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Zebularine(NSC309132 4-Deoxyuridine)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Zebularine(NSC309132 4-Deoxyuridine)图片
CAS NO:3690-10-6
规格:≥98%
包装与价格:
包装价格(元)
50mg电议
100mg电议
250mg电议
500mg电议
1g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)228.2
FormulaC9H12N2O5
CAS No.3690-10-6
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 46 mg/mL (201.6 mM)
Water: 46 mg/mL (201.6 mM)
Ethanol:<1 mg/mL
Solubility (In vivo)Saline: 30 mg/mL
SynonymsZebularine; NSC-309132; NSC 309132; NSC309132; 4-Deoxyuridine; 4 Deoxyuridine
实验参考方法
In Vitro

In vitro activity: Zebularine is a cytidine analogue containing a 2-(1H)-pyrimidinone ring, originally synthesized as a cytidine deaminase inhibitor. Zebularine is shown to form a tight, covalent complex with bacterial methyltransferases. In N. crassa, zebularine inhibits DNA methylation and reactivates a gene previously silenced by methylation. Zebularine is a global inhibitor of DNA methylation, similar to 5-Aza-CR, rather than a selective inhibitor. Zebularine induces the myogenic phenotype in 10T1/2 cells, which is a phenomenon unique to DNA methylation inhibitors. Zebularine reactivates a silenced p16 gene and demethylates its promoter region in T24 bladder carcinoma cells. Zebularine is only slightly cytotoxic to T24 cells. Zebularine is preferentially incorporated into DNA and exhibits greater cell growth inhibition and gene expression in cancer cell lines compared to normal fibroblasts. In addition, zebularine preferentially depletes DNA methyltransferase 1 (DNMT1) and induces expression of cancer-related antigen genes in cancer cells relative to normal fibroblasts.


Cell Assay: For methylation analysis, 10T1/2 cells and T24 cells are treated with the various concentrations of zebularine. For 10T1/2 cells, the medium is changed 24 hours after the initial drug treatment, whereas for T24 cells, the medium is changed 24 hours or 48 hours after the initial drug treatment. DNA and RNA are harvested from 10T1/2 cells 72 hours after initial drug treatment and from T24 cells 96 hours after initial drug treatment. The methylation status of the indicated DNA regions is measured in two separate and independent experiments, both of which are done in duplicate.

In VivoZebularine is only slightly cytotoxic to tumor-bearing mice (average maximal weight change in mice treated with 1000 mg/kg zebularine = 11% [95% CI = 4% to 19%]). Compared with those in control mice, tumor volumes are statistically significantly reduced in mice treated with high-dose zebularine administered by intraperitoneal injection or by oral gavage.
Animal model Male BALB/c nu/nu mice
Formulation & Dosage Dissolved in 0.45% saline; 500 mg/kg, 1000 mg/kg; i.p. and p.o.
ReferencesFASEB J. 2000 Nov;14(14):2339-44; Cancer Res. 2010 Aug 1;70(15):6268-76.