tgfβrii

LY-364947 (HTS466284) is a potent ATP-competitive inhibitor of TGFβR-I.

TGFβRII-IN-2 (Compound 3n) acts as an inhibitor of TGFβRII with an IC50 of 2.4 μM. It effectively blocks the transition from epithelial to mesenchymal states and inhibits cell migration in various cancer cell lines without disrupting the microtubule network.

TGFβRII-IN-3 (Compound 2r) is a selective inhibitor of the TGFβ type II receptor (TGFβ RII) with an IC50 of 4.1 μM. It inhibits TGFβ signaling by promoting protein degradation of TGFβ RII. Additionally, TGFβRI-IN-7 can block the transition from endothelial to mesenchymal states and inhibit cell migration, making it useful for cancer research.

Bintrafusp alfa (M7824) is a bifunctional fusion protein consisting of the extracellular structural domain of TGF-βRII (a TGF-β "trap") fused to a monoclonal antibody against human immunoglobulin G1 fused to programmed death ligand 1 (PD-L1), which is known for its anticancer activity, and can be used to study esophageal cancer. It has anticancer activity and can be used to study esophageal cancer.

Galunisertib (LY2157299) is a TGF-β receptor type I (TGF-βRI) inhibitor (IC50=56 nM) that is selective. Galunisertib has antitumor activity and can be used in combination with PD-1 inhibitors.

TGFβRI-IN-1 is an orally active and selective inhibitor of TGFβ receptor type I (TGFβRI) kinase, with IC50 values of 2 nM and 7.6 μM for TGFβRI and TGFβRII, respectively.