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3-Deazaneplanocin,DZNep
S-腺苷高半胱氨酸和EZH2抑制剂。

3-Deazaneplanocin,DZNep

产品编号:A1905
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Sample solution is provided at 25 µL, 10mM.

引用文献

质量控制

质量控制和MSDS

批次:

化学结构

3-Deazaneplanocin,DZNep

相关生物数据

3-Deazaneplanocin,DZNep

相关生物数据

3-Deazaneplanocin,DZNep

相关生物数据

3-Deazaneplanocin,DZNep

相关生物数据

3-Deazaneplanocin,DZNep

相关生物数据

3-Deazaneplanocin,DZNep

相关生物数据

3-Deazaneplanocin,DZNep

相关生物数据

3-Deazaneplanocin,DZNep

3-Deazaneplanocin,DZNep Dilution Calculator

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化学性质

CAS号 102052-95-9 SDF Download SDF
别名 DZNep, 3-Deazaneplanocin A,NSC 617989,NSC617989
化学名 (1S,2R,5R)-5-(4-aminoimidazo[4,5-c]pyridin-1-yl)-3-(hydroxymethyl)cyclopent-3-ene-1,2-diol
SMILES C1=CN=C(C2=C1N(C=N2)C3C=C(C(C3O)O)CO)N
分子式 C12H24N4O3 分子量 262.26
溶解度 Soluble in Water 储存条件 Store at -20°C
物理性状 A crystalline solid 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。

生物活性

描述 3-deazaneplanocin A (DZNeP),腺苷类似物,是S-腺苷高半胱氨酸水解酶(S-adenosylhomocysteine hydrolase)的竞争性抑制剂,Ki值为50 pM。
靶点 S-adenosylhomocysteine hydrolase          
IC50 50 pM (Ki)          

实验操作

细胞实验[1]:

细胞系

人急性骨髓性白血病(AML)细胞

溶解方法

在DMSO中的溶解度>10 mM。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

100-750 nM;24-72 h

应用

在培养的和原代AML细胞中,DZNep诱导细胞凋亡。在AML HL-60和OCI-AML3细胞中,DZNep耗尽EZH2水平,抑制组蛋白H3赖氨酸27(H3K27)的三甲基化。在cyclin E和HOXA9水平耗尽之后,DZNep诱导p16、p21、p27和FBXO32的水平。

动物实验[2]:

动物模型

Sprague-Dawley大鼠(120-140 g)

剂量

5 μM;实验前24小时处理,随饮食口服。

应用

在非酒精性脂肪性肝病(NAFLD)小鼠模型中,DZNep显著减少EZH2的表达和活性,增加脂质沉积、炎症分子和microRNAs。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。

References:

1. Fiskus W1, Wang Y, Sreekumar A et al. Combined epigenetic therapy with the histone methyltransferase EZH2 inhibitor 3-deazaneplanocin A and the histone deacetylase inhibitor panobinostat against human AML cells. Blood. 2009 Sep 24;114(13):2733-43.

2. Vella S, Gnani D, Crudele A et al. EZH2 down-regulation exacerbates lipid accumulation and inflammation in vitro and in vivo NAFLD.Int J Mol Sci. 2013 Dec 12;14(12):24154-68.

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研究更新

1. Cell-based proteome profiling using an affinity-based probe (AfBP) derived from 3-deazaneplanocin A (DzNep). Chem Asian J. 2013 Aug;8(8):1818-28. doi: 10.1002/asia.201300303. Epub 2013 Jun 7.
Abstract
A novel probe derived from DzNep, an inhibitor of histone methylation, was used to identify potential cellular targets of DzNep in living mammalian cells.
2. 3-Deazaneplanocin A (DZNep), an inhibitor of S-adenosyl-methionine-dependent methyltransferase, promotes erythroid differentiation. J Biol Chem. 2014 Feb 3. [Epub ahead of print]
Abstract
DZNep significantly induced erythroid differentiation in K562 cells and human primary erythroblasts derived from cord blood CD34-positive cells and reduced levels of ETO2 protein in K562 cells, which indicates DZNep induced erythroid differentiation may be partially attributed to its inhibition of ETO2 rather than EZH2 inhibition.
3. PRIMA-1, a Mutant p53 Reactivator, Restores the Sensitivity of TP53 Mutant-type Thyroid Cancer Cells to the Histone Methylation Inhibitor 3-Deazaneplanocin A (DZNep). J Clin Endocrinol Metab. 2014 Feb 10:jc20133147. [Epub ahead of print]
Abstract
DZNep inhibited the growth of TP53 wild-type cells by promoting p53 protein accumulation and activating p53 pathways and failed to inhibit the growth of TP53 mutant-type cells, even though DZNep induced EZH2 depletion and H3K27me3 histone mark reduction were observed in both thyroid cancer cells. However, the combination of DZNep/PRIMA-1 restored the sensitivity of TP53 mutant-type cells to DZNep by reactivating p53.
5. Epigenetic therapy with the histone methyltransferase EZH2 inhibitor 3-deazaneplanocin A inhibits the growth of cholangiocarcinoma cells. Oncol Rep. 2014 Feb;31(2):983-8. doi: 10.3892/or.2013.2922. Epub 2013 Dec 13.
Abstract
DZNep depleted EZH2, inhibited histone lysine 27 trimethylation and suppressed proliferation partially through upregulation of p16INK4a and p17KIP1 in cholangiocarcinoma cell lines RBE and TFK-1 resulting in induced G1 arrest and apoptosis.

产品描述

3- Deazaneplanocin是一种高效的S-腺苷高半胱氨酸水解酶抑制剂,Ki值为0.05 nM[1]。

3- Deazaneplanocin是腺苷的类似物,与底物腺苷竞争抑制S-腺苷高半胱氨酸水解酶。3-Deazaneplanocin对细胞生长的抑制作用较弱。在HL-60细胞中,10 μM的3-Deazaneplanocin处理只能适度减少细胞的生长。在HCC肝癌细胞系Huh1和Huh7中,3-Deazaneplanocin剂量依赖性地抑制细胞的生长和非粘附球的形成。在Huh1细胞中,3-Deazaneplanocin将上皮细胞粘附分子EpCAM从49.0%减少到12.5%。在Huh7细胞中,3-Deazaneplanocin将EpCAM从44.4%减少到11.6%。在异种移植Huh7细胞的小鼠中,3-Deazaneplanocin通过直接影响肿瘤起始细胞的生长和自我更新,从而抑制肿瘤的发生和生长[1, 2]。

参考文献:
[1] Glazer R I, Hartman K D, Knode M C, et al.  3-Deazaneplanocin: a new and potent inhibitor of S-adenosylhomocysteine hydrolase and its effects on human promyelocytic leukemia cell line HL-60. Biochemical and biophysical research communications, 1986, 135(2): 688-694.
[2] Chiba T, Suzuki E, Negishi M, et al.  3-Deazaneplanocin A is a promising therapeutic agent for the eradication of tumor-initiating hepatocellular carcinoma cells. International Journal of Cancer, 2012, 130(11): 2557-2567.