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。

产品编号 T2169Cas号 3690-10-6

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Zebularine

产品编号 T2169别名 NSC309132, 4-DeoxyuridineCas号 3690-10-6

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规格	价格	库存
1 mg	¥ 137	现货
5 mg	¥ 289	现货
10 mg	¥ 469	现货
25 mg	¥ 987	现货
50 mg	¥ 1,820	现货
100 mg	¥ 2,730	现货
500 mg	¥ 6,290	现货
1 mL x 10 mM (in DMSO)	¥ 318	现货

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"Zebularine"的相关化合物库

产品介绍

生物活性

产品描述	Zebularine (4-Deoxyuridine) 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).
靶点活性	Cytidine deaminase:2 μM(Ki)
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.
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。
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].
别名	NSC309132, 4-Deoxyuridine

化学信息

分子量	228.2
分子式	C₉H₁₂N₂O₅
CAS No.	3690-10-6

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

溶解度信息

DMSO: 60 mg/mL (262.93 mM)

H2O: 22.8 mg/mL (100 mM)

溶液配制表

H2O/DMSO

	1mg	5mg	10mg	50mg
1 mM	4.3821 mL	21.9106 mL	43.8212 mL	219.1060 mL
5 mM	0.8764 mL	4.3821 mL	8.7642 mL	43.8212 mL
10 mM	0.4382 mL	2.1911 mL	4.3821 mL	21.9106 mL
20 mM	0.2191 mL	1.0955 mL	2.1911 mL	10.9553 mL
50 mM	0.0876 mL	0.4382 mL	0.8764 mL	4.3821 mL
100 mM	0.0438 mL	0.2191 mL	0.4382 mL	2.1911 mL