PKN3 inhibitor compound 16 is an inhibitor of serine/threonine protein kinase N3 (IC50 = 14 nM).1 It is selective for this kinase over a panel of 234 kinases but does inhibit serine/threonine protein kinase NLK, activin receptor type 1 (ACTR1), and receptor-interacting serine/threonine kinase 2 (RIPK2) at 1 ?M, as well as cyclin G-associated kinase (GAK; IC50 = 74 nM in a bioluminescence resonance energy transfer (BRET) assay).1,2 PKN3 inhibitor compound 16 inhibits viral replication in dengue virus-infected Huh7 cells (EC50 = 3.6 ?M) without inducing cell death with a 50% cytotoxic concentration (CC50) value of >10 ?M.3
References:
[1]. Asquith, C.R.M., Temme, L., East, M.P., et al.Identification of 4-anilinoquin(az)oline as a cell-active protein kinase novel 3 (PKN3) inhibitor chemotypeChemMedChem17(12)e202200161(2022).
[2]. Asquith, C.R.M., Laitinen, T., Bennett, J.M., et al.Design and analysis of the 4-anilinoquin(az)oline kinase inhibition profiles of GAK/SLK/STK10 using quantitative structure-activity relationshipsChemMedChem15(1)26-49(2020).
[3]. Saul, S., Pu, S.-Y., Zuercher, W.J., et al.Potent antiviral activity of novel multi-substituted 4-anilinoquin(az)olinesBioorg. Med. Chem. Lett.30(16)127284(2020).