… kinase 2, TPCA-1 (2-[(aminocarbonyl) amino]-5-(4-fluorophenyl)-3-thiophenecarboxamide), occurs via reduction of proinflammatory cytokines and antigen-induced T …

…, JF Callahan, BJ Bolognese, YH Li, K Carlson…

Index: Podolin, Patricia L.; Callahan, James F.; Bolognese, Brian J.; Li, Yue H.; Carlson, Karey; Davis, T. Gregg; Mellor, Geoff W.; Evans, Christopher; Roshak, Amy K. Journal of Pharmacology and Experimental Therapeutics, 2005 , vol. 312, # 1 p. 373 - 381

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Citation Number: 183

Abstract

Abstract Demonstration that IκB kinase 2 (IKK-2) plays a pivotal role in the nuclear factor-κB- regulated production of proinflammatory molecules by stimuli such as tumor necrosis factor (TNF)-α and interleukin (IL)-1 suggests that inhibition of IKK-2 may be beneficial in the treatment of rheumatoid arthritis. In the present study, we demonstrate that a novel, potent (IC 50= 17.9 nM), and selective inhibitor of human IKK-2, 2-[(aminocarbonyl) amino]-5-(4- ...