PROTAC EZH2 Degrader-2
Based on 1 publication(s) in Google Scholar
PROTAC EZH2 Degrader-2 is a PROTAC EZH2 inhibitor. PROTAC EZH2 Degrader-2 degrades EZH2 in SU-DHL-6 cells in a dose-dependent manner. PROTAC EZH2 Degrader-2 induces apoptosis and reduces mitochondrial membrane potential in SU-DHL-6 cells. PROTAC EZH2 Degrader-2 has anti-cancer and anti-proliferative activity.
(Pink: EZH2 ligand (HY-179351); Blue: MDM2 ligand (HY-128836); Black: linker (HY-W021401)).
For research use only. We do not sell to patients.
- Purity: 98.77%
- CAS No.: 3093642-32-8
- Formula: C77H93Cl2N13O12
- Molecular Weight:1463.55
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Storage:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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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
Publications Citing Use of MedChemExpress (MCE) PROTAC EZH2 Degrader-2
MoreAll PROTACs Isoforms
MoreAll Histone Methyltransferase Isoforms
More
Biological Activity
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EZH2 |
MDM2 |
PROTAC EZH2 Degrader-2 (Compound E-3P-MDM2) (0.037-3 μM, 24-72 h) degrades EZH2, EED, and SUZ12 proteins of PRC2 complex in a concentration and time-dependent manner in SU-DHL-6 cells[1].
PROTAC EZH2 Degrader-2 (0.037-3 μM, 48-72 h) exhibits antiproliferative activity and induces apoptosis in SU-DHL-6 cells[1].
PROTAC EZH2 Degrader-2 (3 μM, 72 h) upregulates the expression of H3K27me3-related genes (ADRB2 and CDKN2) in SU-DHL-6 cells[1].
PROTAC EZH2 Degrader-2 (0.37-30 μM, 48 h) shows more potent inhibitory effect on cell proliferation in SU-DHL-6 (EZH2Y614N) cells than in HBL-1 (EZH2WT) cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SU-DHL-6 cells
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Concentration:0.037, 0.11, 0.33, 1, 3 μM
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Incubation Time:48, 72 h
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Result:Reduced mitochondrial membrane potential.
Upregulated Bax, cytochrome c, cleaved-caspase 9, cleaved-caspase 3.
Disrupted Bax/Bcl-2 balance.
Chemical Information
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CAS No. 3093642-32-8
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Appearance Solid
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Molecular Weight 1463.55
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Formula C77H93Cl2N13O12
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Color White to off-white
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SMILES
CC1=CC(C)=C(CNC(C2=CC(C3=CC=C(CN4CCN(C(C5=CN(CCOCCOCCOCCNC(CN6CCN(C(N7C(C8=CC=C(OC)C=C8OC(C)C)=N[C@H](C9=CC=C(Cl)C=C9)[C@@H]7C%10=CC=C(Cl)C=C%10)=O)CC6=O)=O)N=N5)=O)CC4)C=C3)=CC(N(C%11CCOCC%11)CC)=C2C)=O)C(N1)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications (1)
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Journal Impact Factor
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Most Recent
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bioRxiv
Dual EZH1/2 inhibition enhances DNMT inhibitor efficacy in colon cancer through targeting H3K27me1. [Abstract]2025 Sep 18:2025.09.16.676613. PMID: 41000734
Solvent & Solubility
DMSO : 100 mg/mL (68.33 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, 6 months; -20°C, 1 month (stored under nitrogen). 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 (stored under nitrogen). 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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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 (272 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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 (stored under nitrogen). 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 | 0.6833 mL | 3.4164 mL | 6.8327 mL | 17.0818 mL |
| 5 mM | 0.1367 mL | 0.6833 mL | 1.3665 mL | 3.4164 mL | |
| 10 mM | 0.0683 mL | 0.3416 mL | 0.6833 mL | 1.7082 mL | |
| 15 mM | 0.0456 mL | 0.2278 mL | 0.4555 mL | 1.1388 mL | |
| 20 mM | 0.0342 mL | 0.1708 mL | 0.3416 mL | 0.8541 mL | |
| 25 mM | 0.0273 mL | 0.1367 mL | 0.2733 mL | 0.6833 mL | |
| 30 mM | 0.0228 mL | 0.1139 mL | 0.2278 mL | 0.5694 mL | |
| 40 mM | 0.0171 mL | 0.0854 mL | 0.1708 mL | 0.4270 mL | |
| 50 mM | 0.0137 mL | 0.0683 mL | 0.1367 mL | 0.3416 mL | |
| 60 mM | 0.0114 mL | 0.0569 mL | 0.1139 mL | 0.2847 mL |
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