N-(6-Chloro-9H-b-carbolin-8-yl)nicotinamide Yellow solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. A cell-permeable b-carboline compound that displays anti-inflammatory properties. Acts as a potent, ATP-competitive, and reversible inhibitor of IKK (IC50 =88 nM) with selectivity over 14 other commonly studied kinases (IC50 > 100 µM), including NF-kB inducing kinase. Blocks cellular IkBa phosphorylation and NF-kB activation (EC50 = 5 µM in TNF-a-treated HeLa cells) in vitro and reduces TNF-a release in plasma of LPS-challenged mice in vivo (50 mg/ml p.o.). Purity: ≥98% by HPLC. Ref.: Catley, M.C., et al. 2006. Mol. Pharmacol. 70, 697. Wen, D., et al. 2006. J. Pharm. Exp. Ther. 317, 989. Castro, A.C., et al. 2003. Bioorg. Med. Chem. Lett. 13, 2419. Hideshima, T., et al. 2002. J. Biol. Chem. 277, 16639. |
