Information Pamapimod (R-1503, Ro4402257) is a novel, selective inhibitor ofp38 mitogen-activated protein kinase. It inhibits p38α and p38β enzymatic activity with IC50 values of 0.014±0.002 and 0.48± 0.04 microM, respectively with no activity against p38delta or p38gamma isoforms. Targets p38α (Cell-free assay); p38β (Cell-free assay) 0.014 μM; 0.48 μM In vitro Pamapimod inhibited p38, but inhibition of JNK was not detected. Pamapimod also inhibited lipopolysaccharide (LPS)-stimulated tumor necrosis factor (TNF) α production by monocytes, interleukin (IL)-1β production in human whole blood, and spontaneous TNFα production by synovial explants from RA patients. In vivo In murine collagen-induced arthritis, pamapimod reduced clinical signs of inflammation and bone loss at 50 mg/kg or greater. In a rat model of hyperalgesia, pamapimod increased tolerance to pressure in a dose-dependent manner, suggesting an important role of p38 in pain associated with inflammation. Pamapimod suppresses spontaneous production of TNFα by synovial explants from RA patients. LPS- and TNFα-stimulated production of TNFα and IL-6 in rodents also was inhibited by pamapimod. Cell Research(from reference) Cell lines：Human Monocytic Cell Line, THP-1 Concentrations：15 μM Incubation Time：150 min
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Pamapimod
CAS number：449811-01-2 molecular formula：C19H20F2N4O4
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| Chinese alias | - | ||
| English alias | AC-33182 | DEGARELIX [USAN] | DTXSID6040244 | FLW | PAMAPIMOD [INN] | 6-(2,4-Difluorophenoxy)-2-{[3-Hydroxy-1-(2-Hydroxyethyl)propyl]amino}-8-Methylpyrido[2,3-D]pyrimidin-7(8h)-One | BCP17491 | 6-(2,4-Difluorophenoxy)-2-((3-hydroxy-1-(2-hydroxyethyl)propy | ||
| CAS number | 449811-01-2 | molecular formula | C19H20F2N4O4 |
| molecular weight | 406.38 g/mol | Exact mass | - |
| PSA | 108.000 Ų | logp | 1.298 |
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