LY-2109761

LY-2109761 is a highly potent and selective TGFβ receptor type I and type II (TβRI/II) inhibitor with Ki of 38 nM and 300 nM respectively. It has been used to study the role of TGF-β signaling in tumor cell migration and metastasis in pancreatic tumor cell lines where it completely disrupts Smad-2 phosphorylation, an immediate downstream target of the kinase activity. It can also suppress radiation-induced inflammatory cytokine signaling and proangiogenic genes, including ID1, in human primary fibrobalsts.