PHA-408
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503555-55-3
≥98%
A solid
C29H27ClFN7O2
560
8-[[[5-chloro-2-(4-methyl-1-piperazinyl)-4-pyridinyl]carbonyl]amino]-1-(4-fluorophenyl)-4,5-dihydro-1h-benz[g]indazole-3-carboxamide, pha-767408
An IKKβ inhibitor (IC50 = 0.04 µM); selective for IKKβ over IKKα, Pim-1, Pim-2, Tie2, TrkA, and p70S6K (IC50s = 0.6-28.4 µM), as well as a panel of 26 kinases (IC50s = >30 µM); inhibits IL-1β-induced PGE2 production in synovial fibroblasts isolated from patients with rheumatoid arthritis (IC50 = ~0.6 µM); reduces serum LPS-induced TNF-α production in rats at 50 mg/kg; inhibits joint swelling and bone destruction in a rat model of streptococcal cell wall-induced arthritis at 10 mg/kg; inhibits LPS- or cigarette smoke-induced BALF neutrophil influx and reduces BALF levels of IL-6, TNF-α, and IL-1β in rats at 15 and 45 mg/kg