DM243

DM243 (log concentration range; 4 h) binds to the cyclic nucleotide-binding domains of both EPAC1 and EPAC2, with a modest preference for EPAC1, as indicated by pIC₅₀ values of 4.769 and 4.436, respectively^[1].
DM243 (100 μM) potently activates the EPAC1-Rap1 signaling pathway in EPAC1-transfected U2OS cells, significantly increasing Rap1-GTP levels at a concentration of 100 μM^[1].
DM243 (1 μM) significantly attenuates IL-6/IL-6Rα-induced STAT3 phosphorylation in human umbilical vascular endothelial cells, reducing the normalized phospho-STAT3 signal to a greater extent than other tested analogues^[1].
DM243 (logarithmic concentration range; 1 h pretreatment, 72 h) suppresses TGF-β1-induced fibroblast-to-myofibroblast transition in normal human lung fibroblasts, with midmicromolar potencies (pIC₅₀ = 4.34 for αSMA, pIC₅₀ = 4.40 for Collagen I)^[1].
DM243 (logarithmic concentration range; 72 h) exhibits minimal cytotoxicity in normal human lung fibroblasts at concentrations effective for suppressing TGF-β1-induced fibroblast-to-myofibroblast transition, with only a shallow reduction in nuclear counts observed across the tested range^[1].
DM243 (1 μM) does not activate PKA in EPAC1-transfected U2OS cells, as shown by the absence of detectable phospho-VASP (Ser157) signal^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.