PD98059,167869-21-8

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PD98059

CAS No. : 167869-21-8

MCE 国际站：PD98059

产品活性：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 Mycobacterium bovis Bacillus CalmetteGuerin (BCG) 诱导的细胞自噬 (autophagy)。

研究领域：MAPK/ERK Pathway  |  Stem Cell/Wnt  |  Immunology/Inflammation  |  Autophagy

作用靶点：MEK  |  ERK  |  Aryl Hydrocarbon Receptor  |  Autophagy

In Vitro: 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.

In Vivo: PD98059 (10 mg/kg; i.p.; 1 and 6 hours after Zymosan) significantly reduces the level of p-ERK1/2 in zymosan-injected mice.

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