EN171
Based on 1 Customer Validation
EN171 is a covalent 14-3-3σ molecular glue ligand that sequesters neonuclear substrates, including BRD4 and BLC6, into the cytoplasm by recruiting 14-3-3σ. EN171 covalently targets C38 and C96 on 14-3-3 to enhance the interaction between 14-3-3 and ERα, YAP, and TAZ (with EC50 values of 9 μM for human ERα, 45 μM for YAP, and 107 μM for TAZ). EN171 inhibits the transcriptional activity of estrogen receptors and the Hippo pathway in breast cancer cells. EN171 can be used in studies related to breast cancer.
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- Reinheit: 98.14%
- CAS. Nr.: 2191110-79-7
- Formel: C17H22N2O
- Molecular Weight:270.37
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Speicherung:Pure form -20°C, 3 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
EN171 stabilizes the interaction between purified human 14-3-3σ protein and phosphorylated ERα peptide, with an EC50 of 9 μM after 1 h of incubation[2].
EN171 stabilizes the interaction between purified human 14-3-3σ protein and phosphorylated YAP peptide, with an EC50 of 45 μM after 1 h of incubation[2].
EN171 stabilizes the interaction between purified human 14-3-3σ protein and phosphorylated TAZ peptide, with an EC50 of 107 μM after 1 hour of incubation[2].
EN171 stabilizes the interaction between purified human 14-3-3σ protein and phosphorylated MYC peptide, with an EC50 of 253 μM[2].
EN171 stabilizes the interaction between purified human 14-3-3σ protein and the phosphorylated CDC25B peptide, with an EC50 of 187 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:T47D breast cancer cells
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Concentration:50 μM (EN171-alkyne)
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Incubation Time:1 h
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Result:Increased 14-3-3σ levels by ~14-fold compared to vehicle treatment after enrichment.
Showed no enrichment of the unrelated protein GAPDH.
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Cell Line:T47D breast cancer cells expressing FLAG-tagged 14-3-3σ wild-type or C38S/C96S mutant
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Concentration:100 μM
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Incubation Time:24 h
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Result:Induced ternary complex formation between wild-type 14-3-3σ and endogenous ERα.
Abrogated ternary complex formation in cells expressing the C38S/C96S mutant 14-3-3σ.
Chemical Information
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CAS. Nr. 2191110-79-7
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Appearance Oil
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Molecular Weight 270.37
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Formel C17H22N2O
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Color Colorless to off-white
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SMILES
O=C(N1CCC2(CN(CC2)CC3=CC=CC=C3)C1)C=C
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Pure form -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 25 mg/mL (92.47 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 (283 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)
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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.6986 mL | 18.4932 mL | 36.9864 mL | 92.4659 mL |
| 5 mM | 0.7397 mL | 3.6986 mL | 7.3973 mL | 18.4932 mL | |
| 10 mM | 0.3699 mL | 1.8493 mL | 3.6986 mL | 9.2466 mL | |
| 15 mM | 0.2466 mL | 1.2329 mL | 2.4658 mL | 6.1644 mL | |
| 20 mM | 0.1849 mL | 0.9247 mL | 1.8493 mL | 4.6233 mL | |
| 25 mM | 0.1479 mL | 0.7397 mL | 1.4795 mL | 3.6986 mL | |
| 30 mM | 0.1233 mL | 0.6164 mL | 1.2329 mL | 3.0822 mL | |
| 40 mM | 0.0925 mL | 0.4623 mL | 0.9247 mL | 2.3116 mL | |
| 50 mM | 0.0740 mL | 0.3699 mL | 0.7397 mL | 1.8493 mL | |
| 60 mM | 0.0616 mL | 0.3082 mL | 0.6164 mL | 1.5411 mL | |
| 80 mM | 0.0462 mL | 0.2312 mL | 0.4623 mL | 1.1558 mL |
EN171 Related Classifications
HY-W1005067 Related Classifications
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