| Chemical Properties | Back Directory | [Boiling point ]
730.5±70.0 °C(Predicted) | [density ]
1.660±0.06 g/cm3(Predicted) | [solubility ]
DMSO: soluble | [form ]
A solid | [pka]
5.86±0.10(Predicted) |
| Hazard Information | Back Directory | [Description]
SGK1 inhibitor is an inhibitor of serum- and glucocorticoid-regulated kinase 1 (SGK1) and SGK2. It is selective for SGK1 and SGK2 over SGK3 in the presence of a high concentration of ATP. SGK1 inhibitor prevents phosphorylation of GSK3β in U2OS cells and decreases cell viability in BYL719-insensitive HCC1954 cells when used in combination with the PI3Kα inhibitor BYL719. SGK1 inhibitor reduces tumor growth in an HCC1954 mouse xenograft model when administered in combination with BYL719. | [Uses]
SGK1-IN-5 (Compound 1) is an inhibitor for serum and glucocorticoid regulated kinase SGK 1 with an IC50 of 3 nM. SGK1-IN-5 inhibits SGK-1 dependent phosphorylation of GSK3β in U2OS cells with an IC50 of 1.4 μM. SGK1-IN-5 can be used in research about osteoarthritis or rheumatism[1]. | [References]
[1] Nazare M, et al., N-[4-(1H-PYRAZOLO[3,4-b]PYRAZIN-6-YL)-PHENYL]-SULFONAMIDES AND THEIR USE AS PHARMACEUTICALS. US20130072493. |
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