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Purity: ≥98%
JQ-EZ-05 (also abbreviated as JQEZ5) is a novel, potent, specific and reversible inhibitor of EZH2 (overexpressed in tumor cells such as lung cancer). Epigenetic targets are exciting new avenues for the discovery of targeted anticancer drugs. Zhang etc. have designed the open-source EZH2 inhibitor JQEZ5 which showed potent antitumor efficacy in vitro and in vivo in preclinical studies in murine and human lung adenocarcinoma models expressing high levels of EZH2. EZH2 is a lysine methyltransferase and acts as master regulator of chromatin function, it orchestrates transcriptional silencing of developmental gene networks. Overexpression of EZH2 is commonly observed in human epithelial cancers, such as non-small cell lung carcinoma (NSCLC), yet definitive demonstration of malignant transformation by deregulated EZH2 remains elusive.
| ln Vitro |
JQEZ5 inhibits PRC2's enzymatic functioning with a biochemical IC50 of 80nM. H661 cells treated with increasing dosages of JQEZ5 show markedly lower levels of H3K27me3 without changing H3K27 mono- or di-methylation. After 4 days of treatment, JQEZ5 inhibits the proliferation of EZH2-overexpressing H661 and H522 cells while having no effect on the proliferation of cell lines that were previously thought to be resistant to EZH2 knockdown [1].
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| ln Vivo |
During the course of the three-week treatment, there is a noticeable and swift reduction in tumor size with JQEZ5 (75 mg/kg; intraperitoneal injection; daily). Additionally, the treatment significantly lowers H3K27me3, supporting JQEZ5's on-target effect in mice[1].
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| References |
[1]. Zhang H, et al. Oncogenic Deregulation of EZH2 as an Opportunity for Targeted Therapy in Lung Cancer. Cancer Discov. 2016 Sep;6(9):1006-21
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| Molecular Formula |
C30H38N8O2
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| Molecular Weight |
542.68
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| CAS # |
1913252-04-6
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| SMILES |
CC(N1N=CC2=C(C(NCC3=C(C=C(NC3=O)C)CCC)=O)C=C(C4=CC=C(N=C4)N5CCN(C)CC5)N=C12)C
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.61 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8427 mL | 9.2135 mL | 18.4271 mL | |
| 5 mM | 0.3685 mL | 1.8427 mL | 3.6854 mL | |
| 10 mM | 0.1843 mL | 0.9214 mL | 1.8427 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
JQEZ5 Inhibits Lung Cancer GrowthIn Vivo.Cancer Discov. 2016 Sep; 6(9): 1006–1021. |
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JQEZ5 Inhibits Lung Cancer Growth of EZH2 Overexpressed Human Lung Cancer Cell.Cancer Discov. 2016 Sep; 6(9): 1006–1021. |
Small Molecule EZH2 Inhibitor Development.Cancer Discov. 2016 Sep; 6(9): 1006–1021. |
 A Subset of Human NSCLC Cells are Dependent on EZH2 Overexpression.Cancer Discov. 2016 Sep; 6(9): 1006–1021. |
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EZH2 Overexpression Establishes a Unique and Conserved Super Enhancer-Associated Transcriptional Landscape.Cancer Discov. 2016 Sep; 6(9): 1006–1021. |
 EZH2-Driven Lung Cancer as a Molecularly Distinct Entity.Cancer Discov. 2016 Sep; 6(9): 1006–1021. |
 ZH2 Overexpression Induces Murine Lung Cancer.Cancer Discov. 2016 Sep; 6(9): 1006–1021. |
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 Structure of PRC2 bound to an inhibitor (Inhibitor 1).Cancer Discov. 2016 Sep; 6(9): 949–952. |
 EZH2 inhibitors. Each of the preclinical and clinical molecules shown has a pyridine amide core except CPI-1205. The compounds in clinical studies are tazemetostat, GSK281626, and CPI-1205.Cancer Discov. 2016 Sep; 6(9): 949–952. |
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