JQEZ5
Based on 3 publication(s) in Google Scholar
JQEZ5 is a potent and selective EZH2 lysine methyltransferase inhibitor. JQEZ5 SAM-competitively inhibits polycomb repressive complex 2 (PRC2) with an IC50 of 80 nM. JQEZ5 has anti-tumor effects.
For research use only. We do not sell to patients.
- Purity: 98.14%
- CAS No.: 1913252-04-6
- Formula: C30H38N8O2
- Molecular Weight:542.68
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) JQEZ5
MoreAll Histone Methyltransferase Isoforms
More
Biological Activity
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EZH2 |
JQEZ5 inhibits enzymatic functionality of PRC2 with a biochemical IC50 of 80nM. JQEZ5 exhibits S-adenosyl methionine (SAM)-competitive inhibition of PRC2[1].
H661 cells treated with increasing concentrations of JQEZ5 demonstrate acutely reduced levels of H3K27me3 without affecting H3K27 mono- or di-methylation. JQEZ5 suppresses the proliferation of EZH2-overexpressing H661 and H522 cells after treatment for 4 days without affecting the proliferation of cell lines that were deemed insensitive to EZH2 knockdown[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1913252-04-6
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Appearance Solid
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Molecular Weight 542.68
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Formula C30H38N8O2
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Color Light yellow to yellow
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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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Acta Pharmacol Sin
2022 Feb;43(2):457-469. PMID: 33850273 -
J Transl Med
HO-1 promotes resistance to an EZH2 inhibitor through the pRB-E2F pathway: correlation with the progression of myelodysplastic syndrome into acute myeloid leukemia. [Abstract]2019 Nov 11;17(1):366. PMID: 31711520 -
Gene
EZH2 suppresses insulinoma development by epigenetically reducing KIF4A expression via H3K27me3 modification. [Abstract]2022 May 15:822:146317. PMID: 35182680
Solvent & Solubility
DMSO : 25 mg/mL (46.07 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.61 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
Tumor-bearing genetically-engineered mouse models (GEMMs) are monitored for onset of symptoms (breath distress) and then treated with JQEZ5 for three weeks (75 mg/kg IP daily). Tumors are visualized by MRI and tumor volume of the lungs is calculated using 3D Slicer. For xenograft experiments, H661 cells are dissociated into single cells, counted and resuspended at 2×106 cells per 250 µL of 1:1 media/matrigel. Eight- to 12-week-old female Foxn1nu/Foxn1nu mice are injected subcutaneously with 2×106 cells in two to three spots on the flanks. Tumors are allowed to grow to an approximate size of 200 mm3 (~10 weeks) and the mice are randomized for vehicle (n=3) or JQEZ5 administration (n=6, 75 mg/kg/d, i.p.) for 18 days. Tumor growth is measured by caliper measurements and tumor volume is calculated by standard methods[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (276 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8427 mL | 9.2135 mL | 18.4271 mL | 46.0677 mL |
| 5 mM | 0.3685 mL | 1.8427 mL | 3.6854 mL | 9.2135 mL | |
| 10 mM | 0.1843 mL | 0.9214 mL | 1.8427 mL | 4.6068 mL | |
| 15 mM | 0.1228 mL | 0.6142 mL | 1.2285 mL | 3.0712 mL | |
| 20 mM | 0.0921 mL | 0.4607 mL | 0.9214 mL | 2.3034 mL | |
| 25 mM | 0.0737 mL | 0.3685 mL | 0.7371 mL | 1.8427 mL | |
| 30 mM | 0.0614 mL | 0.3071 mL | 0.6142 mL | 1.5356 mL | |
| 40 mM | 0.0461 mL | 0.2303 mL | 0.4607 mL | 1.1517 mL |
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