433958-69-1Relevant academic research and scientific papers
Discovery of novel and selective IKK-β serine-threonine protein kinase inhibitors. Part 1
Murata, Toshiki,Shimada, Mitsuyuki,Sakakibara, Sachiko,Yoshino, Takashi,Kadono, Hiroshi,Masuda, Tsutomu,Shimazaki, Makoto,Shintani, Takuya,Fuchikami, Kinji,Sakai, Katsuya,Inbe, Hisayo,Takeshita, Keisuke,Niki, Toshiro,Umeda, Masaomi,Bacon, Kevin B.,Ziegelbauer, Karl B.,Lowinger, Timothy B.
, p. 913 - 918 (2007/10/03)
IκB kinase β (IKK-β) is a serine-threonine protein kinase critically involved in the activation of the transcription factor Nuclear Factor kappa B (NF-κB) in response to various inflammatory stimuli. We have identified a small molecule inhibitor of IKK-β. Optimization of the lead compound resulted in improvements in both in vitro and in vivo potency, and provided IKK-β inhibitors exhibiting potent activity in an acute cytokine release model (LPS-induced TNFα).
