Product Size
5 mg
25 mg
Custom Size
Product Overview
Description
Novel, Potent, pyridinone-based, ATP-competitive p38α inhibitor.
Biological Description
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.
Solubility Overview
DMSO 96 mg/mL (201.13 mM); Ethanol 7 mg/mL (14.66 mM); insoluble in water.
Chemical Properties
Chemical Name
3-[3-bromo-4-[(2,4-difluorophenyl)methoxy]-6-methyl-2-oxopyridin-1-yl]-N,4-dimethylbenzamide
Molecular Weight (Da)
477.30
Molecular Formula
C22H19BrF2N2O3
SMILES
CC1=C(C=C(C=C1)C(=O)NC)N2C(=CC(=C(C2=O)Br)OCC3=C(C=C(C=C3)F)F)C
Storage & Handling
Storage Instructions
Shipped 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.
Handling
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.
