APS-2-79 is a KSR -dependent MEK antagonist. APS-2-79 inhibits ATP biotin binding to KSR2 within the KSR2-MEK1 complexe with an IC 50 of 120 nM. APS-2-79 makes the stabilization of the KSR inactive state antagonizes oncogenic Ras-MAPK signaling
In Vitro
APS-2-79 (5 μM) suppresses KSR-stimulated MEK and ERK phosphorylation in 293H cells. APS-2-79 (1 μM) enhances the efficacy of the clinical MEK inhibitor trametinib within cancer cell lines containing K-Ras mutationsMCE has not independently confirmed the accuracy of these methods. They are for reference only.