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Zebularine

现货
Catalog No.
A1915
DNA甲基化抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 550.00
现货
10mg
¥ 700.00
现货
50mg
¥ 2,800.00
现货

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Background

Zebularine, a chemically stable cytidine analog containing a 2-(1H)-pyridimidinone ring, is an effective DNA methylation inhibitor which can act with DNA methyltransferases to form a covalent complex. It has been shown to cause demethylation and reactivation of a silenced and hypermethylated p16 gene. Zebularine is able to induce the myogenic phenotype in 10T1/2 cells, which is a phenomenon unique to DNA methylation inhibitors. zebularine can act as a pro-drug leading to inhibition of DNA methylation and gene activation in fungal and mammalian cells. It was the only slightly cytotoxic to T24 cells in vitro. Zebularine is stable in aqueous solution up to a pH of 12.

Reference

C.B. Yoo, J.C. Cheng and P.A. Jones. Zebularine: a new drug for epigenetic therapy. Biochemical Society Transactions. 2004; 32(6): 910 – 912.

Jonathan C. Cheng, Cindy B. Matsen, Felicidad A. Gonzales, Wei Ye, Sheldon Greer, Victor E. Marquez, Peter A. Jones, Eric U. Selker. Inhibition of DNA Methylation and Reactivation of Silenced Genes by Zebularine. Journal of the National Cancer Institute. 2003; 95(5): 399 – 409.

文献引用

1. Griffin PT, Niederhuth CE, Schmitz RJ. "A Comparative Analysis of 5-Azacytidine- and Zebularine-Induced DNA Demethylation." G3 (Bethesda). 2016 Sep 8;6(9):2773-80. PMID:27402357

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt228.2
Cas No.3690-10-6
FormulaC9H12N2O5
SynonymsNSC 309132
Solubility≥8.3mg/mL in DMSO, ≥50.7mg/mL in H2O
Chemical Name1-[(2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]pyrimidin-2-one
SDFDownload SDF
Canonical SMILESC1=CN(C(=O)N=C1)C2C(C(C(O2)CO)O)O
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

10T1/2细胞

制备方法

在DMSO中的溶解度大于10 mM。若配制更高浓度的溶液,一般步骤如下:请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。

反应条件

30 μM;24小时

实验结果

在10T1/2细胞中,Zebularine诱导肌细胞形成。然而,相对于5-Aza-CdR或5-Aza-CR,Zebularine诱导肌细胞形成的作用更弱。

动物实验 [1]:

动物模型

携带EJ6膀胱细胞异种移植物的BALB/c裸鼠

给药剂量

500或1000 mg/kg;腹腔注射或口服

实验结果

在携带EJ6膀胱细胞异种移植物的BALB/c裸鼠中,腹腔注射或口服给予Zebularine (1000 mg/kg) 显著减少肿瘤体积。此外,Zebularine对携带肿瘤的小鼠仅有微弱的细胞毒性。

注意事项

请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。

References:

[1]. Cheng JC, Matsen CB, Gonzales FA, Ye W, Greer S, Marquez VE, Jones PA, Selker EU. Inhibition of DNA methylation and reactivation of silenced genes by zebularine. J Natl Cancer Inst. 2003 Mar 5;95(5):399-409.

生物活性

描述 Zebularine是一种有效的DNA甲基转移酶和胞嘧啶脱氨酶抑制剂。
靶点 DNA Methyltransferases cytidine deaminase        
IC50   2 μM        

质量控制

化学结构

Zebularine

相关生物数据

Zebularine

相关生物数据

Zebularine