Chemical Name:6-Chloro-5-[[(2R,5S)-4-[(4-fluorophenyl)methyl]-2,5-dimethyl-1-piperazinyl]carbonyl]-N,N,1-trimethyl-α-oxo-1H-Indole-3-acetamide hydrochloride
Biological Activity Selective, ATP-competitive p38 inhibitor (IC50 = 9 nM for p38αin vitro). Displays approximately 10-fold selectivity for p38α over p38β and 2000-fold selectivity for p38α over 20 other kinases. Reduces p38α 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.
Soluble to 10 mM in water and to 100 mM in DMSO
Desiccate at +4°C
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