309913-83-5

Talmapimod is a p38 mitogen-activated protein (MAP) kinase inhibitor. Talmapimod reduced human myeloma cell growth in vivo both at early and advanced phases of the disease in mouse xenograft models. T almapimod that blocks tumor necrosis factor-α, interleukin-1β, and cyclooxygenase-2 synthesis in patients with active rheumatoid arthritis (RA)

ChEBI: An indolecarboxamide obtained by formal condensation of the carboxy group of 6-chloro-3-[(dimethylamino)(oxo)acetyl]-1-methylindole-5-carboxylic acid with the secondary amino group of (2S,5R)-1-[(4-fluorophenyl)methyl]-2, -dimethylpiperazine. It is a potent inhibitor of MAPK and exhibits anti-cancer properties.

SCIO-469 (Talmapimod) is an orally activepotent and selective mitogen-activated protein kinase (MAPK) p38alpha (p38αMAPK14) inhibitor (IC50 = 9 nM; 10-fold over p38β>2000-fold over 20 other kinases) with no significant affinity toward a panel of 70 enzymes and receptors. SCIO-469 inhibits multiple myeloma (MM) growth in mice in vivo (150 or 450 mg/kg powder diet; 5T2MM and 5T33MM) and augments proteasome inhibitor in a murine plasmacytoma model of MM (0.2 mg bortezomib/kg i.v. twice weekly with 30 mg SCIO-469/kg b.i.d. p.o.; RPMI8226).

p38α: 9 nM (IC₅₀); p38β: 90 nM (IC₅₀)