JQEZ5

Pricing Availability   Qty
说明: Potent and selective SAM-competitive EZH2 inhibitor
化学名: N-[(1,2-Dihydro-6-methyl-2-oxo-4-propyl-3-pyridinyl)methyl]-1-(1-methylethyl)-6-[6-(4-methyl-1-piperazinyl)-3-pyridinyl]-1H-pyrazolo[3,4-b]pyridine-4-carboxamide
纯度: ≥98% (HPLC)
说明书
引用文献
评论
文献 (5)

生物活性 for JQEZ5

JQEZ5 is a potent and selective SAM-competitive EZH2 lysine methyltransferase inhibitor (IC50 = 11 nM). Selectively binds EZH2 over a panel of 22 methyltransferases. Reduces global level of the PRC2-associated mark H3K27me3 in K562 cells. Suppresses cell growth in CML cells. Inhibits colony formation of primary human CD34+ CML stem/ progenitor cells. Antitumor effects in vivo.

许可信息

Sold under license from Dana-Farber Cancer Institute.

化合物库 for JQEZ5

JQEZ5 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。

技术数据 for JQEZ5

分子量 542.69
公式 C30H38N8O2
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 1913252-04-6
PubChem ID 121322599
InChI Key LQTWDAYNGMMHLV-UHFFFAOYSA-N
Smiles CN(CC1)CCN1C2=CC=C(C3=NC(N(C(C)C)N=C4)=C4C(C(NCC5=C(CCC)C=C(C)NC5=O)=O)=C3)C=N2

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 JQEZ5

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 10.85 20

制备储备液 for JQEZ5

以下数据基于产品分子量 542.69。 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.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 1 mg 5 mg 10 mg
0.2 mM 9.21 mL 46.07 mL 92.13 mL
1 mM 1.84 mL 9.21 mL 18.43 mL
2 mM 0.92 mL 4.61 mL 9.21 mL
10 mM 0.18 mL 0.92 mL 1.84 mL

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参考文献 for JQEZ5

参考文献是支持产品生物活性的出版物。

Xie et al (2016) Chronic myelogenous leukemia- initiating cells require polycomb group protein EZH2. Send to 6 1237 PMID: 27630126

Frankel et al (2016) Developing EZH2-targeted therapy for lung cancer. Cancer Discov. 6 949 PMID: 27587466

Zhang et al (2016) Oncogenic deregulation of EZH2 as an opportunity for targeted therapy in lung cancer. Cancer Discov. 6 1006 PMID: 27312177


If you know of a relevant reference for JQEZ5, please let us know.

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关键词: JQEZ5, JQEZ5 supplier, potent, selective, EZH2, histone, methyltransferase, inhibitors, inhibits, PRC2, polycomb, repressive, complex, 2, CML, Lysine, Methyltransferases, 6153, Tocris Bioscience

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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

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

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

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

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

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.