SGK1-IN-1 is a highly active and selective inhibitor of SGK-1, with an IC50 of 1 nM.
SGK1-IN-1 (14n) shows an acceptable SGK isoform selectivity with a good activity on hSGK2 and a moderate activity on the hSGK3, with IC50s of 1, 41 nM at 10 μM and 50 μM ATP concentration, respectively. SGK1-IN-1 also displays cellular activity in a SGK1-dependent phosphorylation of GSK3β assay in U2OS cells with activities of 0.69 μM[2].
[1]. ARYL SULFONOHYDRAZIDES. WO 2013041119 A1. [2]. Halland N, et al. Discovery of N-[4-(1H-Pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides as Highly Active and Selective SGK1 Inhibitors. ACS Med Chem Lett. 2014 Oct 23;6(1):73-8.