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PH-797804P38 MAP kinase inhibitor, potent and selective

PH-797804

Catalog No. A8308
Size Price Stock Qty
10mM (in 1mL DMSO) $224.00 In stock
Evaluation Sample $28.00 In stock
5mg $120.00 In stock
25mg $380.00 In stock

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Sample solution is provided at 25 µL, 10mM.

Product Citations

1. Zheng, Lufeng, et al. "The 3′ UTR of the pseudogene CYP4Z2P promotes tumor angiogenesis in breast cancer by acting as a ceRNA for CYP4Z1." Breast cancer research and treatment (2015): 1-14. PMID:25701119

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Chemical structure

PH-797804

Related Biological Data

PH-797804

Related Biological Data

PH-797804

Related Biological Data

PH-797804

Biological Activity

Description PH-797804 is a novel pyridinone inhibitor of p38α with IC50 of 26 nM; 4-fold more selective versus p38β.
Targets p38α          
IC50 26 nM          

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Chemical Properties

Cas No. 586379-66-0 SDF Download SDF
Synonyms PH797804;PH 797804
Chemical Name 3-[3-bromo-4-[(2,4-difluorophenyl)methoxy]-6-methyl-2-oxopyridin-1-yl]-N,4-dimethylbenzamide
Canonical 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
Formula C22H19BrF2N2O3 M.Wt 477.3
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

PH-797804 is a novel, potent, ATP-competitive and reversible inhibitor of human p38 MAP kinase. It specifically inhibits p38α with IC50 value of 26 nM and K(i) value of 5.8 nM.

PH-797804 inhibits LPS induced TNF-α and IL-1β production in monocytes with a concentration-dependently manner. PH-797804 blocks RANKL and M-CSF induced osteoclast formation in primary rat bone marrow cells.

Orally administered PH-797804 suppresses TNF-α level in a dose-dependent manner in LPS induced Lewis rats and also in cynomolgus monkeys. Additionally, PH-797804 has been shown to inhibit chronic inflammation in arthritis models induced by mouse collagen-induced or rat streptococcal cell wall (SCW) extract.

References:
[1] Hope HR1, Anderson GD, Burnette BL, Compton RP, Devraj RV, Hirsch JL, Keith RH, Li X, Mbalaviele G, Messing DM, Saabye MJ,Schindler JF, Selness SR, Stillwell LI, Webb EG, Zhang J, Monahan JB. Anti-inflammatory properties of a novel N-phenyl pyridinone inhibitor of p38 mitogen-activated protein kinase: preclinical-to-clinical translation. J Pharmacol Exp Ther. 2009 Dec;331(3):882-95.