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PH-797804 is an ATP-competitive, readily reversible inhibitor of the alpha isoform of human p38 MAP kinase, exhibiting a K(i) = 5.8 nM. PH-797804 blocks inflammation-induced production of cytokines and proinflammatory mediators in human monocyte and synovial fibroblast cell systems, such as prostaglandin E(2), at concentrations that parallel inhibition of cell-associated p38 MAP kinase. PH-797804 effectively inhibits acute inflammatory responses induced by systemically administered endotoxin in both rat and cynomolgus monkeys after oral dosing. PH-797804 exhibited exceptionally high specificity against MAP kinases and the related kinases. No cross-reactivity was observed in large panels of kinase screens (selectivity ratio of >500-fold). In cellular assays, PH-797804 demonstrated superior potency and selectivity consistent with the biochemical measurements. Finally, PH-797804 reduced tumor necrosis factor-alpha and interleukin-6 production in clinical studies after endotoxin administration in a dose-dependent manner, paralleling inhibition of the target enzyme.
| Molecular Weight | 477.3 |
| Formula | C22H19BrF2N2O3 |
| CAS Number | 586379-66-0 |
| Solubility (25°C) | DMSO 90 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related p38 MAPK Products |
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| SSK1
SSK1 is a senescence-specific killing compound and is a precursor for β-galactosidase, which can reduce the inflammatory response. SSK1 can activate the phosphorylation of p38 MAPK and MKK3/MKK6 in senescent cells, promote mitochondrial DNA damage and selectively killed senescent cells. |
| p38 MAP Kinase Inhibitor III
p38 MAP Kinase Inhibitor III is a p38 MAPK inhibitor with an IC50 of 0.9 μM. p38 MAP Kinase Inhibitor III also inhibits IL-1β and TNF-α release with IC50 values of 0.37 μM and 0.044 μM, respectively. |
| (R)-STU104
(R)-STU104 is a potent and orally active TAK1-MKK3 interaction inhibitor with IC50s of 0.58 μM and 4.0 μM for TNF-α and MKK3 phosphorylation. |
| SB 706504
SB 706504 is a potent p38 MAPK inhibitor that inhibits Lipopolysaccharides-stimulated inflammatory gene expression in macrophages in chronic obstructive pulmonary disease (COPD). |
| RWJ-67657
RWJ-67657 (JNJ 3026582) is an orally active and selective p38α and p38β MAPK inhibitor with IC50s of 1 and 11 μM, respectively. |
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