MYF-01-37 is a covalent TEAD inhibitor targeting Cys380. MYF-01-37 has a reversible inhibition on YAP/TEAD interaction[1].
MYF-01-37 (10 μM; 24h) results in inhibition of direct YAP/TEAD interaction in HEK 293T cells, and in the reduction in canonical YAP target gene CTGF expression in PC-9 cells[1]. MYF-01-37 (0.1, 1, 10, 100 μM) has minimal impact on cell viability of several EGFR-mutant NCSLC cell lines[1]. MYF-01-37 (10 μM; 10 days) combinated with OT (combination of osimertinib and trametinib) leads to a dramatic decrease in dormant cells compared to OT alone[1].
[1]. Kari J Kurppa, et al. Treatment-Induced Tumor Dormancy through YAP-Mediated Transcriptional Reprogramming of the Apoptotic Pathway. Cancer Cell. 2020 Jan 13;37(1):104-122.e12.