Specification
Description
MYF-01-37 is a novel covalent inhibitor of TEAD targeting Cys380 when incubated with the TEAD2 protein.
Synonyms
MYF-01-37; MYF 01-37; MYF01-37; MYF-0137; MYF 0137; MYF0137
IUPAC Name
1-(3-methyl-3-((3-(trifluoromethyl)phenyl)amino)pyrrolidin-1-yl)prop-2-en-1-one
Canonical SMILES
C=CC(N1CC(NC2=CC=CC(C(F)(F)F)=C2)(C)CC1)=O
InChI
InChI=1S/C15H17F3N2O/c1-3-13(21)20-8-7-14(2,10-20)19-12-6-4-5-11(9-12)15(16,17)18/h3-6,9,19H,1,7-8,10H2,2H3
InChI Key
MTBDEVWWJBIUOK-UHFFFAOYSA-N
Solubility
To be determined
Shelf Life
>2 years if stored properly
Storage
Dry, dark and at 0-4 °C for short term (days to weeks) or -20 °C for long term (months to years).
Biological Target
MYF-01-37 is a covalent TEAD inhibitor targeting Cys380. MYF-01-37 has a reversible inhibition on YAP/TEAD interaction.
Drug Formulation
To be determined
Elemental Analysis
C, 60.40; H, 5.74; F, 19.11; N, 9.39; O, 5.36
HS Tariff Code
2934.99.9001
In Vitro Activity
MYF-01-37 was developed as a covalent binder to TEAD, targeting Cys380 when incubated with the TEAD2 protein (C359 in TEAD1). 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.
Reference: Cancer Cell. 2020 Jan 13; 37(1): 104-122.e12. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7146079/
Shipping
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Stock Solution Storage
0-4 °C for short term (days to weeks), or -20 °C for long term (months).