Selective, ATP-competitive p38 inhibitor (IC50 = 9 nM for p38alpha in vitro). Displays approximately 10-fold selectivity for p38alpha over p38beta and 2000-fold selectivity for p38alpha over 20 other kinases. Reduces p38alpha phosphorylation in multiple myeloma cells in vitro and in vivo, activity results in decreased tumor burden and angiogenesis in murine models of multiple myeloma. Also enhances bortezomib-induced cytotoxicity against multiple myeloma cells.
Target-Kategorie:
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