产品描述
| 敏感性 | 对热敏感 |
| 溶解性 | Soluble in DMSO (6.5 mg/ml), anhydrous DMSO (25 mg/ml), ethanol (0.6 mg/ml), dichloromethane, methanol, DMF (~20 mg/ml), and DMSO:PBS (1:9 pH7.2) (~0.25 mg/ml). Insoluble in 2-hydroxypropyl-β-cyclodextrin, water, and dilute aqueous acid. |
| 存贮条件 | 储存温度-20°C |
| 应用 | A selective inhibitor of MEK and blocker of MAP |
| 产品介绍 | PD98059是一种非ATP竞争性的MEK抑制剂，无细胞试验中IC50为2 μM，特异性抑制MEK-1介导的MAPK激活；不直接抑制ERK1或ERK2。 |
| 备注 | PD98059 is a non-ATP competitive MEK inhibitor with IC50 of 2 μM, specifically inhibits MEK-1-mediated activation of MAPK; does not directly inhibit ERK1 or ERK2. |
| 生化机理 | PD 98059 is a potent, selective and reversible cell permeable inhibitor of MEK-1 (MAPKK1 or MAPKs ) that binds to the inactive form of MEK-1, blocking MEK-1 activation and leading to inhibition of phosphorylation and the activation of MAP kinase. In PC12 pheochromocytoma cells, it produced complete blockage of any increase in MAPK activity (IC50 = 2 μM) produced by nerve growth factor. It has been shown to enhance self-renewal of embryonic stem cells and has been used to unravel the role of the MAPK cascade in biological systems. The compound has been reported to induce GSTA2 (glutathione S-transferase A2) production in H4IIE cells. PD 98059 has also been shown to enhance insulin-mediated increase in glutathione levels as well as, independent of MEK1 inhibition, elevate primary cultured rat hepatocyte glutathione levels. |
| 别名 | PD 98059;PD-98059;2-(2-氨基-3-甲氧苯基)色酮; 2-(2-氨基-3-甲氧苯基)-4H-1-苯并吡喃-4-酮;PD 98059; PD-98059;PD 98,059; 2-(2-Amino-3-methoxyphenyl)-4H-1-benzopyran-4-one;2-(2-Amino-3-methoxyphenyl)chromone;2′-Amino-3′-methoxyflavone |
