GNE-7883 (GNE7883) is a potent, reversible, allosteric inhibitor of the YAP1-TEAD interaction.
The potent inhibition of pan-TEAD lipidation with GNE-7883 translated well to the disruption of YAP1 binding to each of the four TEAD isoforms by the YAP1 HTRF assay.
GNE-7883 potently inhibited proliferation of the OVCAR-8 and NCI-H226 cells, with EC50 values of 115 nM and 333 nM, respectively.
GNE-7883 (250 mg/kg, subcutaneous dosing) showed strong in vivo tumor growth inhibition (TGI) of 102% in the mesothelioma NCIH226 xenograft mouse model.
