Galunisertib (LY2157299): Selectivity & Specificity
Galunisertib (LY2157299) is a potent inhibitor of ALK4 (80 nM), TGFBR1 (170 nM), MINK (190 nM), TGFBR2 (210 nM), RIPK2 (220 nM), CSNK1A1 (260 nM), MAP4K4 (280 nM), GAK (310 nM), CSNK1E1 (400 nM), BMPR1B (470 nM), BRAF (500 nM), TNIK (510 nM), RSK4 (720 nM), ABL1 (860 nM), ZAK (860 nM), NLK (910 nM), SMAD2, SMAD3, COL1A1, ACTA2, SERPINH1, FN1, TGFB1, TGFBR, HSP47, MIR21, CD44, THY1, SKIL, PMEPA1, AFP, MKI67, CDH1, ID1, p-TβRI, cancer stem cells, macrophage osteogenic signaling, TGF-β/Smad3 signaling pathway, and TGF-β signaling. Galunisertib (LY2157299) exhibits the greatest inhibitory potency toward ALK4 (IC50 = 80 nM).