62mL

2.31mL
参考文献

[1]Knockaert M, Lenormand P, et al. p42/p44 MAPKs are intracellular targets of the CDK inhibitor purvalanol. Oncogene. 2002 Sep 19;21(42):6413-24.

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

[3]Pavletich NP. Mechanisms of cyclin-dependent kinase regulation: structures of Cdks, their cyclin activators, and Cip and INK4 inhibitors. J Mol Biol. 1999 Apr 16;287(5):821-8. doi: 10.1006/jmbi.1999.2640. PMID: 10222191.

[4]Knockaert M, Lenormand P, Gray N, Schultz P, Pouysségur J, Meijer L. p42/p44 MAPKs are intracellular targets of the CDK inhibitor purvalanol. Oncogene. 2002 Sep 19;21(42):6413-24. doi: 10.1038/sj.onc.1205908. PMID: 12226745.

[5]Bullard KM, Broccardo C, Keenan SM. Effects of cyclin-dependent kinase inhibitor Purvalanol B application on protein expression and developmental progression in intra-erythrocytic Plasmodium falciparum parasites. Malar J. 2015 Apr 8;14:147. doi: 10.1186/s12936-015-0655-x. PMID: 25879664; PMCID: PMC4403934.