EZH2-IN-2
Based on 1 Customer Validation
EZH2-IN-2 (Example 69) is a EZH2 inhibitor with an IC50 and a TR-FRET IC50 of 64 nM and 20 nM. EZH2-IN-2 can be used for the research of cancer or precancerous condition related to EZH2 activity.
For research use only. We do not sell to patients.
- Purity: 98.51%
- CAS No.: 2238821-31-1
- Formula: C36H46N6O3
- Molecular Weight:610.79
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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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Histone Modification Research Compound Library
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Anti-Cancer Compound Library
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Reprogramming Compound Library
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Anti-Blood Cancer Compound Library
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Cancer Stem Cells Compound Library
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Heterocyclic Compound Library
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Anti-Hematopathy Compound Library
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
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Bioactive Compound Library
HY-L001
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Methylation Compound Library
HY-L203
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High-Throughput Bioactive Compound Library
HY-L205
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Posttranslational Modification Library
HY-L226
All Histone Methyltransferase Isoforms
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Biological Activity
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EZH2 64 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Daudi | GI50 |
>10 μM
Compound: 29
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Antiproliferative activity against human Daudi cells expressing wild type EZH2 assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay
Antiproliferative activity against human Daudi cells expressing wild type EZH2 assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay
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[PMID: 34664960] |
| KARPAS-422 | GI50 |
0.05 μM
Compound: 29
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Antiproliferative activity against human KARPAS-422 cells harboring EZH2 Y641N mutant assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay
Antiproliferative activity against human KARPAS-422 cells harboring EZH2 Y641N mutant assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay
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[PMID: 34664960] |
| Pfeiffer | GI50 |
0.003 μM
Compound: 29
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Antiproliferative activity against human Pfeiffer cells harboring EZH2 A677G mutant assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay
Antiproliferative activity against human Pfeiffer cells harboring EZH2 A677G mutant assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay
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[PMID: 34664960] |
| Raji | GI50 |
>10 μM
Compound: 29
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Antiproliferative activity against human Raji cells expressing wild type EZH2 assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay
Antiproliferative activity against human Raji cells expressing wild type EZH2 assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay
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[PMID: 34664960] |
| SUD4 | GI50 |
3.87 μM
Compound: 29
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Antiproliferative activity against human SU-DHL-4 cells harboring EZH2 Y641S mutant assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay
Antiproliferative activity against human SU-DHL-4 cells harboring EZH2 Y641S mutant assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay
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[PMID: 34664960] |
| SU-DHL-6 | GI50 |
1.1 μM
Compound: 29
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Antiproliferative activity against human SU-DHL-6 cells harboring EZH2 Y641N mutant assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay
Antiproliferative activity against human SU-DHL-6 cells harboring EZH2 Y641N mutant assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay
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[PMID: 34664960] |
| U2932 | GI50 |
>10 μM
Compound: 29
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Antiproliferative activity against human U2932 cells expressing wild type EZH2 assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay
Antiproliferative activity against human U2932 cells expressing wild type EZH2 assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay
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[PMID: 34664960] |
Chemical Information
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CAS No. 2238821-31-1
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Appearance Solid
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Molecular Weight 610.79
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Formula C36H46N6O3
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Color White to light yellow
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SMILES
O=C(NCC1=C(C)C=C(C)NC1=O)C2=CC(C3=CC=C(N4CCN(CC5CC5)CC4)N=C3C)=CC(N(C(C6CC6)=O)CC)=C2C
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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 6 months -20°C 1 month
Solvent & Solubility
DMSO : 10 mg/mL (16.37 mM; ultrasonic and warming and heat to 60°C; 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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: ≥ 1 mg/mL (1.64 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1 mg/mL (1.64 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Purity & Documentation
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Data Sheet (270 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Portuguese - PT (251 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.6372 mL | 8.1861 mL | 16.3722 mL | 40.9306 mL |
| 5 mM | 0.3274 mL | 1.6372 mL | 3.2744 mL | 8.1861 mL | |
| 10 mM | 0.1637 mL | 0.8186 mL | 1.6372 mL | 4.0931 mL | |
| 15 mM | 0.1091 mL | 0.5457 mL | 1.0915 mL | 2.7287 mL |
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