产品描述:
SB-505124 inhibits the TGF-β1 receptor serine/threonine kinase ALK5 with an IC50 value of 47 nM.{21040} Though it is a less potent antagonist of ALK4 (IC50 = 129 nM) and ALK7, SB-505124 selectively and concentration-dependently inhibits ALK4-, ALK5-, and ALK7-dependent activation of downstream SMAD2 and SMAD3 and TGF-β–induced MAP kinase pathway components without altering ALK1-3 or ALK6-induced SMAD signaling.{21040} In an assay determining in vitro phosphorylation of SMAD3, SB-505124 is more potent than SB-431452 (Item No. 13031) with IC50 values of 47 versus 94 nM, respectively.{21040}