Nuclear Factor-kappa B (NF-κB) is a transcription factor family that regulates a large number of genes that are involved in important physiological processes, including survival, inflammation, and immune responses[3]. SC75741 is a potent inhibitor of NF-κB with an EC50 of 200 nM[2]. SC75741 also acts as a broad and efficient blocker of IV replication in non-toxic concentrations. The underlying molecular mechanism of SC75741 action involves impaired DNA binding of the NF-κB subunit p65, resulting in reduced expression of cytokines, chemokines, and pro-apoptotic factors, subsequent inhibition of caspase activation and block of caspase-mediated nuclear export of viralribonucleoproteins. SC75741 reduces viral replication and H5N1-induced IL-6 and IP-10 expression in the lung of infected mice. Besides its virustatic effect the drug suppresses virus-induced overproduction of cytokines and chemokines, suggesting that it might prevent hypercytokinemia that is discussed to be an important pathogenicity determinant of highly pathogenic IV. Importantly the drug exhibits a high barrier for development of resistant virus variants. Thus, SC75741-derived drugs may serve as broadly non-toxic anti-influenza agents[1].
SC75741 细胞研究
细胞系
浓度
检测类型
检测时间
活动说明
数据源
A549 cells
Function assay
5 h
Inhibition of NF-kappaB in A549 cells after 5 hrs by reporter gene assay, EC50=0.2 μM
17869512
PBMC
Proliferation assay
Antiproliferative activity against human PBMC, IC50=2.2 μM
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