LY2157299 (Galunisertib) is a potent, specific inhibitor of TGF-β receptor I kinase ((TGF-βRI, ALK5) with IC50 of 56 nM.
LY2157299 (Galunisertib) inhibits TGF-β-mediated SMAD2 activation and hematopoietic suppression in primary hematopoietic stem cells in a dose-dependent manner, stimulates hematopoiesis from primary MDS bone marrow specimens.
LY2157299 (Galunisertib) ameliorates anemia in a TGF-β overexpressing transgenic mouse model of bone marrow failure.
LY2157299 (Galunisertib) displays significant antitumor activity against both Calu6 and MX1 xenografts in mice.
