tcsc0023129 LY3200882

LY3200882 is a novel and highly selective inhibitor of TGF-β receptor type 1 (TGFβRI).

IC50 & Target: TGFβRI^[1]

In Vitro: LY3200882 is a novel, highly selective inhibitor of TGF-β receptor type 1 (TGFβRI). LY3200882 potently inhibits TGFβ mediated SMAD phosphorylation in vitro in tumor and immune cells. LY3200882 has shown anti-metastatic activity in vitro in migration assays. In in vitro immune suppression assays, LY3200882 has shown the ability to rescue TGFβ1 suppressed or T regulatory cell suppressed naïve T cell activity and restore proliferation^[1].

In Vivo: LY3200882 potently inhibits TGFβ mediated SMAD phosphorylation in vivo in subcutaneous tumors in a dose dependent fashion. LY3200882 has shown anti-metastatic activity in vivo in an experimental metastasis tumor model (intravenous EMT6-LM2 model of triple negative breast cancer)^[1].