MYF-01-37 是共价TEAD抑制剂，靶向 Cys380，能够可逆地抑制 YAP/TEAD 相互作用。

MYF-01-37 is a novel covalent TEAD inhibitor.

Pretreating cells with MYF-01–37 led to loss of direct TEAD pull-down by biotin-MYF-01–037 ?from whole-cell lysate, confirming MYF-01–037 binding to TEAD in cells.?This target engagement of TEAD resulted 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.?This reduction was abrogated by the overexpression of TEAD1 C359S mutant that disrupts the covalent binding of the drug to TEAD, but not by overexpression of wild-type TEAD1, demonstrating that the observed inhibition of YAP activity is due to on-target covalent binding of the compound to TEAD.

2416417-65-5

C15H17F3N2O

298.309

1-[3-Methyl-3-[3-(trifluoromethyl)anilino]pyrrolidin-1-yl]prop-2-en-1-one

DMSO:55 mg/ml (184.38 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years