SB-525334

SB-525334

CAT N°: 16281
Price:

From 49.00 41.65

SB-525334 is a potent inhibitor of the TGF-? receptor 1 (TGF-? R1, ALK5) kinase (IC50 = 14.36 nM).{27599} It is ~4-fold less effective against ALK4 and inactive against ALK2, ALK3, and ALK6.{27599} SB-525334 blocks TGF-?1-induced phosphorylation and nuclear translocation of SMAD2/3 as well as TGF-?1-directed gene expression.{27599} It is effective in vivo, preventing puromycin aminonucleoside-induced renal fibrosis and bleomycin-induced pulmonary fibrosis.{27599,27600,27601} SB-525334 also modulates carcinogenesis and suppresses the development of pulmonary arterial hypertension in animals.{27601,27602,27603}

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • 6-[2-(1,1-dimethylethyl)-5-(6-methyl-2-pyridinyl)-1H-imidazol-4-yl]-quinoxaline
  • Correlated keywords
    • SB525334 SB-525334 TGF? RI kinase inhibitor VIII TGF ? potent ATP-competitive receptor TbR-I/ALK5 TbR-I ALK5 TbRI ALK-5 ALK 5 TbR I transforming growths factor-? TGF-?RI factors TGF?RI TGF ?RI cell-permeable quinoxalines compound cell permeable ATPs competitive TGF-b types Smad2/3 activation Smad2 Smad3 Smad-2 Smad-3 2 3 Smad nuclear localization TGF-b1-dependent p3TP-luciferase luciferase p3TP ARE-luciferase transcription ARE CTR-IB CTP IB CTPIB COL1A1 procollagen ?1 and PAI-1 PAI1 PAI 1 plasminogen activator inhibitor-1 T?R-I mRNA expression kidney cells bleomycin-induced pulmonary fibrosis bleomycin renal proximal tubule biochemistry intracellular signaling signal transduction biochemical cancer hypertension translocation gene
  • Product Overview:
    SB-525334 is a potent inhibitor of the TGF-? receptor 1 (TGF-? R1, ALK5) kinase (IC50 = 14.36 nM).{27599} It is ~4-fold less effective against ALK4 and inactive against ALK2, ALK3, and ALK6.{27599} SB-525334 blocks TGF-?1-induced phosphorylation and nuclear translocation of SMAD2/3 as well as TGF-?1-directed gene expression.{27599} It is effective in vivo, preventing puromycin aminonucleoside-induced renal fibrosis and bleomycin-induced pulmonary fibrosis.{27599,27600,27601} SB-525334 also modulates carcinogenesis and suppresses the development of pulmonary arterial hypertension in animals.{27601,27602,27603}

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