tcsc0039319 TBK1 / IKKε-IN-1

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.

IC50 & Target: IC50: <100 nM (TBK1), <100 nM (IKKε)^[1]

In Vitro: 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].