PD98059 是一种有效的选择性的 MEK 抑制剂，IC50 为 5 µM。PD98059 与 MEK 的无活性形式结合，从而阻止上游激酶激活 MEK1 (IC50 为 2-7 µM) 和 MEK2 (IC50 为 50 µM)。PD98059 是一种 ERK1/2 信号的抑制剂。PD98059 是一种芳烃受体 (AHR) 的配体，可抑制细胞中 TCDD 结合 (IC50 为 4 µM) 和 AHR 转化 (IC50 为 1 µM)。PD98059 还可抑制细胞自噬 (autophagy)。
| CAS No. | 167869-21-8 |
| 生物活性 | PD98059 is a potent and selective MEK inhibitor with an IC50 of 5 µM. PD98059 binds to the inactive form of MEK, thereby preventing the activation of MEK1 (IC50 of 2-7 µM) and MEK2 (IC50 of 50 µM) by upstream kinases. PD98059 is a ERK1/2 signaling inhibitor. PD98059 is a ligand for the aryl hydrocarbon receptor (AHR), and suppresses TCDD binding (IC50 of 4 μM) and AHR transformation (IC50 of 1 μM). PD98059 also inhibits autophagy. |
| 分子式 | C16H13NO3 |
| 分子量 | 267.28 |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存条件 | 4°C, protect from light |
| 溶解性数据 | DMSO : 33.33 mg/mL (124.70 mM; Need ultrasonic) H2O : < 0.1 mg/mL (insoluble) |
| 体内研究 | PD98059 (10 mg/kg; i.p.; 1 and 6 hours after Zymosan) significantly reduces the level of p-ERK1/2 in zymosan-injected mice. |
| 体外研究 | PD98059 (20 μM; 24 hours) causes G1-phase cell cycle arrest in OCI-AML-3 cells. PD98059 (10 μM; 22 hours) results in concentration-dependent reductions in the dually phosphorylated forms of ERK1 and ERK2. PD98059 both prevents ERK activation and blocks formation of TDP-43 and HuR-positive SGs. |
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