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Submit ReviewJQEZ5 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.
Sold under license from Dana-Farber Cancer Institute.
JQEZ5 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 10.85 | 20 |
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.
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 |
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.
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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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。
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.
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.
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.
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.