K-975

K-975 is a first-in-class TEAD inhibitor, directly inhibiting YAP/TAZ-TEAD protein-protein interaction and showing a potent anti-tumor effect in malignant pleural mesothelioma. K-975 was covalently bound to an internal cysteine residue located in the palmitate-binding pocket of TEAD. K-975 had a strong inhibitory effect against protein-protein interactions between YAP1/TAZ and TEAD in cell-free and cell-based assays.