3-Deazaneplanocin A (DZNep) hydrochloride
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
3-Deazaneplanocin A (DZNep) hydrochloride是一种选择性的EZH2抑制剂,IC50范围介于0.08-0.24 μM之间 [1]。据报道,DZNep对SAHH(S-adenosylhomocysteine hydrolase)也具有抑制活性,Ki值为50 pM [4]。
ENZ2是PRC2的一个亚基,在调控细胞增殖和细胞周期进程中起重要作用。据报道,ENZ2在多种肿瘤包括前列腺癌、乳腺癌、膀胱癌和AML中是过度表达的。在HepG2细胞系中,DZNep通过增加PA/OA依赖性的脂质堆积从而诱导细胞内脂质的增加和TNF-α/TGF-β在mRNA水平上的表达[3]。
DZNep是一种有效的ENZ2抑制剂。在人急性骨髓性白血病(AML)细胞系HL-60和OCI-AML3中,DZNep以剂量依赖的方式减少ENZ2、cyclin E和HOXA9的表达,诱导p16、p21、p27及FBXO32的表达,从而诱导细胞凋亡[2]。
在代谢和组织学上模拟人NAFLD(非酒精性脂肪性肝病)的高脂肪/高果糖饮食喂养(HFA / HFR-D)大鼠模型中,DZNep通过抑制ENZ2具有有效抗炎和抗纤维化的作用[3]。
参考文献:
[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.
- 1. Lin Xu , Jiandong Gao, et al. "Emodin ameliorates tubulointerstitial fibrosis in obstructed kidneys by inhibiting EZH2." Biochem Biophys Res Commun. 2020 Dec 4;S0006-291X(20)32138-0. PMID:33288199
- 2. 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
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 298.73 |
Cas No. | 120964-45-6 |
Formula | C12H14N4O3·HCl |
Synonyms | NSC 617989 hydrochloride,DZNep,3-Deazaneplanocin A |
Solubility | insoluble in EtOH; ≥14.94 mg/mL in DMSO; ≥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 |
SDF | Download SDF |
Canonical SMILES | C1=CN=C(C2=C1N(C=N2)C3C=C(C(C3O)O)CO)N.Cl |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 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。溶液形式一般不宜长期储存,请尽快用完。 |
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. |
描述 | 3-Deazaneplanocin A hydrochloride是组蛋白甲基转移酶抑制剂。 | |||||
靶点 | histone methyltransferase | |||||
IC50 |
质量控制和MSDS
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