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Description: SIS3 HCl is a potent and selective inhibitor of Smad3 which is a receptor-regulated intracellular protein that functions downstream of TGF-beta and activin receptors and mediates their signaling, playing a role in cell proliferation, differentiation, apoptosis and formation of extracellular matrix. SIS3 can block excessive ECM production from the TGF-beta1-treated normal fibroblasts and scleroderma fibroblasts, the model of cells with autocrine TGF-beta signaling in vitro. Addition of SIS3 attenuates the effects of TGF-beta1 by reducing the transcriptional activity. SIS3 also inhibits the myofibroblast differentiation of fibroblasts by TGF-beta1.
References: Mol Pharmacol. 2006 Feb; 69(2):597-607. Epub 2005 Nov 15.
Related CAS#: 1009104-85-1 (free base); 521984-48-5 (HCl)
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