EN171 | 14-3-3 modulator | Probechem Biochemicals

Chemical Structure : EN171

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EN171 (EN-171)

货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	270.38
分子式	C17H22N2O
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	1-(7-benzyl-2,7-diazaspiro[4.4]nonan-2-yl)prop-2-en-1-one

参考文献

1. Qian Shao, et al. bioRxiv. 2023 Nov 6:2023.11.06.565850.

EN171 (EN-171)

生物&药学活性

物理化学性质&存储条件

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EN171 (EN-171)

生物&药学活性

物理化学性质&存储条件

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