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Zebularine泽布拉林,3690-10-6

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  • ¥350 - 3300
  • MedChemExpress(MCE)已认证
  • 美国
  • HY-13420
  • 2025年12月05日
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    • 详细信息
    • 文献和实验
    • 技术资料
    • 保存条件

      Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.

    • 英文名

      NSC309132; 4-Deoxyuridine

    • 库存

      货期:1-2天

    • 供应商

      MedChemExpress LLC

    • CAS号

      3690-10-6

    • 规格

      10 mM * 1 mL/5 mg/10 mg/50 mg/100 mg

    规格:10 mM * 1 mL产品价格:¥385.0
    规格:5 mg产品价格:¥350.0
    规格:10 mg产品价格:¥570.0
    规格:50 mg产品价格:¥2200.0
    规格:100 mg产品价格:¥3300.0

    MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务。

    Zebularine

    CAS No. : 3690-10-6

    MCE 国际站:Zebularine

    产品活性:Zebularine (NSC309132; 4-Deoxyuridine)是DNA甲基转移酶抑制剂;也可抑制胞苷脱氨酶Ki值为0.95 μM。

    研究领域:Epigenetics  |  Autophagy

    作用靶点:DNA Methyltransferase  |  Autophagy

    In Vitro: Zebularine exerts its demethylation activity by stabilizing the binding of DNMTs to DNA, hindering the methylation and decreasing the dissociation, thereby trapping the enzyme and preventing turnover even at other sites. zebularine enhances tumor cell chemo- and radiosensitivity? and has antimitogenic and angiostatic activities. Zebularine inhibits DNA methylation and reactivates a gene previously silenced by methylation. 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 demethylated its promoter region in T24 bladder carcinoma cells. Zebularine treatment inhibits cell growth in a dose and time dependent manner with an IC50 of ~100 μM and 150 μM in MDA-MB-231 and MCF-7 cells, respectively, on 96 h exposure. At high doses zebularine induced changes in apoptotic proteins in a cell line specific manner manifested by alteration in caspase-3, Bax, Bcl2 and PARP cleavage. Zebularine is also a potent competitive inhibitor of the enzyme CR deaminase. The Ki for zebularine is 0.95μM.

    In Vivo: Zebularine is only slightly cytotoxic to tumor-bearing mice. 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. Zebularine also enhances the survival time of mice with L1210 leukemia treated with 5-AZA-CdR. About 27% of the mice treated with this drug combination has a survival time longer than the mice treated with only 5-AZA-CdR.

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    ¥350 - 3300