For research use only. Not for therapeutic Use.
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].
| Catalog Number | I019988 |
| CAS Number | 1279829-87-6 |
| Synonyms | N-[4-(3-amino-2H-pyrazolo[3,4-b]pyrazin-6-yl)phenyl]-5-chloro-2-fluorobenzenesulfonamide |
| Molecular Formula | C17H12ClFN6O2S |
| Purity | ≥95% |
| InChI | InChI=1S/C17H12ClFN6O2S/c18-10-3-6-12(19)14(7-10)28(26,27)25-11-4-1-9(2-5-11)13-8-21-15-16(20)23-24-17(15)22-13/h1-8,25H,(H3,20,22,23,24) |
| InChIKey | DDKHTWASHUKHLD-UHFFFAOYSA-N |
| SMILES | C1=CC(=CC=C1C2=NC3=NNC(=C3N=C2)N)NS(=O)(=O)C4=C(C=CC(=C4)Cl)F |
| Reference | [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. |
