TM2 TEAD inhibitor is an effective and reversible inhibitor of TEA domain transcription factors, exhibiting IC50 values of 38 nM and 156 nM for TEAD4 auto-palmitoylation and TEAD2 palmitoylation, respectively. TM2 TEAD inhibitor blocks TEAD-YAP binding and suppresses its transcriptional activity, exhibiting significant antiproliferative effects in YAP-dependent cancer cells. It demonstrates potent efficacy both as a monotherapy and in combination with MEK inhibitors. Furthermore, TM2 TEAD inhibitor strongly inhibits YAP-dependent liver organoid growth in vitro, supporting its potential application as an anticancer therapeutic strategy.
Molekulargewicht:
435.57
Reinheit:
99.91%
CAS Nummer:
[1008768-41-9]
Formel:
C26H33N3O3
Target-Kategorie:
YAP
T83951
T83951
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