PROTAC eDHFR Degrader-1
Based on 1 Customer Validation
PROTAC eDHFR Degrader-1 is a PROTAC eDHFR degrader. PROTAC eDHFR Degrader-1 binds eDHFR-tagged proteins and Cereblon, thereby driving ternary complex formation, ubiquitination and proteasomal degradation. PROTAC eDHFR Degrader-1 degrades eDHFR-tagged proteins in multiple cell types and rodent models, and enables multiplex orthogonal protein regulation. PROTAC eDHFR Degrader-1 can be used in research related to metastatic ovarian cancer.
(Pink: eDHFR ligand (HY-W587663); Blue: Cereblon ligand (HY-41547); Black: linker).
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 98.09%
- CAS. Nr.: 2849442-92-6
- Formel: C36H44N8O10
- Molecular Weight:748.78
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
Beschreibung
In Vitro
PROTAC eDHFR Degrader-1 (compound 7c) (2 nM-100 μM; 4 h-48 h) potently induces dose-dependent degradation of eDHFR-YFP in JURKAT-eDHFR-YFP cells[1].
PROTAC eDHFR Degrader-1 (2 nM-100 μM; 6 h-24 h) induces significant, reversible, dose-dependent degradation of eDHFR-YFP in HEK293T-eDHFR-YFP cells[1].
PROTAC eDHFR Degrader-1 mediates the degradation of eDHFR-YFP in HEK293T-eDHFR-YFP cells via the ubiquitin-proteasome pathway, a process that requires the formation of a ternary complex with eDHFR and the Cereblon E3 ligase; it induces partial degradation of eDHFR-Luc in HCT116-eDHFR-Luc cells with low Cereblon expression; and it potently induces dose-dependent degradation of eDHFR-Luc in OVCAR8-eDHFR-Luc cells[1].
PROTAC eDHFR Degrader-1 (2 nM-100 μM; 24 h) potently induces the degradation of various eDHFR fusion proteins (CD122, Lck, RUNX1) in HEK293T cells[1].
PROTAC eDHFR Degrader-1 (2 nM-100 μM; 24 h) selectively induces the degradation of EGFP-eDHFR in OVCAR8-mCherry-FKBP12F36V-EGFP-eDHFR cells, and functions orthogonally to the dTAGv-1/FKBP12F36V system[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
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Cell Line:HEK293T-eDHFR-YFP cells (HEK293T cells stably expressing eDHFR-YFP-T2A-firefly luciferase)
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Concentration:2 nM, 25 nM, 100 nM, 25 μM, 100 μM
100 nM (wash out test) -
Incubation Time:6 h, 12 h, 24 h
1, 2, 4, 8, 16, 24 h (wash out test) -
Result:Achieved maximum downregulation of eDHFR-YFP after 24 h incubation with 25-100 nM.
Showed a dose-dependent effect with a "hook effect" at higher concentrations.
Restored eDHFR-YFP expression fully within 24 h after a 24 h incubation with 100 nM followed by washout.
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Cell Line:HEK293T cells stably expressing eDHFR-fused proteins (CD122-eDHFR-FLAG, Lck-eDHFR-FLAG, RUNX1-eDHFR-FLAG)
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Concentration:2 nM, 25 nM, 100 nM, 25 μM, 100 μM
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Incubation Time:24 h
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Result:Achieved optimal degradation of CD122-eDHFR-FLAG, Lck-eDHFR-FLAG, and RUNX1-eDHFR-FLAG with 25-100 nM after 24 h incubation.
Exhibited optimal degradation regardless of the subcellular localization of the target protein.
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Cell Line:OVCAR8-mCherry-FKBP12F36V-EGFP-eDHFR cells (OVCAR8 cells stably expressing both mCherry-FKBP12F36V and EGFP-eDHFR)
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Concentration:2 nM, 25 nM, 100 nM, 25 μM, 100 μM
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Incubation Time:24 h
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Result:Downregulated EGFP-eDHFR at 25-100 nM without affecting mCherry-FKBP12F36V abundance.
Downregulated both fusion proteins to near-complete depletion relative to vehicle controls when co-treated with dTAGv-1.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 2849442-92-6
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Appearance Solid
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Molecular Weight 748.78
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Formel C36H44N8O10
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Color Light yellow to yellow
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SMILES
NC1=C(CC2=CC(OC)=C(OCCCC(NCCOCCOCCNC3=CC=CC(C(N4C5CCC(NC5=O)=O)=O)=C3C4=O)=O)C(OC)=C2)C=NC(N)=N1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 100 mg/mL (133.55 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (274 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
Verweise
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 | 1.3355 mL | 6.6775 mL | 13.3551 mL | 33.3876 mL |
| 5 mM | 0.2671 mL | 1.3355 mL | 2.6710 mL | 6.6775 mL | |
| 10 mM | 0.1336 mL | 0.6678 mL | 1.3355 mL | 3.3388 mL | |
| 15 mM | 0.0890 mL | 0.4452 mL | 0.8903 mL | 2.2258 mL | |
| 20 mM | 0.0668 mL | 0.3339 mL | 0.6678 mL | 1.6694 mL | |
| 25 mM | 0.0534 mL | 0.2671 mL | 0.5342 mL | 1.3355 mL | |
| 30 mM | 0.0445 mL | 0.2226 mL | 0.4452 mL | 1.1129 mL | |
| 40 mM | 0.0334 mL | 0.1669 mL | 0.3339 mL | 0.8347 mL | |
| 50 mM | 0.0267 mL | 0.1336 mL | 0.2671 mL | 0.6678 mL | |
| 60 mM | 0.0223 mL | 0.1113 mL | 0.2226 mL | 0.5565 mL | |
| 80 mM | 0.0167 mL | 0.0835 mL | 0.1669 mL | 0.4173 mL | |
| 100 mM | 0.0134 mL | 0.0668 mL | 0.1336 mL | 0.3339 mL |
PROTAC eDHFR Degrader-1 Related Classifications
HY-149678 Related Classifications
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Keywords
- PROTAC eDHFR Degrader-1
- 2849442-92-6
- PROTAC eDHFR Degrader1
- PROTAC eDHFR Degrader 1
- PROTACs
- Dihydrofolate reductase (DHFR)
- ubiquitin-proteasome pathway
- HEK293T cells
- eDHFR-tagged proteins
- metastatic ovarian cancer
- Cereblon
- Cereblon E3 ligase
- JURKAT-eDHFR-YFP cells
- OVCAR8-mCherry-FKBP12F36V-EGFP-eDHFR cells
- HEK293T-eDHFR-YFP cells
- HCT116-eDHFR-Luc cells
- Inhibitor
- inhibitor
- inhibit