DM243

DM243 is an EPAC1 activator and STAT3 modulator with a pIC50 of 4.769. It increases the levels of GTP-bound Rap1 in cells expressing EPAC1 without activating EPAC2 or PKA. DM243 reduces STAT3 phosphorylation levels in endothelial cells induced by IL-6/IL-6Rα. This compound inhibits the transformation of fibroblasts into myofibroblasts induced by TGF-β1, thereby decreasing the levels of α-smooth muscle actin and type I collagen in pulmonary fibroblasts. DM243 exhibits very low cytotoxicity in normal human lung fibroblasts.