| Bioactivity | Pamapimod (Ro4402257) is a potent, selective and orally active p38 MAPK inhibitor with IC50s of 14 nM and 480 nM and Kis of 1.3 nM and 120 nM for p38α and p38β, respectively. Pamapimod has no activity against p38δ or p38γ isoforms. Pamapimod has the potential for rheumatoid arthritis and other autoimmune diseases treatment[1]. | ||||||||||||
| Invitro | Pamapimod binds to JNK kinases with Ki values of 190 nM, 16 nM and 19 nM for Jnk1, Jnk2 and Jnk3, respectively[1]. After lipopolysaccharide (LPS) stimulation of the human myelomonocytic cell line (THP-1), secretion of TNF-α is inhibited by Pamapimod, with an EC50 of 25 nM. Pamapimod suppresses TNF-α and IL-1β production in whole blood, with EC50 values of 0.40 and 0.10 μM, respectively[1]. | ||||||||||||
| In Vivo | Pamapimod (0-150 mg/kg; oral gavage; once daily; DBA/1J female mice) treatment reduces inflammation and bone loss in murine collagen-induced arthritis[1]. Animal Model: | ||||||||||||
| Name | Pamapimod | ||||||||||||
| CAS | 449811-01-2 | ||||||||||||
| Formula | C19H20F2N4O4 | ||||||||||||
| Molar Mass | 406.38 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Hill, R. J. et al. Pamapimod, a novel p38 mitogen-activated protein kinase inhibitor: preclinical analysis of efficacy and selectivity. The Journal of pharmacology and experimental therapeutics 327, 610-619, doi:10.1124/jpet.108.139006 (2008). |
Pamapimod
CAS: 449811-01-2 F: C19H20F2N4O4 W: 406.38
Pamapimod (Ro4402257) is a potent, selective and orally active p38 MAPK inhibitor with IC50s of 14 nM and 480 nM and Kis
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