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PD 169316

CAS No. : 152121-53-4

MCE 站：PD 169316

产品活性：PD 169316 是一种高效，细胞透过的，有选择性的 p38 MAP kinase 抑制剂，IC₅₀ 值为 89 nM。PD169316 选择性地抑制磷酸化 p38 的激酶活性，但不阻碍上游激酶磷酸化 p38。PD169316 显示对 Enterovirus71 有抗病毒活性。

研究领域：MAPK/ERK Pathway  |  Autophagy  |  Anti-infection

作用靶点：p38 MAPK  |  Autophagy  |  Enterovirus

In Vitro: PD169316 (10 μM) inhibits TGFβ and Activin A, but not BMP4 signaling in CaOV3 cells. PD169316 (0.2-20 μM) inhibits TGFβ-induced Smad2 nuclear translocation, Smad7 mRNA induction, and reporter gene activity in CaOV3 cells. PD169316 (10 μM) shows a significantly increased rate of proliferation in Nestin knockdown cells, and can rescue the effect of Nestin knockdown on cell viability in the absence of EGF. PD169316 significantly inhibits p38 MAP kinase activity with no significant change in ERK activity in PC12 cells. PD169316 (10 μM) blocks apoptosis induced by trophic factor withdrawal in differentiated PC12 cells.PD169316 (10 μM, 30 min) selectively inhibits the kinase activity of the phosphorylated p38 without hindering upstream kinases to phosphorylate p38. Increased phospho p-38 levels in the presence of PD169316 are most likely due to blockade of negative feedback loop of dephosphorylation of p38 MAPK by MAPK phosphatases.

In Vivo: PD169316 (1 mg/kg, intramuscular injection every day for 14 consecutive days) shows antiviral activity in a suckling mouse model.

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