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SB525334

品牌 厂商性质 产地 货期
阿拉丁 生产商 上海 现货

询价
产品参数
货号 CAS号 操作
S129327-10mg 356559-20-1 询价
S129327-1g 356559-20-1 询价
S129327-50mg 356559-20-1 询价
S129327-5mg 356559-20-1 询价
产品介绍

  • 分子式 C21H21N5
  • 分子量343.42
  • Beilstein号
  • EC号 MFCD11045307
  • MDL号
  • PubChem编号

属性

熔点 255.97 °C
溶解性 Soluble in DMSO (≥20 mg/ml), water (<1 mg/ml) at 25 °C, ethanol (69 mg/ml) at 25 °C, and 1eq. HCl (100 mM).
存贮条件 储存温度 2-8°C

描述

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

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注:该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案,不可用于临床诊断或治疗等相关用途