SF-3-030 is a novel ATP-dependent/catalytic site inhibitor of ERK1/2, inhibits A375 cell viability with IC50 of 4.9 uM.
SF-3-030 showed selective inhibition of cancer cell lines with activating mutations in the ERK1/2 pathway.
SF-3-030 inhibited viability of four melanoma cell lines containing either BRAF or NRas mutations with IC50 of 5-10 uM.
SF-3-030 selectively regulates ERK-dependent immediate early gene expression, causes differential changes in AP-1 protein levels characterized by inhibition of Fra-1, FosB, and the alternative splice variant FosB2 but no effect on c-Fos levels, and induces ROS mediates inhibition of A375 cell proliferation.
