Signaling Pathway



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TGF-β (Transforming growth factor beta) is a protein that controls proliferation, cellular differentiation, and other functions in most cells. It is a type of cytokine which plays a role in immunity, cancer, bronchial asthma, heart disease, diabetes, Hereditary hemorrhagic telangiectasia, Marfan syndrome, Vascular Ehlers-Danlos syndrome, Loeys–Dietz syndrome, Parkinson's disease and AIDS. TGF-β is a secreted protein that exists in at least three isoforms called TGF-β1, TGF-β2 and TGF-β3. TGF-β acts as an antiproliferative factor in normal epithelial cells and at early stages of oncogenesis. The SMAD pathway is the canonical signaling pathway that TGF-β family members signal through. In this pathway, TGF-β dimers bind to a type II receptor which recruits and phosphorylates a type I receptor. The type I receptor then recruits and phosphorylates a receptor regulated SMAD (R-SMAD). The R-SMAD then binds to the common SMAD (coSMAD) SMAD4 and forms a heterodimeric complex. This complex then enters the cell nucleus where it acts as a transcription factor for various genes, including those to activate the mitogen-activated protein kinase 8 pathway, which triggers apoptosis.

TGF-beta/Smad Inhibitors & Modulators (7)

Product Name Catalog No. Brief Description
Chebulinic acid


Chebulinic acid is a potent natural inhibitor of M.



Disitertide also named P144, is a inhibitor of TGF-β1.



Halofuginone is a plant derivative that has been shown to inhibit Th17 differentiation, and recently tested as a potential immunosuppressant.



Oxymatrine, an alkaloid from the roots of Sophora species, with anti-inflammatory, antifibrosis, and antitumor effects, inhibits the iNOS expression and TGF-β/Smad pathway.



Pirfenidone(AMR69) is an inhibitor for TGF-β production and TGF-β stimulated collagen production, reduces production of TNF-α and IL-1β, and also has anti-fibrotic and anti-inflammatory properties.



SIS3 is a potent and selective inhibitor of Smad3.

SRI-011381 hydrochloride


SRI-011381 hydrochloride is a TGF-beta signaling agonist.