Background:

Target: IKK2

IC50: N/A

AZD3264 is a novel and small molecule IKK2 inhibitor.

IKK2 serves as a protein subunit of IκB kinase, which is a component of the cytokine-activated intracellular signaling pathway involved in triggering immune responses. IKK's activity induces the activation of a transcription factor NF-κB. Activated IKK2 phosphorylates IκB (IκBα), which binds NF-κB to inhibit its function. Phosphorylated IκB is degraded by the ubiquitination pathway, freeing NF-κB, and allowing its entry into the cell nucleus where it activates target genes involved in inflammation and other immune responses. Suppression of IKK2 has been identified as a potential therapeutic option to treat cancer and inflammatory diseases, including asthma, chronic pulmonary obstructive disorder (COPD) and rheumatoid arthritis [1].

In vitro: AZD3264, by inhibiting IKK2, was currently in preclinical development for the potential treatment of inflammatory diseases such as asthma, chronic pulmonary obstructive disorder (COPD) and rheumatoid arthritis [2].

In vivo: N/A

参考文献:
1.  Llona-Minguez S, Baiget J, Mackay SP. Small-molecule inhibitors of IkappaB kinase (IKK) and IKK-related kinases. Pharm Pat Anal. 2013;2(4):481-98.
2.  Murugan A, et al. Org. Process Res. Dev. 2014, 18, 646-651.