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Description: Potent and selective SAM-competitive EZH2 inhibitor
Chemical Name: 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
Purity: ≥98% (HPLC)
Biological Activity 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.
Licensing Information
Sold under license from Dana-Farber Cancer Institute.
Compound Libraries for JQEZ5
JQEZ5 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for JQEZ5
| M. Wt | 542.69 |
| Formula | C30H38N8O2 |
| Storage | Store at -20°C |
| Purity | ≥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 |
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.
Solubility Data for JQEZ5
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 10.85 | 20 |
Preparing Stock Solutions for JQEZ5
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 |
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Product Datasheets for JQEZ5
References for JQEZ5
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.
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Keywords: JQEZ5, JQEZ5 supplier, potent, selective, EZH2, histone, methyltransferase, inhibitors, inhibits, PRC2, polycomb, repressive, complex, 2, CML, Lysine, Methyltransferases, 6153, Tocris Bioscience
Citations for JQEZ5
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
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.