Product namePH-797804, p38 alpha inhibitor
DescriptionNovel, potent, pyridinone-based, ATP-competitive p38α inhibitor
PH-797804 is a novel pyridinone-based ATP-competitive inhibitor of p38α. Potently inhibits p38α in cell-free assays (IC50 = 26 nM, Ki = 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.
Storage instructionsShipped at 4°C. Store at +4°C short term (1-2 weeks). Store at -20°C long term. It is important to note that this is air sensitive and impurities can occur as a result of air oxidation. Store In the Dark. Store under desiccating conditions.
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.
Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
This product has been referenced in:
- Schönrogge M et al. a-cyano-4-hydroxycinnamate impairs pancreatic cancer cells by stimulating the p38 signaling pathway. Cell Signal 47:101-108 (2018). Read more (PubMed: 29609037) »
- Selness SR et al. Discovery of PH-797804, a highly selective and potent inhibitor of p38 MAP kinase. Bioorg Med Chem Lett 21:4066-71 (2011). Read more (PubMed: 21641211) »
- Hope HR et al. Anti-inflammatory properties of a novel N-phenyl pyridinone inhibitor of p38 mitogen-activated protein kinase: preclinical-to-clinical translation. J Pharmacol Exp Ther 331:882-95 (2009). Read more (PubMed: 19720877) »
- Xing L et al. Structural bioinformatics-based prediction of exceptional selectivity of p38 MAP kinase inhibitor PH-797804. Biochemistry 48:6402-11 (2009). Read more (PubMed: 19496616) »