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.

Research Areas >> Cancer

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.

Resveratrol | MRT67307 | BMS-345541 | MLN120B | ACHP (Hydrochloride) | TPCA-1 | IKK-16 | IMD 0354 | LY2409881 | SC-514 | BI 605906 | Bay 65-1942 (hydrochloride) | TBK1/IKKε-IN-2 | AZD3264 | PS-1145