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SB525334,TGFBR1抑制剂

SB525334 （订货以英文为准）

编号：S129327
CAS号：356559-20-1
分子式：C21H21N5
分子量：343.42
货号 品牌 包装 目录价 您的价格 库存 数量 购买
S129327-10mg 阿拉丁 10mg ¥165.90
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S129327-50mg 阿拉丁 50mg ¥739.90
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S129327-5mg 阿拉丁 5mg ¥111.90
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S129327-1g 阿拉丁 1g ¥6119.90
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S129327-100mg 阿拉丁 100mg ¥1249.90
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产品名称 SB525334
中文名称 SB525334,TGFBR1抑制剂
CAS号 356559-20-1
分子式（M.F.） C21H21N5
分子量（M.W.） 343.42
储存条件 2-8°C储存
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
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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