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Submit Review3-Deazaneplanocin A hydrochloride
说明： EZH2 histone methyltransferase inhibitor
别名： DZNep,NSC 617989
化学名： (1S,2R,5R)-5-(4-Amino-1H-imidazo[4,5-c]pyridin-1-yl)-3-(hydroxymethyl)-3-cyclopentene-1,2-diol hydrochloride
纯度： ≥98% (HPLC)
生物活性 for 3-Deazaneplanocin A hydrochloride
3-Deazaneplanocin A hydrochloride is a histone methyltransferase inhibitor; decreases global histone methylation. 3-Deazaneplanocin A hydrochloride inhibits EZH2 histone methyltransferase and s-adenosylhomocysteine (SAH) hydrolase activity. Blocks trimethylation of lysine 27 on histone H3 and lysine 20 on histone H4 in vitro. 3-Deazaneplanocin A hydrochloride induces apoptosis in multiple cancer cell lines and has no apoptotic effect on normal cells. Enhances Oct4 expression in chemically induced pluripotent stem cells (CiPSCs).
DZNep synthesized to Ancillary Material Grade also available.
For more information about how 3-Deazaneplanocin A hydrochloride may be used, see our protocol: Highly Efficient Generation of CiPSCs from MEFs
技术数据 for 3-Deazaneplanocin A hydrochloride
| 分子量 | 298.73 |
| 公式 | C12H14N4O3.HCl |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 120964-45-6 |
| PubChem ID | 14563109 |
| InChI Key | UNSKMHKAFPRFTI-FDKLLANESA-N |
| Smiles | OCC([C@@H](O)[C@H]3O)=C[C@H]3N2C=NC1=C(N)N=CC=C12.Cl |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for 3-Deazaneplanocin A hydrochloride
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| water | 2.99 | 10 |
制备储备液 for 3-Deazaneplanocin A hydrochloride
以下数据基于产品分子量 298.73。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 33.48 mL | 167.38 mL | 334.75 mL |
| 0.5 mM | 6.7 mL | 33.48 mL | 66.95 mL |
| 1 mM | 3.35 mL | 16.74 mL | 33.48 mL |
| 5 mM | 0.67 mL | 3.35 mL | 6.7 mL |
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产品说明书 for 3-Deazaneplanocin A hydrochloride
参考文献 for 3-Deazaneplanocin A hydrochloride
参考文献是支持产品生物活性的出版物。
Tan et al (2007) Pharmacologic disruption of Polycomb-repressive complex 2-mediated gene repression selectively induces apoptosis in cancer cells. Genes Dev. 21 1050 PMID: 17437993
Miranda et al (2009) DZNep is a global histone methylation inhibitor that reactivates developmental genes not silenced by DNA methylation. Mol.Cancer Ther. 8 1579 PMID: 19509260
Tseng et al (1989) Synthesis of 3-deazaneplanocin A, a powerful inhibitor of S-adenosylhomocysteine hydrolase with potent and selective in vitro and in vivo antiviral activities. J.Med.Chem. 32 1442 PMID: 2544721
Hou et al (2013) Pluripotent stem cells induced from mouse somatic cells by small-molecule compounds. Science 341 651 PMID: 23868920
If you know of a relevant reference for 3-Deazaneplanocin A hydrochloride, please let us know.
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关键词: 3-Deazaneplanocin A hydrochloride, 3-Deazaneplanocin A hydrochloride supplier, 3-DeazaneplanocinA, NSC617989, Histone, methylation, inhibitors, inhibits, EZH2, trimethylation, apoptosis, s-adenosylhomocysteine, hydrolase, SAHH, CiPSCs, stem, cells, reprogramming, induced, pluripotent, pluripotency, PRC2, polycomb, repressive, complex, 2, DZNep, NSC, 617989, Stem, Cell, Reprogramming, Lysine, Methyltransferases, 4703, Tocris Bioscience
4 篇 3-Deazaneplanocin A hydrochloride 的引用文献
引用文献是使用了 Tocris 产品的出版物。 3-Deazaneplanocin A hydrochloride 的部分引用包括：
Ping et al (2018) Genome-wide DNA methylation analysis reveals that mouse chemical iPSCs have closer epigenetic features to mESCs than OSKM-integrated iPSCs. Cell Death Dis 9 187 PMID: 29416007
Wang et al (2017) Using low-risk factors to generate non-integrated human induced pluripotent stem cells from urine-derived cells. Stem Cell Res Ther 8 245 PMID: 29096702
Jerzy et al (2017) The role of microRNA-5196 in the pathogenesis of systemic sclerosis. Eur J Clin Invest 47 555-564 PMID: 28639412
Stefan et al (2016) Histone Demethylation and Toll-like Receptor 8-Dependent Cross-Talk in Monocytes Promotes Transdifferentiation of Fibroblasts in Systemic Sclerosis Via Fra-2. Arthritis Rheumatol 68 1493-504 PMID: 26814616
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3-Deazaneplanocin A hydrochloride 实验方案
以下实验方案包含使用 3-Deazaneplanocin A hydrochloride（目录编号 4703）的更多信息。
该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
Epigenetics Scientific Review
Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.
Stem Cells Scientific Review
Written by Kirsty E. Clarke, Victoria B. Christie, Andy Whiting and Stefan A. Przyborski, this review provides an overview of the use of small molecules in the control of stem cell growth and differentiation. Key signaling pathways are highlighted, and the regulation of ES cell self-renewal and somatic cell reprogramming is discussed. Compounds available from Tocris are listed.
Cancer Metabolism Poster
This poster summarizes the main metabolic pathways in cancer cells and highlights potential targets for cancer therapeutics. Genetic changes and epigenetic modifications in cancer cells alter the regulation of cellular metabolic pathways providing potential cancer therapeutic targets.
Epigenetics in Cancer Poster
This poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.
Stem Cells Poster
Written by Rebecca Quelch and Stefan Przyborski from Durham University (UK), this poster describes the isolation of pluripotent stem cells, their maintenance in culture, differentiation, and the generation and potential uses of organoids.