PROTAC EED degrader-1
Based on 1 Customer Validation
PROTAC EED degrader-1 is a von Hippel-Lindau-based PROTAC targeting EED with a pKD of 9.02. PROTAC EED degrader-1 is a polycomb repressive complex 2 (PRC2) inhibitor (pIC50=8.17) targeting the EED subunit.
(Pink: EED ligand (HY-130815); Blue: VHL ligand (HY-125845); Black: linker (HY-130637)).
For research use only. We do not sell to patients.
- Purity: 99.18%
- CAS No.: 2639882-72-5
- Formula: C55H60FN11O8S
- Molecular Weight:1054.20
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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
Biological Activity
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VHL |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| KARPAS-422 | GI50 |
45 nM
Compound: 107; PROTAC 2
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Antiproliferative activity against human Karpas422 cells after 14 days by celltiter-glo luminescent cell viability assay
Antiproliferative activity against human Karpas422 cells after 14 days by celltiter-glo luminescent cell viability assay
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[PMID: 33283516] |
PROTAC EED degrader-1 (Compound PROTAC 2) binds to EED with a pKD of 9.02±0.09 and inhibits PRC2 function with a pIC50 of 8.17±0.24[1].
PROTAC EED degrader-1 (0.01-100 μM; 14 days) can potently inhibit proliferation of an EZH2 mutant DLBCL cell line Karpas422[1].
PROTAC EED degrader-1 (0.1-3 μM; 48 hours) reduces the protein levels of EED, EZH2, H3K27me3 in Karpas422 cells[1].
PROTAC EED degrader-1 (1 μM ; 1-24 h) promotes degradation of EED, EZH2, and SUZ12 in Karpas422 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Karpas422 cells
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Concentration:0.01, 0.1, 1, 10, 100μM
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Incubation Time:4, 8, 12, 14 days
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Result:Reduced proliferation. GI50=0.045 uM (Day 14).
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Cell Line:Karpas422 cells
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Concentration:0.1, 1, and 3 μM
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Incubation Time:48 hours
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Result:The protein levels of EED, EZH2, H3K27me3 was reduced.
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Cell Line:Karpas422 cells
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Concentration:1 μM
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Incubation Time:1, 2, 4, 6, 8, 24 hours
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Result:EED protein levels decreased within 1-2 h of treatment.
Chemical Information
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CAS No. 2639882-72-5
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Appearance Solid
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Molecular Weight 1054.20
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Formula C55H60FN11O8S
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Color White to off-white
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SMILES
FC1=CC=C2C(CCO2)=C1CNC3=NC=C(C4=C(C)N=C(CCC(NCCOC5=CC=C(OCC(N[C@@H](C(C)(C)C)C(N6[C@H](C(NCC7=CC=C(C8=C(C)N=CS8)C=C7)=O)C[C@@H](O)C6)=O)=O)C=C5)=O)C=C4)C9=NN=CN39
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 150 mg/mL (142.29 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. 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: ≥ 3.75 mg/mL (3.56 mM); Clear solution
This protocol yields a clear solution of ≥ 3.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (37.5 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.
Purity & Documentation
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Data Sheet (271 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)
- Korean - KR (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, 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 | 0.9486 mL | 4.7429 mL | 9.4859 mL | 23.7147 mL |
| 5 mM | 0.1897 mL | 0.9486 mL | 1.8972 mL | 4.7429 mL | |
| 10 mM | 0.0949 mL | 0.4743 mL | 0.9486 mL | 2.3715 mL | |
| 15 mM | 0.0632 mL | 0.3162 mL | 0.6324 mL | 1.5810 mL | |
| 20 mM | 0.0474 mL | 0.2371 mL | 0.4743 mL | 1.1857 mL | |
| 25 mM | 0.0379 mL | 0.1897 mL | 0.3794 mL | 0.9486 mL | |
| 30 mM | 0.0316 mL | 0.1581 mL | 0.3162 mL | 0.7905 mL | |
| 40 mM | 0.0237 mL | 0.1186 mL | 0.2371 mL | 0.5929 mL | |
| 50 mM | 0.0190 mL | 0.0949 mL | 0.1897 mL | 0.4743 mL | |
| 60 mM | 0.0158 mL | 0.0790 mL | 0.1581 mL | 0.3952 mL | |
| 80 mM | 0.0119 mL | 0.0593 mL | 0.1186 mL | 0.2964 mL | |
| 100 mM | 0.0095 mL | 0.0474 mL | 0.0949 mL | 0.2371 mL |
PROTAC EED degrader-1 Related Classifications
HY-130614 Related Classifications
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