TED-347 |
Catalog No.GC39540 |
TED-347은 TEAD4⋅Yap1 단백질-단백질 상호작용에 대해 5.9μM의 EC50을 갖는 YAP-TEAD 단백질-단백질 상호작용에서 강력하고 비가역적이며 공유 및 알로스테릭 억제제입니다. TED-347은 10.3μM의 Ki로 TEAD4의 중앙 포켓 내에서 Cys-367과 구체적이고 공유적으로 결합합니다. TED-347은 TEAD 전사 활성을 차단하고 항종양 활성을 갖는다.
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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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