In recent years, galunisertib (LY2157299 monohydrate), a selective, small molecule that can be taken orally to inhibit TGF-β receptor I kinase, exhibits antitumor activity across various cancer models, including breast, colon, lung, and HCC, by specifically downregulating SMAD2 phosphorylation and inhibiting the canonical TGF-β pathway (Herbertz et al., 2015). The gene discussed is TGFB1; the disease is cancer.