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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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| BIRB796
BIRB 796 (Doramapimod) is a protein kinase inhibitor of p38 MAPK with Kd of 100pM. |
| Selonsertib
GS-4997 is a highly selective and potent once-daily oral ASK1 inhibitor with potential anti-inflammatory, antineoplastic and anti-fibrotic activities. |
| Adezmapimod
Adezmapimod (SB203580) is a P38 MAPK inhibitor with an IC50 of 0.3-0.5 μM, which is 10 times less selective than SAPK3(106T) and SAPK4(106T), and inhibits PKB phosphorylation with an IC50 of 3-5 μM. |
| SB 202190
SB 202190 is a highly selective, potent and cell permeable inhibitor of p38 MAP kinase with IC50 values of 50 and 100 nM inhibiting p38α and p38β, respectively. |
| VX-702
VX-702 is a highly selective inhibitor of p38 MAPKα with IC50 of 4-20 nM. |
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