HPN-01 is a potent and selective IKK inhibitor, with pIC 50 values of 6.4, 7.0 and <4.8 for IKK-α , IKK-β and IKK-ε, respectively. HPN-01 displays greater 50-fold selectivity over a panel of more than 50 other kinases, including ALK5 , CDK-2, EGFR , ErbB2, GSK3β, PLK1 , Src , and VEGFR-2
In Vitro
HPN-01 effectively suppress LPS-stimulated secretion of TNF-α, IL-1β, and IL-6 from human PBMCs (pIC 50 =6.1, 6.4, and 5.7, respectively). HPN-01 also inhibits TNF-α-induced NF-κB nuclear translocation in human lung fibroblast cells (pIC 50 =5.7). HPN-01 inhibits the expression of SREBP-1and SREBP-2 in cultured primary human hepatocytes with IC 50 s of 1.71 μΜ and 3.43 μΜ, respectively. HPN-01 is being development for the treatment of nonalcoholic fatty liver disease (NAFLD). MCE has not independently confirmed the accuracy of these methods. They are for reference only.