VT-107, as an analogous to VT104, is an orally active and potent pan-TEAD auto-palmitoylation inhibitor. VT-107 can be used for the research of cancer
In Vitro
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. ?\nVT107 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: HEK293T cells Concentration: 3 μmol/L Incubation Time: 20 hours Result: Inhibited palmitoylation of both endogenous TEAD1 and TEAD3 proteins and was the most potent at blocking the palmitoylation of endogenous TEAD4 protein.
In Vivo
VT107 (10 mg/kg; p.o.) is a enantiomer analogous to VT104 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Mouse Dosage: 10 mg/kg (Pharmacokinetic Analysis) Administration: P.o. Result: Enantiomer analogous to VT104.
