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.
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.
