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VT107 is an inhibitor of the protein-protein interaction between YAP/TAZ and TEAD1 or TEAD4.1 It inhibits autopalmitoylation of TEAD1-4 in HEK293 cells expressing the human transcription factors when used at 3 µM and inhibits YAP/TAZ-TEAD transcriptional activity in a cell-based reporter assay (IC50 = 4.93 nM). VT107 inhibits the growth of NF2-deficient NCI-H2052 and NCI-H2373 mesothelioma and NCI H226 lung cancer cells (IC50s = 20.4, 9.35, and 8.67 nM, respectively) but not wild-type NF2-expressing NCI H28, NCI 2452, or MSTO-211H cells (IC50s = 2,790, >3,000, and >3,000 nM, respectively).
WARNING This product is not for human or veterinary use.
1. Small molecule inhibitors of TEAD auto-