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VT103 is an inhibitor of TEA domain transcription factor 1 (TEAD1; IC50 = 1.02 nM).1 It inhibits TEAD autopalmitoylation in HEK293 cells expressing TEAD1 but not HEK293 cells expressing TEAD2, TEAD3, or TEAD4 when used at a concentration of 3 µM. VT103 also inhibits palmitoylation of endogenous TEAD1 in NCI-H2373 pleural mesothelioma cells. In vivo, VT103 (0.3-10 mg/kg) reduces tumor volume in NCI-H2373 and NCI H226 mesothelioma mouse xenograft models.
WARNING This product is not for human or veterinary use.
1. Small molecule inhibitors of TEAD auto-