产品描述
| 敏感性 | 对光敏感 |
| 溶解性 | Soluble in DMSO (200 mg/ml), DMF (~20 mg/ml), water (0.5 mg/ml at 25 °C), and ethanol (2 mg/ml at 25 °C). |
| 存贮条件 | 储存温度 2-8°C |
| 应用 | A potent and selective Raf-1 inhibitor. |
| 产品介绍 | ZM 336372是一种有效的，选择性的c-Raf抑制剂，IC50为70 nM，比作用于B-RAF选择性高10倍，对PKA/B/C， AMPK， p70S6等没有抑制作用。 |
| 备注 | ZM 336372 is a potent and selective c-Raf inhibitor with IC50 of 70 nM, 10-fold selectivity over B-RAF, no inhibition to PKA/B/C, AMPK, p70S6, etc. |
| 生化机理 | ZM 336372 is a reversible, selective inhibitor of the protein kinase Raf-1 (IC50 = 70nM). Although ZM 336372 weakly inhibits Raf-B, it is 10 fold more potent against Raf-1 and so is considered more selective towards this kinase. ZM 336372 inhibits Raf-1 by competing with ATP to bind to the protein. Alternate studies suggest that ZM 336372 can induce apoptosis in pancreatic adenocarcinoma cell lines by inhibiting glycogen synthase kinase-3β (GSK-3β) through phosphorylation of GSK-3&beta at Ser 9. In addition, ZM 336372 can suppress the proliferation of hepatocellular carcinoma cells by inhibiting hormone secretion and up-regulating cell cycle inhibitors. Furthermore, ZM 336372 can also act as an agonist towards Raf-1, activating the MAPK pathway, which can be suppressed after activation by Raf-1 itself, using a novel feedback loop in which activation is always followed by inactivation. ZM 336372 is an inhibitor of p38 α and p38 β. |
| 别名 | ZM336372; ZM-336372; 3-(二甲基氨基)-N-[3-[(4-羟基苯甲酰基)氨基]-4-甲基苯基]苯甲酰胺;3-(Dimethylamino)-N-[3-[(4-hydroxybenzoyl)amino]-4-methylphenyl]-benzamide;ZM336372; ZM-336372 |
