Description
A p38 MAPK inhibitor (IC50 = 9 nM for p38α); 10-fold selective for p38α over p38β MAPK and 2,000-fold selective over a panel of 20 additional kinases; inhibits secretion of IL-6 from multiple myeloma patient-derived BMSCs in a concentration-dependent manner; increases PS-341-induced growth inhibition, DNA fragmentation, and caspase-8 and PARP cleavage in MM.1S cells at 100 and 200 nM; reduces microvessel density and tumor load and increases survival in a 5T33MM murine myeloma model at 150 and 450 mg/kg