DM243 is an EPAC1 activator and STAT3 modulator with an pIC50 of 4.769. DM243 increases GTP-bound Rap1 levels in EPAC1-expressing cells, with no activation of EPAC2 or PKA. DM243 reduces IL-6/IL-6Ralpha-evoked STAT3 phosphorylation in endothelial cells. DM243 suppresses TGF-beta1-induced fibroblast-to-myofibroblast transition, reducing alpha-smooth muscle actin and Collagen I levels in lung fibroblasts. DM243 exhibits minimal cytotoxicity in normal human lung fibroblasts[1].
Molekulargewicht:
395.41
CAS Nummer:
[3106606-59-8]
Formel:
C22H21NO6
Target-Kategorie:
Acyltransferase,STAT
Anwendungsbeschreibung:
MCE Product type: Reference compound
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