PROTAC_ERRα
Based on 1 Customer Validation
PROTAC_ERRα is a potent and selective ERRα PROTAC degrader (DC50: ~100 nM in MCF-7 cells). PROTAC_ERRα recruits the VHL E3 ubiquitin ligase to ERRα, inducing ERRα ubiquitination and proteasomal degradation in a VHL-dependent manner. PROTAC_ERRα can be used in breast cancer-related research.
(Pink: ERRα ligand (HY-U00425); Blue: VHL ligand (HY-125845); Black: linker).
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- Pureza : 99.71%
- No. CAS: 1801547-15-8
- Fòrmula: C46H47F3N6O9S2
- Peso molecular:949.03
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
ERRα ~100 nM (DC50) |
VHL |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MCF7 | DC50 |
100 nM
Compound: 12; PROTAC_ERRalpha
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Protac activity at VHL/ERRalpha in epoxomicin pre-treated human MCF7 cells assessed as induction of ERRalpha protein degradation incubated for 8 hrs by Western blot analysis
Protac activity at VHL/ERRalpha in epoxomicin pre-treated human MCF7 cells assessed as induction of ERRalpha protein degradation incubated for 8 hrs by Western blot analysis
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[PMID: 31047748] |
In Vitro
PROTAC_ERRα (10-1000 nM; 8 h) potently induces proteasome-dependent degradation of ERRα in breast cancer MCF-7 cells, with a DC50 of approximately 100 nM and a maximum reduction of 86% in protein levels[1].
PROTAC_ERRα (100-500 nM; 4-24 h) exhibits high specificity for ERRα degradation in MCF-7 breast cancer cells, and only causes additional downregulation of BCR at 500 nM after 24 h of incubation[1].
PROTAC_ERRα (100 nM) induces a 50% VHL-dependent downregulation of ERRα in MCF7 breast cancer cells[2].
PROTAC_ERRα induces VHL- and proteasome-dependent, dose-dependent degradation of ERRα in intact cells, with a DC50 of 100 nM[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:MCF7 cells
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Concentration:0, 10, 30, 100, 300 and 1000 nM
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Incubation Time:8 h
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Result:Decreased in ERRα level in a dose-dependent fashion and the maximal level of degradation (DC50) is 86%.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CD-1 (female)[1]
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Dosage:100 mg/kg
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Administration:i.p.; every eight hours; four total doses
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Result:Reduced ERRα protein levels by 44% in heart tissue compared to vehicle-treated controls.
Reduced ERRα protein levels by 44% in kidney tissue compared to vehicle-treated controls.
Reduced ERRα protein levels by 39% in MDA-MB-231 tumor tissue compared to vehicle-treated controls.
Chemical Information
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No. CAS 1801547-15-8
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Appearance Solid
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Peso molecular 949.03
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Fòrmula C46H47F3N6O9S2
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Color White to off-white
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SMILES
O=C(/C(SC1=O)=C/C2=CC(OC)=C(C=C2)OC3=C(C=C(C=C3)C#N)C(F)(F)F)N1CCOCCC(N[C@@H](C(C)(C)C)C(N4[C@@H](C[C@H](C4)O)C(NCC5=CC=C(C6=C(N=CS6)C)C=C5)=O)=O)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 125 mg/mL (131.71 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)
Protocolo
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Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.
Pureza y Documentación
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Ficha de datos (276 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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Instrucciones de manejo (2659 KB)
Referencias
[1]. Bondeson DP, et al. Catalytic in vivo protein knockdown by small-molecule PROTACs. Nature chemical biology. 2015 Aug;11(8):611-7. [Content Brief]
[2]. Gu S, et al. PROTACs: An Emerging Targeting Technique for Protein Degradation in Drug Discovery. Bioessays. 2018 Apr;40(4):e1700247. [Content Brief]
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 | 1.0537 mL | 5.2685 mL | 10.5371 mL | 26.3427 mL |
| 5 mM | 0.2107 mL | 1.0537 mL | 2.1074 mL | 5.2685 mL | |
| 10 mM | 0.1054 mL | 0.5269 mL | 1.0537 mL | 2.6343 mL | |
| 15 mM | 0.0702 mL | 0.3512 mL | 0.7025 mL | 1.7562 mL | |
| 20 mM | 0.0527 mL | 0.2634 mL | 0.5269 mL | 1.3171 mL | |
| 25 mM | 0.0421 mL | 0.2107 mL | 0.4215 mL | 1.0537 mL | |
| 30 mM | 0.0351 mL | 0.1756 mL | 0.3512 mL | 0.8781 mL | |
| 40 mM | 0.0263 mL | 0.1317 mL | 0.2634 mL | 0.6586 mL | |
| 50 mM | 0.0211 mL | 0.1054 mL | 0.2107 mL | 0.5269 mL | |
| 60 mM | 0.0176 mL | 0.0878 mL | 0.1756 mL | 0.4390 mL | |
| 80 mM | 0.0132 mL | 0.0659 mL | 0.1317 mL | 0.3293 mL | |
| 100 mM | 0.0105 mL | 0.0527 mL | 0.1054 mL | 0.2634 mL |
PROTAC_ERRα Related Classifications
HY-147174 Related Classifications
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