MYF-01-37

MYF-01-37 is a small molecule research compound that functions as a covalent inhibitor of the Transcriptional Enhancer Associate Domain (TEAD) family of transcription factors. It specifically targets the conserved cysteine residue (Cys380 in TEAD2 and Cys359 in TEAD1) located within the palmitate-binding pocket of the TEAD protein. By covalently binding to this site, MYF-01-37 disrupts the interaction between TEAD and its transcriptional co-activator Yes-associated protein (YAP), a central component of the Hippo signaling pathway. This disruption leads to the suppression of YAP-TEAD-mediated transcriptional activity and the downregulation of downstream target genes such as CTGF. Research has demonstrated that MYF-01-37 can enhance the efficacy of EGFR and MEK inhibitors, such as osimertinib and trametinib, in EGFR-mutant non-small-cell lung cancer (NSCLC) models, suggesting a potential role in overcoming adaptive resistance to targeted therapies. It is currently utilized as a chemical probe in oncology research and is not approved for clinical use.

Other names

1-(3-methyl-3-((3-(trifluoromethyl)phenyl)amino)pyrrolidin-1-yl)prop-2-en-1-oneCAS 2416417-65-5CAS2416417-65-5CAS-2416417-65-5