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SGK inhibitors act on serum- and glucocorticoid-regulated kinases (SGKs), a family of three kinases. The founding member, SGK1, was cloned in 1993 as a gene whose transcription rises quickly after glucocorticoid or serum exposure. SGK1, SGK2 and SGK3 are close relatives of protein kinase B (Akt) and become active downstream of phosphoinositide 3-kinase (PI3K) signaling. In kidney epithelia, SGK1 phosphorylates the ubiquitin ligase Nedd4-2 and keeps more epithelial sodium channels (ENaC) at the cell surface. SGK1 is also studied in hypertension, insulin signaling and tumor cell survival. GSK-650394, EMD638683 and SI-113 inhibit SGK1, and GSK-650394 also acts on SGK2. PROTAC SGK3 degrader-1 removes SGK3 through a proteolysis-targeting chimera (PROTAC) design.
Synonyms: SGK3-PROTAC1
SGK3-PROTAC1 is a PROTAC molecule designed to selectively degrade SGK3 by linking the 308-R SGK inhibitor to the VHL-binding ligand VH032. Through recruitment of the VHL E3 ligase, SGK3-PROTAC1 induces proteasomal degradation of SGK3, providing a targeted approach for studying SGK3 function in cellular signaling and disease.
PROTAC SGK3 degrader-2 is a selective PROTAC designed to engage SGK3 while targeting its degradation pathways. Unlike its trans counterpart, this compound possesses a cis hydroxyl group in the VH032 moiety, preventing its interaction with the VHL E3 ligase. It exhibits inhibitory effects on SGK3, SGK1, and S6K1, with IC50 values of 0.6 μM, 1.4 μM, and 1.7 μM, respectively, but does not induce SGK3 degradation. PROTAC SGK3 degrader-2 serves as an essential control reagent in research examining the specific biological effects of SGK3-PROTAC1-mediated degradation.
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