• All
  • Primary Antibodies
  • Conjugated Antibodies for IF
  • Conjugated Antibodies for FC
  • Secondary Antibodies
  • Antibody Labeling KitsNew
  • ELISA Kits
  • IHC Kits
  • Magnetic Cell Separation Kits
  • Cytokines & Growth Factors
  • Neutralizing/activating Antibodies
  • Nanobody-based Reagents
  • Accessory Products and Kits
  • Fusion Proteins
×
×
Host
0
Species Reactivity
0
Species Reactivity
0
Conjugate
0
Conjugate
0
Compatible Species
0
Conjugate
0

Zebularine

Zebularine (4-Deoxyuridine) 是一种 DNA 甲基化抑制剂，还抑制胞苷脱氨酶。它通过以共价水合物的形式与活性大小结合，充当胞苷脱氨酶的过渡态类似物抑制剂。

CAS号

3690-10-6

分子式

C9H12N2O5

主要靶点

Autophagy|DNA Methyltransferase

仅限科研使用

Cat No : CM00582

Print datasheet

Synonyms

NSC309132|4-Deoxyuridine

验证数据展示

  • CAS No.: 3690-10-6

    Zebularine
    CAS#: 3690-10-6

产品信息

Zebularine is a DNA methylation inhibitor. Acts as a transition state analog inhibitor of cytidine deaminase by binding to the active size as covalent hydrates. It also inhibits cytidine deaminase (Ki: 2 μM, in a cell-free assay).

CAS号 3690-10-6
分子式 C9H12N2O5
主要靶点 Autophagy|DNA Methyltransferase
主要通路 表观遗传|自噬
分子量 228.2
纯度 99.84%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 NSC309132|4-Deoxyuridine

靶点活性

Cytidine deaminase:2 μM(Ki)

体内活性

Zebularine可与细菌甲基转移酶形成紧密共价复合物。作用于N. crassa时,Zebularine使DNA甲基化受到抑制,并使甲基化导致的沉默基因被重新激活。作用于T24膀胱癌细胞时,Zebularine使沉默的p16基因被重新激活,且使其启动子区域去甲基化。Zebularine对T24细胞只有轻微的细胞毒性。与正常成纤维细胞相比,Zebularine会优先掺入癌细胞系的DNA,且更大程度抑制其细胞生长与基因表达。此外,与正常成纤维细胞相比,Zebularine会首先抑制癌细胞的DNA甲基转移酶1,并诱导癌症相关的抗原基因表达。

体外活性

Zebularine（1000 mg/kg）对携带肿瘤的小鼠具有轻微细胞毒性,平均最大重量变化为11％（95％可信区间：4％-19％）.与对照组相比,高剂量Zebularine（i.p/p.o.）处理可显著减小小鼠的肿瘤体积.

溶解度

DMSO:22.8 mg/mL (100 mM),H2O:22.8 mg/mL (100 mM)

细胞实验

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[2].

参考文献

1.Zhou L, et al. J Mol Biol, 2002, 321(4), 591-599.
2.Lemaire M, et al. Cancer Chemother Pharmacol, 2009, 63(3), 411-416.
3.Cheng JC, et al. J Natl Cancer Inst, 2003, 95(5), 399-409.
4.Cheng JC, et al. Cancer Cell, 2004, 6(2), 151-158.

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
=
×
×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
×
=
×
C1   V1   C2   V2