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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.
Sold under license from Dana-Farber Cancer Institute.
JQEZ5 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
The following data is based on the product molecular weight 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.
|Concentration / Solvent Volume / Mass||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|
References are publications that support the biological activity of the product.
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.
Keywords: 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!
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