Shelf life (days): 1460.0
Formulation: A solid
Formal Name: 8-[[[5-chloro-2-(4-methyl-1-piperazinyl)-4-pyridinyl]carbonyl]amino]-1-(4-fluorophenyl)-4,5-dihydro-1H-benz[g]indazole-3-carboxamide
Purity: ≥98%
Formula Markup: C29H27ClFN7O2
Formula Weight: 560.0
CAS Number: 503555-55-3
Notes: PHA-408 is an inhibitor of IκB kinase β (IKKβ; IC50 = 0.04 µM).{67846} It is 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 for all). PHA-408 inhibits IL-1β-induced production of prostaglandin E2 (PGE2; Item No. 14010) in synovial fibroblasts isolated from patients with rheumatoid arthritis (IC50 = ~0.6 µM). In vivo, PHA-408 (50 mg/kg) reduces serum LPS-induced TNF-α production in rats. It inhibits joint swelling and bone destruction in a rat model of streptococcal cell wall-induced arthritis when administered at a dose of 10 mg/kg. PHA-408 (15 and 45 mg/kg) inhibits LPS- or cigarette smoke-induced bronchoalveolar lavage fluid (BALF) neutrophil influx and reduces BALF levels of IL-6, TNF-α, and IL-1β in rats.{67847}
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