A wide range of cellular functions such as cell proliferation, differentiation, adhesion, migration, and apoptosis are regulated by TGF-β superfamily members. The TGF-βs include the three major TGF-β isoforms, TGF-β1, TGF-β2, and TGF-β3 which are expressed in mammals. TGF-β transduces signals through a complex of two related but structurally and functionally distinct serine/threonine kinase receptors, termed type 1 and type II. Deregulation of TGF-β signaling has been also implicated in various human diseases including cancer, pancreatic diseases, and hematological malignancies.