PROTAC EED degrader-2
Based on 1 publication(s) in Google Scholar
PROTAC EED degrader-2 is a von Hippel-Lindau-based PROTAC targeting EED with a pKD of 9.27. PROTAC EED degrader-2 is a polycomb repressive complex 2 (PRC2) inhibitor (pIC50=8.11) targeting the EED subunit.
(Pink: EED ligand (HY-130815); Blue: VHL ligand (HY-125845); Black: linker (HY-W014099)).
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- Pureté: 99.90%
- CAS No.: 2639882-69-0
- Formule: C50H58FN11O6S
- Masse moléculaire:960.13
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Stockage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) PROTAC EED degrader-2
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Activité biologique
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VHL |
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Cell Line
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Type | Value | Description | References |
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| KARPAS-422 | GI50 |
57 nM
Compound: 106; PROTAC 1
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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] |
| KARPAS-422 | GI50 |
57 nM
Compound: 72
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Antiproliferative activity against human KARPAS-422 cells assessed as cell growth inhibition measured after 7 to 10 days by celltitre-glo-luminescent assay
Antiproliferative activity against human KARPAS-422 cells assessed as cell growth inhibition measured after 7 to 10 days by celltitre-glo-luminescent assay
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[PMID: 35093670] |
PROTAC EED degrader-2 (Compound PROTAC 1) binds to EED with a pKD of 9.27±0.05 and inhibits PRC2 function with a pIC50 of 8.11±0.09[1].
PROTAC EED degrader-2 (0.01-100 μM; 14 days) can potently inhibit proliferation of an EZH2 mutant DLBCL cell line Karpas422[1].
PROTAC EED degrader-2 (0.1-3 μM; 48 hours) reduces the protein levels of EED, EZH2, H3K27me3 in Karpas422 cells[1].
PROTAC EED degrader-2 (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, 100 μM
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Incubation Time:4, 8, 12, 14 days
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Result:Reduced proliferation. GI50=0.057 μM (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. 2639882-69-0
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Appearance Solid
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Masse moléculaire 960.13
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Formule C50H58FN11O6S
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Color White to off-white
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SMILES
FC1=CC=C2C(CCO2)=C1CNC3=NC=C(C4=NN=CN34)C5=C(N=C(C=C5)CCC(NCCCCC(N[C@H](C(N6[C@@H](C[C@H](C6)O)C(NCC7=CC=C(C=C7)C8=C(N=CS8)C)=O)=O)C(C)(C)C)=O)=O)C
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (1)
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Journal Impact Factor
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Most Recent
Solvant et solubilité
DMSO : 80 mg/mL (83.32 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 (protect from light). 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 (protect from light). 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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2 mg/mL (2.08 mM); Clear solution
This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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.
Pureté et documentation
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Fiche technique (274 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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Instruction de manipulation (2659 KB)
Références
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 (protect from light). 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 | 1.0415 mL | 5.2076 mL | 10.4153 mL | 26.0381 mL |
| 5 mM | 0.2083 mL | 1.0415 mL | 2.0831 mL | 5.2076 mL | |
| 10 mM | 0.1042 mL | 0.5208 mL | 1.0415 mL | 2.6038 mL | |
| 15 mM | 0.0694 mL | 0.3472 mL | 0.6944 mL | 1.7359 mL | |
| 20 mM | 0.0521 mL | 0.2604 mL | 0.5208 mL | 1.3019 mL | |
| 25 mM | 0.0417 mL | 0.2083 mL | 0.4166 mL | 1.0415 mL | |
| 30 mM | 0.0347 mL | 0.1736 mL | 0.3472 mL | 0.8679 mL | |
| 40 mM | 0.0260 mL | 0.1302 mL | 0.2604 mL | 0.6510 mL | |
| 50 mM | 0.0208 mL | 0.1042 mL | 0.2083 mL | 0.5208 mL | |
| 60 mM | 0.0174 mL | 0.0868 mL | 0.1736 mL | 0.4340 mL | |
| 80 mM | 0.0130 mL | 0.0651 mL | 0.1302 mL | 0.3255 mL |
PROTAC EED degrader-2 Related Classifications
HY-130615 Related Classifications
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