2-Naphthalenecarboxamide, N-[(1S)-1-(6-amino-2-pyridinyl)ethyl]-5-[4-(trifluoromethyl)phenyl]-

Biological Activity

VT-107, as an analogous to VT104, is a potent pan-TEAD auto-palmitoylation inhibitor. VT-107 can be used for the research of cancer[1]. VT107 (3 μmol/L; 20 hours; HEK293T cells) inhibits palmitoylation of both endogenous TEAD1 and TEAD3 proteins and is the most potent at blocking the palmitoylation of endogenous TEAD4 protein[1].VT107 prevents palmitoylation of the TEAD1 protein. VT107 is slightly more potent than VT104 on TEAD2 and TEAD4. VT107 results in the disappearance of palmitoylated TEAD1 with a concomitant increase in unpalmitoylated TEAD1. VT107 decreases the levels of palmitoylated TEAD3 and TEAD4 and increases the levels of unpalmitoylated TEAD3 and TEAD4. VT107 blocks YAP and TAZ interaction with both TEAD1 and TEAD4. VT107 potently inhibits the proliferation of NF2-mutated/deficient cell lines[1]. VT107 (10 mg/kg; p.o.) is a enantiomer analogous to VT104[1].

References

[1]. Tang TT, et al. Small Molecule Inhibitors of TEAD Auto-palmitoylation Selectively Inhibit Proliferation and Tumor Growth of NF2-deficient Mesothelioma. Mol Cancer Ther. 2021; 20(6):986-998.