PH-797804
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.
- 1. Maruyama, Hidekazu, et al. "Endothelin-1 alters BMP signaling to promote proliferation of pulmonary artery smooth muscle cells." Can J Physiol Pharmacol. 2022 Oct 1;100(10):1018-1027. PMID: 36037530
- 2.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
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 477.3 |
| Cas No. | 586379-66-0 |
| Formula | C22H19BrF2N2O3 |
| Synonyms | PH797804;PH 797804 |
| Solubility | ≥23.85 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH |
| Chemical Name | 3-[3-bromo-4-[(2,4-difluorophenyl)methoxy]-6-methyl-2-oxopyridin-1-yl]-N,4-dimethylbenzamide |
| SDF | Download SDF |
| 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 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| 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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