产品描述
| 熔点 | 230 °C |
| 溶解性 | Soluble in DMSO (100 mM), water (<1 mg/ml at 25 °C), ethanol (<1 mg/ml at 25 °C), DMF (~0.1 mg/ml), and 1:1 DMF:PBS (pH 7.2) (~0.5 mg/ml). |
| 存贮条件 | 储存温度 2-8°C |
| 应用 | A selective ATP-competitive inhibitor of TGF-β Receptor I kinase. |
| 产品介绍 | LY364947是一种有效的，ATP竞争性的TGFβR-I抑制剂，IC50为59 nM，比作用于TGFβR-II选择性高7倍。 |
| 备注 | LY364947 is a potent ATP-competitive inhibitor of TGFβR-I with IC50 of 59 nM, shows 7-fold selectivity over TGFβR-II. |
| 生化机理 | LY 364947 is a diheteroaryl-substituted pyrazole compound used as a selective, ATP-competitive inhibitor of TGF-βRI (TGF-β Receptor I kinase). Studies of mouse fibroblasts show that LY 364947 inhibits cellular growth and transcription activation via TGF-β Receptor I kinase inhibition. In addition, TGF-β Receptor I kinase is responsible for fibroblast proliferation and the accumulation of astrocytes around the fibrotic scar when injury occurs to cells. In vitro studies report that in the presence of LY 364947 the amount of reactive astrocytes at the lesion site is also reduced. Furthermore, studies show that LY 364947 strongly effects intraplug vasculature by increasing the extravasation of Dextran . LY 364947 is an inhibitor of eIF2 alpha, MLTK, p38 alpha and TGF β RII. |
| 别名 | 4-[3-(2-吡啶基)-1H-吡唑-4-基]喹啉;HTS466284; LY-364947;TGF-β RI Kinase Inhibitor; 3-(Pyridin-2-yl)-4-(4-quinonyl)]-1H-pyrazole; 4-[3-(2-pyridinyl)-1H-pyrazol-4-yl]-quinoline ;HTS 466284 ;Transforming Growth Factor-β Type I Receptor Kinase Inhibitor |
