MYF-03-69

MYF-03-69 is a small molecule inhibitor of TEA/TEF-domain (TEAD) transcription factors, specifically targeting the TEAD palmitoylation pocket. Developed by researchers at the Dana-Farber Cancer Institute and the Broad Institute, it is designed to disrupt Hippo pathway signaling, which is frequently dysregulated in cancers such as mesothelioma. While single-agent TEAD inhibition typically induces cell cycle arrest, MYF-03-69 has demonstrated potent growth suppression in Hippo-mutated models. Recent research indicates that combining MYF-03-69 with EZH2 inhibitors can overcome resistance and induce apoptosis through the activation of tumor-intrinsic innate immune signaling.