An inhibitor of TGF-β signaling
SMAD3 is a receptor-regulated intracellular protein that functions downstream of TGF-β and activin receptors and mediates their signaling, playing a role in cell proliferation, differentiation, apoptosis and formation of extracellular matrix. SMAD3 Inhibitor, SIS3 selectively inhibits TGF-β and activin signaling by suppressing Smad3 phosphorylation (IC50 = 3 µM) without affecting the MAPK/p38, ERK, or PI3-kinase signaling pathways.[1] It has been shown to reduce TGF-β1-induced type 1 procollagen expression and myofibroblast differentiation in normal dermal fibroblasts as well as scleroderma fibroblasts.[1]
Reference:
[1]. Jinnin, M., Ihn, H., and Tamaki, K. Characterization of SIS3, a novel specific inhibitor of Smad3, and its effect on transforming growth factor-β1-induced extracellular matrix expression. Molecular Pharmacology 69(2), 597-607 (2006).
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