2191110-79-7
Chemical Structure
EN171
- CAS No.: 2191110-79-7
- Formula:C17H22N2O
- Molecular Weight:270.37
InChIKey: VKQVCQHCQMFBNJ-UHFFFAOYSA-N
SMILES: O=C(N1CCC2(CN(CC2)CC3=CC=CC=C3)C1)C=C
Biological Activity: 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[1][2].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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EN171 | 98.14% | 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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References
- [1]. Shao Q, et al. Covalent 14-3-3 molecular glues and heterobifunctional molecules against nuclear transcription factors and regulators[J]. BioRxiv, 2023.
- [2]. Shao Q, et al. Targeted Protein Localization by Covalent 14-3-3 Recruitment. Journal of the American Chemical Society. 2024 Sep 11;146(36):24788-24799. [Content Brief]
