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Description

A cell-permeable, potent, selective, and allosteric site-binding inhibitor of IKK-2 (IC50 ~300 nM) that displays anti-inflammatory properties. Exhibits ~10-fold greater selectivity for IKK-2 over IKK-1 (IC50 ~4.0 µ,M) and does not inhibit IKKepsilon and a panel of more than 15 unrelated protein kinases even at concentrations as high as 100 µ,M. Inhibits cellular IkappaBalpha phosphorylation (IC50 = 4 µ,M in THP-1 cells) and LPS-induced cytokine production both in vitro (IC50 = 1-5 µ,M in THP-1 cells) and in vivo (IC50 = 10 mg/kg in mice). Effectively blocks inflammation and joint destruction in a murine arthritis model., A cell-permeable quinoxaline compound that displays anti-inflammatory properties. Acts as a potent, selective, and allosteric site-binding inhibitor of IKK-2 (IC50 = ~ 300 nM). Exhibits ~10-fold greater selectivity over IKK-1 (IC50 = ~ 4 µ,M) and no activity towards IKKepsilon and a panel of more than 15 unrelated protein kinases even at concentrations as high as 100 µ,M. Inhibits cellular IkappaBalpha phosphorylation (IC50 = 4 µ,M in THP-1 cells) and LPS-induced cytokine production both in vitro (IC50 = 1-5 µ,M in THP-1 cells) and in vivo (IC50 = 10 mg/kg in mice). Effectively blocks inflammation and joint destruction in a murine arthritis model.