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HPN-01 is a potent and selective IKK inhibitor, with pIC50 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[1].

IKK-α: 6.4 (pIC₅₀); IKK-β: 7.0 (pIC₅₀); IKK-ε: <4.8 (pIC₅₀)

[1] Christopher JA, et al. The discovery of 2-amino-3,5-diarylbenzamide inhibitors of IKK-alpha and IKK-beta kinases. Bioorg Med Chem Lett. 2007 Jul 15;17(14):3972-7. DOI:10.1016/j.bmcl.2007.04.088
[2] Ke Li, et al. Amino-aryl-benzamide compounds and methods of use thereof.WO2018204775A1.