DM245 is an EPAC1 activator and STAT3 phosphorylation inhibitor with a target pIC 50 of 4.801. DM245 activates EPAC1 to increase Rap1-GTP levels, with no activation of EPAC2 or PKA . DM245 reduces IL-6/IL-6Rα-evoked STAT3 phosphorylation in endothelial cells. DM245 suppresses TGF-β1-induced fibroblast-to-myofibroblast transition, reducing αSMA and Collagen I levels. DM245 exhibits minimal cytotoxicity in normal human lung fibroblasts, with negligible loss of intact nuclei after 72 h exposure.
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