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PH-797804

CAS No. : 586379-66-0

MCE 站：PH-797804

产品活性：PH-797804 是一种 ATP 竞争性的，选择性的 p38α/p38β 抑制剂，对 p38α 的 IC₅₀ 为 26 nM，K_i 值为 5.8 nM；对 p38β 的 K_i 值为 40 nM，对 JNK2 没有抑制作用.

研究领域：MAPK/ERK Pathway  |  Autophagy

作用靶点：p38 MAPK  |  Autophagy

In Vitro: PH-797804 blocks LPS-induced TNF-α production ａnd p38 kinase activity in the human monocytic U937 cell line, with comparable IC₅₀ of 5.9 nM ａnd 1.1 nM. PH-797804 has no inhibitory effect on either the JNK pathway (c-Jun phosphorylation) or ERK pathway (ERK phosphorylation) in U937 cells at concentrations up to 1 μM. PH-797804 inhibits RANKL- ａnd M-CSF-induced osteoclast formation in a concentration-dependent manner, with IC50 of 3 nM in primary rat bone marrow cells.
IC₅₀ values for PH-797804 against the following targets have been determined to be greater than 200 μM (unless specified): CDK2, ERK2, IKK1, IKK2, IKKi, MAPKAP2, MAPKAP3, MKK7 (>100 μM), MNK, MSK (>164 μM), PRAK, RSK2, ａnd TBK1, which means the activity of PH-797804 is specific.

In Vivo: Orally dosing of PH-797804 effectively inhibits acute inflammatory responses induced by systemically administered endotoxin in both rat ａnd cynomolgus monkeys. PH-797804 treatment for 10 days demonstrates robust anti-inflammatory activity in chronic disease models, significantly reducing both joint inflammation ａnd associated bone loss in streptococcal cell wall-induced arthritis in rats ａnd mouse collagen-induced arthritis. Dose-response analysis resulted in ED50 values of 0.07 mg/kg ａnd 0.095 mg/kg in rat ａnd cynomolgus monkeys, respectively. PH-797804 inhibits LPS-induced TNF-α, IL-6, ａnd MK-2 activity in a dose- ａnd concentration-dependent manner in a human endotoxin challenge model.

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