BMS-582949

Description: BMS-582949 (also known as PS540446) is a potent and highly selective p38 mitogen-activated protein kinase (p38 MAPK) inhibitor with IC50 of 13nM. It is currently in phase II clinical trials for the treatment of rheumatoid arthritis. p38MAPK is an important element of inflammatory pathways in atherothrombosis and its inhibition may lead to reduced inflammation within atherosclerotic plaques. BMS-582949 inhibits both p38 kinase activity and activation of p38. BMS-582949 is found to inhibit p38 activation in cells, as measured by phosphorylation of p38. BMS-582949 treatment of cells in which p38 has been activated by LPS rapidly reversed p38 activation as shown by loss of phosphorylation of p38. BMS-582949 is therefore a dual action p38 kinase inhibitor, inhibiting both p38 kinase activity and p38 activation in cells.

References: J Med Chem. 2010 Sep 23; 53(18):6629-39; Arthritis Rheum. 2010, 62 Suppl 10:1513.

Related CAS#: 912806-16-7 (HCl); 948842-66-8 (BMS-751324, prodrug of BMS-582949)

Publications Citing Use of InvivoChem BMS-582949: Cells . 2020 Jun 16; 9(6):1472. doi: 10.3390/cells9061472.

PS540446; BMS-582949; BMS 582949; PS-540446; PS 540446; BMS582949; BMS582949 free base;

Chemical Name: 4-((5-(cyclopropylcarbamoyl)-2-methylphenyl)amino)-5-methyl-N-propylpyrrolo[2, 1-f][1, 2, 4]triazine-6-carboxamide

Exact Mass: 406.2117