
Description | GSK8612isahighlypotentandselectiveinhibitorforTBK1(Tank-bindingKinase-1)withpKdof8.0.Within10-foldaffinitywithrespecttoTBK1,nooff-targetsofGSK8612couldbeidentified. | ||
---|---|---|---|
Targets |
| ||
Invitro | Incellularassays,thissmallmoleculeinhibitstoll-likereceptor(TLR)3-inducedinterferonregulatoryfactor(IRF)3phosphorylationinRamoscellsandtypeIinterferon(IFN)secretioninprimaryhumanmononuclearcells.InTHP1cells,GSK8612isabletoinhibitsecretionofinterferonbeta(IFNβ)inresponsetodsDNAandcGAMP,thenaturalligandforSTING.GSK8612hasloweraffinityforphosphorylatedTBK1.GSK8612inhibitsrecombinantTBK1withanaveragepIC50of6.8inabiochemicalfunctionalassay.TheactualselectivityofGSK8612forTBK1inthecellswilldependontheactivationstateofTBK1[1]. | ||
Invivo | GSK8612ishighlyproteinboundinmouse,ratandhumanblood[1]. |
ebiomall.com






>
>
>
>
>
>
>
>
>
>
>
>

