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 | |||||
Quality Control & MSDS
- View current batch:
Chemical structure
Related Biological Data
Related Biological Data
Related Biological Data
