TBK1/IKKε-IN-1 是一种双重 TBK1 和 IKKε 抑制剂,IC50s 值 <100 nM。详细信息请参考专利文献 US20160376283 A1 中 Example 60 中的化合物 274。
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TBK1/IKKε-IN-1 is a dual TBK1 and IKKε inhibitor extracted from patent US20160376283 A1, Compound 274 in Example 60, has IC50s of <100 nM. TBK1|100 nM (IC50)|IKKε|100 nM (IC50)
IKKε and TBK1 are serine/threonine kinases which are highly homologous to one another and other IkB kinases (IKK-α and IKK-β). The two kinases play an integral role in the innate immune system. Double-stranded RNA viruses are recognised by the Toll-like receptors 3 and 4 and the RNA helicases RIG-I and MDA-5 and result in activation of the TRIF-TBK1/IKKε-IRF3 signalling cascade, which results in a type I interferon response[1].
[1]. Brian A. Sherer, et al. Tbk/ikk inhibitor compounds and uses thereof. US 20160376283 A1.
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