Talmapimod

Talmapimod (SCIO-469) is an orally active and selective inhibitor of p38α MAPK with an IC₅₀ of 9 nM. Talmapimod inhibits the secretion of inflammatory factors (such as TNFα, IL-1β, IL-6, and VEGF) by suppressing the p38α MAPK pathway, and it also inhibits angiogenesis and osteoclast activation. Talmapimod inhibits the growth of multiple myeloma cells and induces apoptosis. Talmapimod can be used to study various hematological malignancies (such as multiple myeloma, myelodysplastic syndrome)^[1][2][3][4]. IC50 & Target:IC50: 9 nM (p38)^[1]. In Vitro:Talmapimod (SCIO-469) (100-200 nM; 1 hour) inhibits phosphorylation of p38 MAPK in MM cells^[1].
Talmapimod inhibits LPS-induced TNF-a production in human whole blood^[2].
Talmapimod decreases constitutive p38alpha MAPK phosphorylation of both 5T2MM and 5T33MM cells^[3]. In Vivo:Targeting p38α MAPK with Talmapimod (SCIO-469) decreases myeloma burden in addition to preventing the development of myeloma bone disease^[2].
Talmapimod inhibits multiple myeloma growth and prevents bone disease in the 5T2MM and 5T33MM models^[3].
Talmapimod (10-90 mg/kg; p.o.; twice daily orally for 14 days) dose-dependently reduced tumor growth and also dose-dependently reduced weight of the palpable tumors at termination^[4].