4-(2′-Aminoethyl)amino-1,8-dimethylimidazo[1,2-a]quinoxaline Off-white solid. PROTECT FROM LIGHT. HYGROSCOPIC. PACKAGED UNDER INERT GAS. 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 µM) and no activity towards IKKe and a panel of more than 15 unrelated protein kinases even at concentrations as high as 100 µM. Inhibits cellular IkBa phosphorylation (IC50 = 4 µM in THP-1 cells) and LPS-induced cytokine production both in vitro (IC50 = 1-5 µM in THP-1 cells) and in vivo (IC50 = 10 mg/kg in mice). Effectively blocks inflammation and joint destruction in a murine arthritis model. Purity: ≥96% by HPLC. Ref.: Townsend, R.M., et al. 2004. Transplantation 77, 1090. MacMaster, J.F., et al. 2003. Inflamm. Res. 52, 508. McIntyre, K.W., et al. 2003. Arthritis Rheum. 48, 2652. Burke, J. R., et al. 2003. J. Biol. Chem. 278, 1450. |
