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Chemical Structure : EN171
Catalog No.: PC-21486Not For Human Use, Lab Use Only.
EN171 is 14-3-3 molecular glue that covalently targets 14-3-3 to enhance 14-3-3 interactions with ERa (EC50=9 uM), YAP, and TAZ, impairs estrogen receptor and Hippo pathway transcriptional activity.
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EN171 is 14-3-3 molecular glue that covalently targets 14-3-3 to enhance 14-3-3 interactions with ERa (EC50=9 uM), YAP, and TAZ, impairs estrogen receptor and Hippo pathway transcriptional activity.
EN171 causes dose-responsive stabilization of 14-3-3s with YAP and TAZ phosphopeptides with EC50 of 45 and 107 uM, respectively.
EN171 does not stabilize 14-3-3 interactions with phosphopeptide substrates from USP8, p65, c-RAF, TP53, SOS1, or ABL1 at 1 mM.
EN171 also could be used as a covalent 14-3-3 recruiter in heterobifunctional molecules to sequester nuclear neo-substrates such as BRD4 into the cytosol.
EN171 dose-responsively impairs both ERa and Hippo transcriptional activity in T47D and MCF7 breast cancer cells, respectively.
| M.Wt | 270.38 | |
| Formula | C17H22N2O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Qian Shao, et al. bioRxiv. 2023 Nov 6:2023.11.06.565850.
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