YAP/TAZ Inhibitor-3

YAP/TAZ inhibitor-3 is an inhibitor of the protein-protein interaction between TEA domain transcription factor (TEAD) and the transcriptional coactivators yes-associated transcriptional regulator (YAP) and its paralog, transcriptional coactivator with PDZ-binding motif (TAZ).^1,2 It inhibits TEAD1-4 palmitoylation, which is essential for the TEAD-YAP/TAZ interaction, in HEK293T cells expressing TEAD1-4 when used at a concentration of 3 µM. YAP/TAZ inhibitor-3 inhibits the proliferation of a variety of mesothelioma cells, including those with homozygous NF2 mutations (GI₅₀s = 8-74 nM) or heterozygous NF2 truncations (GI₅₀s = 178-1,511 nM), both of which lead to constitutive TEAD activation, as well as some mesothelioma cells expressing wild-type NF2 (GI₅₀s = 38->3,000 nM).¹ It also reduces tumor growth in an NCI H226 mouse xenograft model when administered at doses of 3 and 10 mg/kg.

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1. Yap, T.A., Kwiatkowski, D.J., Dagogo-Jack, I., et al. YAP/TEAD inhibitor VT3989 in solid tumors: A phase ½ trial. Nat. Med. 31(12), 4281-4290 (2025).

2. Chen, F., Su, J., Liu, Y., et al. Targeting YAP/TAZ-TEAD and their protein-protein interaction for precision cancer therapy. Eur. J. Med. Chem. 302(Pt. 2), (2026).