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Potent and selective p38α/β inhibitor (IC50 values are 26 and 102 nM, respectively). Exhibits >100-fold selectivity for p38α/β over 71 other kinases, enzymes and GPCRs, including p38γ, p38δ, JNK and ERK2. Inhibits LPS-induced TNFα production in U937 monocytes in vitro. Suppresses acute and chronic inflammatory responses in rat models of arthritis. Orally active.
PH 797804 is the (-)-atropisomer, which is 100-fold more potent than its (+)-atropisomer.
Sold for research purposes under agreement from Pfizer Inc
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 477.3. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.5 mM||4.19 mL||20.95 mL||41.9 mL|
|2.5 mM||0.84 mL||4.19 mL||8.38 mL|
|5 mM||0.42 mL||2.1 mL||4.19 mL|
|25 mM||0.08 mL||0.42 mL||0.84 mL|
References are publications that support the biological activity of the product.
Hope et al (2009) 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 PMID: 19720877
Selness et al (2011) Discovery of PH-797804, a highly selective and potent inhibitor of p38 MAP kinase. Bioorg.Med.Chem.Lett. 21 4066 PMID: 21641211
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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MAPK Signaling Scientific Review
MAP kinase signaling is integral to the regulation of numerous cellular processes such as proliferation and differentiation, and as a result is an important focus of cancer and immunology research. Updated for 2016, this review discusses the regulation of the MAPK pathway and properties of MAPK cascades. Compounds available from Tocris are listed.