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Chemical Structure : MYF-01-037
CAS No.: 2416417-65-5
Catalog No.: PC-73155Not For Human Use, Lab Use Only.
MYF-01-37 is a novel covalent TEAD inhibitor targeting Cys380, binds to palmitoylation pocket in TEAD1, targets YAP dependency upon combined EGFR/MEK inhibition.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 25 mg | $158 | In stock | |
| 100 mg | $348 | In stock | |
| 250 mg | $548 | In stock | |
| 1 g | Get quote |
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MYF-01-037 (MYF-01-37) is a novel covalent TEAD inhibitor targeting Cys380, binds to palmitoylation pocket in TEAD1, targets YAP dependency upon combined EGFR/MEK inhibition.
MYF-01-037 exhibited 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-01-037 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
| M.Wt | 298.309 | |
| Formula | C15H17F3N2O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
1-(3-methyl-3-((3-(trifluoromethyl)phenyl)amino)pyrrolidin-1-yl)prop-2-en-1-one |
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1. Kari J Kurppa, et al. Cancer Cell. 2020 Jan 13;37(1):104-122.e12.
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