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3-Deazaneplanocin A (DZNep) hydrochloride

现货
Catalog No.
A8182
SAHH和EZH2抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 2,960.00
现货
1mg
¥ 800.00
现货
5mg
¥ 3,500.00
现货
10mg
¥ 5,000.00
现货
25mg
¥ 9,000.00
现货

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Background

3-Deazaneplanocin A (DZNep) hydrochloride is a selective inhibitor of ENZ2 inhibitor with IC50 value of 0.08-0.24 μM [1].
ENZ2 is a sub-unit of PRC2 and plays an important role in regulating cell proliferation and cell-cycle progression. It has been reported that ENZ2 is over-expressed in many tumors, including prostate, breast, bladder cancers and AML [2]. In HepG2 cell lines, DZNep treatment markedly induced the intracellular lipids increasement and TNF-αand TGF-βexpression in mRNA level by augmenting PA/OA-dependent lipid accumulation [3].
DZNep is a potent ENZ2 inhibitor. When tested with human acute myeloid leukemia (AML) HL-60 and OCI-AML3 cell lines, administration of DZNep induced cell apoptosis by depleting ENZ2, cyclin E and HOXA9 expressions and inducing p16, p21,p27 and FBXO32 expressions in a dose-dependent manner [2].
In high-fat/high-fructose diet fed (HFa/HFr-D) rat mouse model that resembles human NAFLD metabolically and histologically, DZNep functioned as the effective agent to anti-inflammatory and anti-fibrotic roles by inhibiting ENZ2 [3].
It is also reported that DZNep has the inhibitory activity for (SAHH (S-adenosylhomocysteine hydrolase) with Ki value of 50 pM [4].
References:
[1].    Kikuchi, J., et al., Epigenetic therapy with 3-deazaneplanocin A, an inhibitor of the histone methyltransferase EZH2, inhibits growth of non-small cell lung cancer cells. Lung Cancer, 2012. 78(2): p. 138-43.
[2].    Fiskus, W., 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. 114(13): p. 2733-43.
[3].    Vella, S., et al., EZH2 down-regulation exacerbates lipid accumulation and inflammation in in vitro and in vivo NAFLD. Int J Mol Sci, 2013. 14(12): p. 24154-68.
[4].    Glazer, R.I., et al., 3-Deazaneplanocin A: a new inhibitor of S-adenosylhomocysteine synthesis and its effects in human colon carcinoma cells. Biochem Pharmacol, 1986. 35(24): p. 4523-7.

文献引用

1. Hu W, Jia X, et al. "Chaetospirolactone reverses the apoptotic resistance towards TRAIL in pancreatic cancer." Biochem Biophys Res Commun. 2017 Oct 28. pii: S0006-291X(17)32129-0. PMID:29107694

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt298.73
Cas No.120964-45-6
FormulaC12H14N4O3.HCl
SynonymsNSC 617989 hydrochloride,DZNep,3-Deazaneplanocin A
Solubility≥14.9mg/mL in DMSO, <2.99 mg/mL in EtOH, ≥18.32 mg/mL in H2O with ultrasonic
Chemical Name(1S,2R,5R)-5-(4-aminoimidazo[4,5-c]pyridin-1-yl)-3-(hydroxymethyl)cyclopent-3-ene-1,2-diol;hydrochloride
SDFDownload SDF
Canonical SMILESC1=CN=C(C2=C1N(C=N2)C3C=C(C(C3O)O)CO)N.Cl
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。

试验操作

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HL-60和OCI-AML3 AML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。DZNep在cyclin E和HOXA9耗尽之后诱导p16、p21、p27和FBXO32。

动物实验[2]:

动物模型

Sprague-Dawley大鼠(120–140 g)

剂量

5 μM;实验前预处理24小时;随饮食口服。

应用

在非酒精脂肪肝疾病(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.

生物活性

描述 3-Deazaneplanocin A hydrochloride是组蛋白甲基转移酶抑制剂。
靶点 histone methyltransferase          
IC50            

质量控制

化学结构

3-Deazaneplanocin A (DZNep) hydrochloride

相关生物数据

3-Deazaneplanocin A (DZNep) hydrochloride

相关生物数据

3-Deazaneplanocin A (DZNep) hydrochloride

相关生物数据

3-Deazaneplanocin A (DZNep) hydrochloride