PH-797804 is a novel pyridinone-based ATP-competitive inhibitor of p38α. Potently inhibits p38α in cell-free assays (IC₅₀ = 26 nM, K_i = 5.8 nM). Displays 4-fold selectivity versus p38β. Inactive against JNK2. Inhibits LPS-induced production of TNFα (IC₅₀ = 5.9 nM) and p38 kinase activity (IC₅₀ = 1.1 nM) in U937 cells. No effect on the JNK or ERK pathways at concentrations up to 1 μM in U937 cells.  IC₅₀ is > 200 μM versus CDK2, ERK2, IKK1, IKK2, IKKi, MAPKAP2, MAPKAP3, MNK, PRAK, RSK2, and TBK1; > 100 μM versus MKK7 and MSK. Inhibits acute inflammatory responses in a number of preclinical animal models.

DMSO 96 mg/mL (201.13 mM)

Ethanol 7 mg/mL (14.66 mM)

Insoluble in water

Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.

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Synthetic

• Cell Biology
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