SB-525334

SB-525334 is a potent inhibitor of the TGF-beta receptor 1 (TGF-beta R1, ALK5) kinase (IC50 = 14.36 nM). It is ~4-fold less effective against ALK4 and inactive against ALK2, ALK3, and ALK6. SB-525334 blocks TGF-beta1-induced phosphorylation and nuclear translocation of SMAD2/3 as well as TGF-beta1-directed gene expression. It is effective in vivo, preventing puromycin aminonucleoside-induced renal fibrosis and bleomycin-induced pulmonary fibrosis. SB-525334 also modulates carcinogenesis and suppresses the development of pulmonary arterial hypertension in animals.Formal Name: 6-[2-(1,1-dimethylethyl)-5-(6-methyl-2-pyridinyl)-1H-imidazol-4-yl]-quinoxaline. CAS Number: 356559-20-1. Synonyms: TGF-beta RI Kinase Inhibitor VIII. Molecular Formula: C21H21N5. Formula Weight: 343.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 20 mg/ml, Ethanol: 30 mg/ml, Ethanol:PBS(pH 7.2) (1:1): 0.5 mg/ml. lambdamax: 235, 365 nm. SMILES: CC(C)(C)C(N1)=NC(C2=CC=CC(C)=N2)=C1C(C=C3)=CC4=C3N=CC=N4. InChi Code: InChI=1S/C21H21N5/c1-13-6-5-7-16(24-13)19-18(25-20(26-19)21(2,3)4)14-8-9-15-17(12-14)23-11-10-22-15/h5-12H,1-4H3,(H,25,26). InChi Key: DKPQHFZUICCZHF-UHFFFAOYSA-N.