SB-505124

SB-505124 inhibits the TGF-beta1 receptor serine/threonine kinase ALK5 with an IC50 value of 47 nM. 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-beta-induced MAP kinase pathway components without altering ALK1-3 or ALK6-induced SMAD signaling. In an assay determining in vitro phosphorylation of SMAD3, SB-505124 is more potent than SB-431452 (Cay-13031) with IC50 values of 47 versus 94 nM, respectively.Formal Name: 2-[4-(1,3-benzodioxol-5-yl)-2-(1,1-dimethylethyl)-1H-imidazol-5-yl]-6-methyl-pyridine. CAS Number: 694433-59-5. Molecular Formula: C20H21N3O2. Formula Weight: 335.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 17 mg/ml, Ethanol: 20 mg/ml, Ethanol:PBS (pH 7.2) (1:1): 0.5 mg/ml. SMILES: CC(C)(C)C1=NC(C2=CC(OCO3)=C3C=C2)=C(C4=NC(C)=CC=C4)N1. InChi Code: InChI=1S/C20H21N3O2/c1-12-6-5-7-14(21-12)18-17(22-19(23-18)20(2,3)4)13-8-9-15-16(10-13)25-11-24-15/h5-10H,11H2,1-4H3,(H,22,23). InChi Key: WGZOTBUYUFBEPZ-UHFFFAOYSA-N.