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MYF-01-37

Chemical Structure : MYF-01-37

CAS No.: 2416417-65-5

MYF-01-37 (MYF-1-37)

Catalog No.: PC-73155Not For Human Use, Lab Use Only.

MYF-01-37 (MYF-1-37) is a novel covalent TEAD inhibitor targeting Cys380, binds to palmitoylation pocket in TEAD1, targets YAP dependency upon combined EGFR/MEK inhibition.

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Biological Activity

MYF-01-37 (MYF-1-37) is a novel covalent TEAD inhibitor targeting Cys380, binds to palmitoylation pocket in TEAD1, targets YAP dependency upon combined EGFR/MEK inhibition.
MYF-01-37 (MYF-1-37) exhibits inhibition of direct YAP/TEAD interaction in HEK 293T cells and the reduction in canonical YAP target gene CTGF expression in PC-9 cells, this redcution effect 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.
MYF-01-37 (MYF-1-37) combined with OT completely suppressed the increased YAP activity induced by OT treatment in PC-9 YAP reporter cells, led to a robust increase in BMF expression, and to subsequent increase in apoptosis in PC-9 and HCC4006 cells compared to OT alone

Physicochemical Properties

M.Wt 298.309
Formula C15H17F3N2O
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

1-(3-methyl-3-((3-(trifluoromethyl)phenyl)amino)pyrrolidin-1-yl)prop-2-en-1-one

References

1. Kari J Kurppa, et al. Cancer Cell. 2020 Jan 13;37(1):104-122.e12.

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