VT107 is a potent pan-TEAD auto-palmitoylation inhibitor (3 μM; using TEAD isotype-overexpressing HEK293T) that blocks TEAD-mediated gene transcription (IC50 = 4.93 nM) by preventing its association with YAP/TAZ. VT107 selectively inhibits the proliferation of mesothelioma cultures with NF2 mutation (NCI-H2051 IC50 = 20.4 nM), deletion (NCI-H2373 IC50 = 9.35 nM) or deficiency (NCI-H226 IC50 = 8.67 nM), but not those with wild-type NF2.
