- Cat. No.
- A13309
GSK-650394
GSK 650394 is a glucocorticoid- and serum-regulated kinase 1 (SGK1) inhibitor which displays antiproliferative properties against the LNCaP prostate carcinoma cell line.
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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.
GSK 650394 is a glucocorticoid- and serum-regulated kinase 1 (SGK1) inhibitor which displays antiproliferative properties against the LNCaP prostate carcinoma cell line.
EMD638683 R-Form is the R-form of EMD638683. EMD638683 is a highly selective SGK1 inhibitor with IC50 of 3 μM.
EMD638683 S-Form is the S-form of EMD638683. EMD638683 is a highly selective SGK1 inhibitor with IC50 of 3 μM.
EMD638683 is a potent inhibitor of SGK1 with an IC50 value of 3 uM.
SGK1-IN-1 is a highly active and selective inhibitor of SGK-1, with an IC50 of 1 nM.
SI-113 is an inhibitor of SGK1, demonstrating an IC50 of 600 nM. This compound is known to induce autophagy, making it a valuable tool for studying cellular mechanisms related to SGK1 activity. It has potential applications in research areas such as cancer biology and neurodegenerative diseases, where modulation of autophagy may be beneficial.
SGK1-IN-4 is a selective inhibitor of Serum/Glucocorticoid-regulated Kinase 1 (SGK1), demonstrating oral bioactivity. This compound has potential applications in the study of osteoarthritis, targeting pathways involved in inflammation and cellular signaling. Its ability to modulate SGK1 activity makes it a valuable tool for investigating SGK1's role in various biological processes and disease states.
SGK1-IN-2 is a selective inhibitor of serum and glucocorticoid-regulated kinase 1 (SGK1), characterized by an IC50 value of 5 nM at an ATP concentration of 10 μM. This compound effectively regulates SGK1 activity, influencing various cellular processes such as cell survival, proliferation, and metabolism. SGK1-IN-2 is valuable for research applications focused on cancer biology, cardiovascular diseases, and metabolic disorders.
SGK1-IN-3 is a potent selective inhibitor of SGK1, exhibiting an IC50 of less than 1 μM. This compound demonstrates significant inhibitory activity, making it a valuable tool for investigating the role of SGK1 in various biological processes. Its application in research may provide insights into the mechanisms underlying osteoarthritis and contribute to the development of novel therapeutic strategies.
SGK1-IN-6 is a selective inhibitor of SGK1, demonstrating a high potency with an IC50 value of 0.39 μM. This compound effectively suppresses tumor growth in the PC3 xenograft model in BALB/c nude mice while exhibiting no significant toxicity. SGK1-IN-6 is ideal for research applications focused on cancer biology and the exploration of SGK1's role in tumorigenesis.
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SGK1-IN-5 is a potent inhibitor of serum and glucocorticoid-regulated kinase 1 (SGK1) with an IC50 of 3 nM. This compound effectively inhibits SGK1-dependent phosphorylation of glycogen synthase kinase 3 beta (GSK3β) in U2OS cells, demonstrating an IC50 of 1.4 μM. SGK1-IN-5 is valuable for research applications related to osteoarthritis and rheumatism, contributing to the understanding of pathways involved in inflammatory and degenerative joint diseases.
SGK1-IN-9 is an inhibitor of serum/glucocorticoid-regulated kinase 1 (SGK1). This compound exhibits potential anti-cancer activity by modulating cell survival pathways and influencing tumor cell proliferation. It is suitable for use in cancer research to investigate the role of SGK1 in various malignancies and explore therapeutic strategies targeting this kinase.
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SGK1-IN-7 is a selective inhibitor of SGK1, exhibiting a blood-brain barrier permeability with an IC50 of 0.72 μM. This compound effectively reduces the phosphorylation of TAU protein at the Ser396 and Ser214 sites and counters the toxicity induced by Okadaic acid. SGK1-IN-7 is a valuable tool for research into the mechanisms underlying Alzheimer's disease.
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SGK1-IN-8 is a potent inhibitor of SGK1 and GSK3β, exhibiting an IC50 of 0.11 μM against human SGK1 and 3.39 μM against human GSK3β. This compound effectively inhibits the catalytic activities of both SGK1 and GSK3β, leading to a reduction in the phosphorylation of the TAU protein at the Ser214 site. SGK1-IN-8 is utilized in research focused on Alzheimer's disease and related neurodegenerative disorders.
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