| Bioactivity | SGK1-IN-1 is a highly active and selective inhibitor of SGK-1, with an IC50 of 1 nM. | ||||||||||||
| Target | IC50: 1 nM (SGK-1). | ||||||||||||
| Invitro | 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]. | ||||||||||||
| Name | SGK1-IN-1 | ||||||||||||
| CAS | 1279829-87-6 | ||||||||||||
| Formula | C17H12ClFN6O2S | ||||||||||||
| Molar Mass | 418.83 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| 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. |