SGC-GAK-1 is an inhibitor of cyclin G-associated kinase (GAK; Ki = 3.1 nM).1 It is greater than 50-fold selective for GAK over a panel of 400 kinases at 1 ?M but does bind to RIPK2 in a bioluminescence resonance energy transfer (BRET) engagement assay (IC50 = 360 nM). SCG-GAK-1 reduces the viability of LNCaP and 22Rv1 prostate cancer cells with IC50 values of 0.65 and 0.17 ?M, respectively. It also inhibits dengue virus infection in Huh7 cells (EC50 = 0.08 ?M).2
1.Asquith, C.R.M., Berger, B.-T., Wan, J., et al.SGC-GAK-1: A chemical probe for cyclin G associated kinase (GAK)J. Med. Chem.62(5)2830-2836(2019) 2.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)