产品说明书

Purvalanol A

Print
Chemical Structure| 212844-53-6 同义名 : NG-60
CAS号 : 212844-53-6
货号 : A106338
分子式 : C19H25ClN6O
纯度 : 99%+
分子量 : 388.894
MDL号 : MFCD02179211
存储条件：

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(128.57 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

无水乙醇: 8 mg/mL(20.57 mM)，配合低频超声助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇
动物实验配方：
生物活性
靶点

  • CDK4

    CDK4/CyclinD1, IC50:850 nM

  • CDK2

    CDK2/CyclinE, IC50:35 nM

    CDK2/CyclinA, IC50:70 nM

  • Cdc

    Cdc2/CyclinB, IC50:4 nM
描述 CDK2 is a serine/threonine-protein kinase involved in the control of the cell cycle; essential for meiosis, but dispensable for mitosis. CDK2 triggers duplication of centrosomes and DNA, acts at the G1-S transition to promote the E2F transcriptional program and the initiation of DNA synthesis, and modulates G2 progression. CDK2 controls the timing of entry into mitosis/meiosis by controlling the subsequent activation of cyclin B/CDK1 by phosphorylation, and coordinates the activation of cyclin B/CDK1 at the centrosome and in the nucleus. Purvalanol A is a CDK2 inhibitor, which inhibits cdc2-cyclin B, cdk2-cyclin A, cdk2-cyclin E, cdk4-cyclin D1, and cdk5-p35 with IC50s of 4, 70, 35, 850, 75 nM, respectively. Based on kinase assays performed in immunoprecipitates, the IC50s of purvalanol A against 2 yeast CDKs (Cdc28p and Pho85p) were 7 μM and 2 μM, respectively[3]. According to a MTT cell viability assay, purvalanol A induced cell viability loss by 50% in MCF-7 cells at the concentration of 25 μM when incubated in vitro for 24h[4].In a spinal cord injury model established in Sprague–Dawley rats, 5 μl of purvalanol A at the concentration of 10 mM in DMSO was immediately injected into the injury site. The results were that purvalanol A restricted compaction of the injury cavity and astrocyte infiltration into the cavity. Purvalanol A treatment also attenuated regenerative responses of anterogradely labeled corticospinal tract axons. Moreover, purvalanol A treatments reduced astrocyte migration and in parallel retarded the extension of spinal axon, observed by the technique of implantation of a polymeric tube into the spinal cord[5].
作用机制 Purvalanol A is a CDK2 inhibitor that acts by blocking the ATP-binding site[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.57mL

0.51mL

0.26mL

12.86mL

2.57mL

1.29mL

25.71mL

5.14mL

2.57mL
参考文献

[1]Obakan P, Arısan ED, et al. Purvalanol A is a strong apoptotic inducer via activating polyamine catabolic pathway in MCF-7 estrogen receptor positive breast cancer cells. Mol Biol Rep. 2014 Jan;41(1):145-54.

[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]Gray NS, Wodicka L, Thunnissen AM, Norman TC, Kwon S, Espinoza FH, Morgan DO, Barnes G, LeClerc S, Meijer L, Kim SH, Lockhart DJ, Schultz PG. Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors. Science. 1998 Jul 24;281(5376):533-8.

[4]Obakan P, Arısan ED, Özfiliz P, Çoker-Gürkan A, Palavan-Ünsal N. Purvalanol A is a strong apoptotic inducer via activating polyamine catabolic pathway in MCF-7 estrogen receptor positive breast cancer cells. Mol Biol Rep. 2014 Jan;41(1):145-54.

[5]Seo TB, Chang IA, Lee JH, Namgung U. Beneficial function of cell division cycle 2 activity in astrocytes on axonal regeneration after spinal cord injury. J Neurotrauma. 2013 Jun 15;30(12):1053-61.