ACHP hydrochloride is a potent and specific inhibitor for IKK-β (IKK2) with IC50 of 8.5 nM, moderately inhibits IKK-α with IC50 of 250 nM.
ACHP exhibits good selectivity over other kinases, such as IKK3, Syk and MKK4 (IC50>20 uM).
ACHP inhibits TNFα-induced RANTES production in A549 cells with IC50 of 40 nM, inhibits NF-κB-dependent reporter gene activation in TNFα -activated HEK293 cells and PMA/calcium ionophore-activated Jurkat T cells.
ACHP demonstrates in vivo anti-inflammatory assays (1mg/kg, po) in arachidonic acid-induced ear edema model in mice.
ACHP also inhibits TNF-α-induced HIV-1 replication in latently infected cells with EC50 of 0.56 uM.
