Chemical Structure : EN171
CAS No.:
2191110-79-7
EN171
(EN 171)
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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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270.38
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Formula
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C17H22N2O
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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1-(7-benzyl-2,7-diazaspiro[4.4]nonan-2-yl)prop-2-en-1-one
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References
1. Qian Shao, et al. bioRxiv. 2023 Nov 6:2023.11.06.565850.
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