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MYF-01-37 (1-[3-Methyl-3-[3-(trifluoromethyl)anilino]pyrrolidin-1-yl]prop-2-en-1-one) is a novel covalent TEAD inhibitor.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | $34 | In Stock | |
5 mg | $55 | In Stock | |
10 mg | $97 | In Stock | |
25 mg | $178 | In Stock | |
50 mg | $313 | In Stock | |
100 mg | $468 | In Stock | |
500 mg | $987 | In Stock | |
1 mL x 10 mM (in DMSO) | $61 | In Stock |
Description | MYF-01-37 (1-[3-Methyl-3-[3-(trifluoromethyl)anilino]pyrrolidin-1-yl]prop-2-en-1-one) is a novel covalent TEAD inhibitor. |
In vitro | 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. |
Alias | 1-[3-Methyl-3-[3-(trifluoromethyl)anilino]pyrrolidin-1-yl]prop-2-en-1-one |
Molecular Weight | 298.3 |
Formula | C15H17F3N2O |
Cas No. | 2416417-65-5 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 55 mg/ml (184.38 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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