| 应用 |
A potent ATP-competitive inhibitor against receptor TbR-I/ALK5. |
| 产品介绍 |
SB525334是一种有效的，选择性的TGFβ receptor I (ALK5)抑制剂，IC50为14.3 nM，作用于ALK4比作用于ALK5效果低4倍，可抑制ALK2， 3，和6活性。 |
| 备注 |
SB525334 is a potent and selective inhibitor of TGFβ receptor I (ALK5) with IC50 of 14.3 nM, is 4-fold less potent to ALK4 than ALK5 and inactive to ALK2, 3, and 6. |
| 生化机理 |
TGF-β RI Kinase Inhibitor VIII is a cell-permeable quinoxaline compound that acts as a potent, highly selective, ATP-competitive inhibitor against type I TGF-β receptor TβR-I/ALK5 (IC50 = 14.3 nM), while exhibiting 4-fold less potency toward ALK4 (IC50 = 58.5 nM) and little or no activity against ALK2/3/6 and a panel of 26 other commonly studied kinases (≤29% inhibition at 10 μM). TGF-β RI Kinase Inhibitor VIII effectively blocks (by >95%) TGF-β1-induced Smad2/3 activation (2 μM in ELT-3 cultures) and nuclear localization (1 μM in RPTE cultures), as well as TGF-β1-dependent p3TP- and ARE-luciferase transcription (0.1 μM in HaCat cultures). TGF-β RI Kinase Inhibitor VIII is an inhibitor of ACTR-IB, COL1A1(procollagen α1(I)) and PAI-1(plasminogen activator inhibitor-1). |
| 别名 |
SB 525334;SB-525334; 6-[2-(1,1-二甲基乙基)-5-(6-甲基-2-吡啶基)-1H-咪唑-4-基]喹喔啉;6-[2-tert-Butyl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-4-yl]-quinoxaline;TGF-β RI Kinase Inhibitor VIII;SB-525334 |
