TED-347 |
Katalog-Nr.GC39540 |
TED-347 ist ein potenter, irreversibler, kovalenter und allosterischer Inhibitor der YAP-TEAD-Protein-Protein-Wechselwirkung mit einem EC50-Wert von 5,9 μM fÜr die TEAD4⋅Yap1-Protein-Protein-Wechselwirkung. TED-347 bindet spezifisch und kovalent an Cys-367 innerhalb der zentralen Tasche von TEAD4 mit einem Ki von 10,3 μM. TED-347 blockiert die TranskriptionsaktivitÄt von TEAD und hat eine AntitumoraktivitÄt.
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Cas No.: 2378626-29-8
Sample solution is provided at 25 µL, 10mM.
TED-347 is a potent, irreversible, covalent and allosteric inhibitor at YAP-TEAD protein-protein interaction with an EC50 of 5.9 μM for TEAD4⋅Yap1 protein-protein interaction. TED-347 specifically and covalently bonds with Cys-367 within the central pocket of TEAD4 with a Ki of 10.3 μM. TED-347 blocks TEAD transcriptional activity and has antitumor activity[1].
[1]. Khuchtumur Bum-Erdene, et al. Small-Molecule Covalent Modification of Conserved Cysteine Leads to Allosteric Inhibition of the TEAD⋅Yap Protein-Protein Interaction. Cell Chem Biol. 2019 Mar 21;26(3):378-389.e13.
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