VT-107

VT-107 is an orally active, potent small molecule pan-TEAD auto-palmitoylation inhibitor. It functions by specifically inhibiting YAP/TAZ-TEAD-dependent transcription, a key component of the Hippo signaling pathway that is frequently co-opted in oncogenesis. By blocking the palmitoylation of TEAD proteins—specifically TEAD1, TEAD3, and TEAD4—VT-107 prevents the assembly of the functional YAP/TAZ-TEAD transcriptional complex. This inhibition leads to reduced expression of genes involved in cell proliferation and survival. VT-107 has shown particular efficacy in NF2-deficient mesothelioma models, where it significantly inhibits tumor growth. It is currently used as a research compound for cancer therapy development.