pan-TEAD-IN-1

pan-TEAD-IN-1 (Compound 3) is an orally active pan-TEAD inhibitor targeting the palmitoylation site of TEAD, disrupting its interaction with the coactivators YAP/TAZ, thereby suppressing the transcriptional upregulation of oncogenes (e.g., Ctgf and Cyr61) in the Hippo signaling pathway. pan-TEAD-IN-1 exhibits excellent activity with a luciferase IC₅₀ of 0.36 nM and an H226 cell IC₅₀ of 1.52 nM. It also shows favorable pharmacokinetics (AUC_0–∞ = 228.7 μg/mL·min, T_1/2 = 183.9 min). In TEAD-dependent xenograft mouse models, pan-TEAD-IN-1 significantly inhibited tumor growth, showing promise for research in TEAD-dependent cancers.

• Data Sheet (266 KB)