PROTAC ERRα Degrader-3
Based on 1 publication(s) in Google Scholar
PROTAC ERRα Degrader-3 is a potent and selective ERRα degrader based on von Hippel-Lindau ligand. PROTAC ERRα Degrader-3 is capable of specifically degrading ERRα protein by >80% at a concentration of 30 nM. PROTAC ERRα Degrader-3 is inactive against ERRβ and ERRγ proteins.
(Pink: ERRα ligand (HY-126351); Blue: VHL ligand (HY-125845); Black: linker (HY-W015878)).
For research use only. We do not sell to patients.
- Purity: 98.74%
- CAS No.: 2306388-65-6
- Formula: C47H50F6N6O7S
- Molecular Weight:956.99
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Storage:Powder -20°C, 3 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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Anti-Cancer Compound Library
HY-L025
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Covalent Screening Library
HY-L036
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Anti-Breast Cancer Compound Library
HY-L074
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Nuclear Receptor Compound Library
HY-L126
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Heterocyclic Compound Library
HY-L138
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Membrane Receptor-targeted Compound Library
HY-L150
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PROTAC Library
HY-L151
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Highly Selective Inhibitors Library
HY-L158
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Anti-Ovarian Cancer Compound Library
HY-L173
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Multi-Target Compound Library
HY-L176
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Covalent Screening Library Plus
HY-L036P
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Bioactive Compound Library
HY-L001
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High-Throughput Bioactive Compound Library
HY-L205
Publications Citing Use of MedChemExpress (MCE) PROTAC ERRα Degrader-3
MoreAll PROTACs Isoforms
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Biological Activity
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ERRα |
VHL |
PROTAC ERRα Degrader-3 (compound 6c; 0.3 nM-10 μM; 4 hours) dose-dependently induces ERRα degradation with an efficacious dose as low as 3.0 nM at 4.0 h. PROTAC ERRα Degrader-3 potently decreases protein levels of ERRα downstream target genes, e.g., ATP5B, medium-chain acyl CoA dehydrogenase (MCAD), and pyruvate dehydrogenase kinase 4 (PDK4) in the MDA-MB-231 cells after a 24 h treatment[1].
PROTAC ERRα Degrader-3 exhibits an IC50 value of 12.67 nM to block the protein-protein interaction of ERRα with PGC-1α peptide and induces approximately 96% protein degradation at 100 nM (D100 nM) after 4.0 h treatment[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231 cells
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Concentration:0.3 nM, 1 nM, 3 nM, 10 nM, 30 nM, 100 nM, 300 nM, 1 μM, 3 μM, 10 μM
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Incubation Time:4 hours
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Result:Dose-dependently induced ERRα degradation.
Chemical Information
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CAS No. 2306388-65-6
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Appearance Solid
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Molecular Weight 956.99
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Formula C47H50F6N6O7S
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Color Off-white to light yellow
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SMILES
COC(C=C1/C=C(C#N)/C(NCCCCC(N[C@@H](C(C)(C)C)C(N2[C@@H](C[C@H](C2)O)C(NCC3=CC=C(C4=C(C)N=CS4)C=C3)=O)=O)=O)=O)=C(C=C1)OCC5=C(C=C(C=C5)C(F)(F)F)C(F)(F)F
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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
Publications (1)
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Journal Impact Factor
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Most Recent
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Drug Metab Dispos
Applications of contemporary tools to measure plasma protein binding of targeted protein degraders. [Abstract]2025 May;53(5):100066. PMID: 40286535
Solvent & Solubility
DMSO : 80 mg/mL (83.60 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: ≥ 2 mg/mL (2.09 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 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 (274 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)
- 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. 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 |
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| DMSO | 1 mM | 1.0449 mL | 5.2247 mL | 10.4494 mL | 26.1236 mL |
| 5 mM | 0.2090 mL | 1.0449 mL | 2.0899 mL | 5.2247 mL | |
| 10 mM | 0.1045 mL | 0.5225 mL | 1.0449 mL | 2.6124 mL | |
| 15 mM | 0.0697 mL | 0.3483 mL | 0.6966 mL | 1.7416 mL | |
| 20 mM | 0.0522 mL | 0.2612 mL | 0.5225 mL | 1.3062 mL | |
| 25 mM | 0.0418 mL | 0.2090 mL | 0.4180 mL | 1.0449 mL | |
| 30 mM | 0.0348 mL | 0.1742 mL | 0.3483 mL | 0.8708 mL | |
| 40 mM | 0.0261 mL | 0.1306 mL | 0.2612 mL | 0.6531 mL | |
| 50 mM | 0.0209 mL | 0.1045 mL | 0.2090 mL | 0.5225 mL | |
| 60 mM | 0.0174 mL | 0.0871 mL | 0.1742 mL | 0.4354 mL | |
| 80 mM | 0.0131 mL | 0.0653 mL | 0.1306 mL | 0.3265 mL |
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