SGK
Serum-glucocorticoid regulated kinase; Serum and glucocorticoid-regulated kinase
Serum- and glucocorticoid-inducible kinases (SGKs) form a novel family of serine/threonine kinases that are activated in response to a variety of extracellular stimuli. SGK family contains three isoforms: SGK1, SGK2, and SGK3. The mRNA encoding SGK1, the best-studied member of the SGK family, is rapidly induced in response to a variety of stimuli, including growth factors, steroid and peptide hormones, cytokines, changes in cell volume, and brain injury.
SGKs are related to Akt (also called PKB), a serine/threonine kinase that plays a crucial role in promoting cell survival. The SGK family members share similar structure, substrate specificity and function with AKT and signal downstream of the phosphatidylinositol 3-kinase (PI3K) signalling pathway. They regulate a range of fundamental cellular processes such as cell proliferation and survival, thereby playing an important role in cancer development. In addition, SGKs not only regulate cell proliferation and survival, but also play important roles in cancer development via an AKT-independent signalling pathway. The importance of SGKs in cancer development and the scarcity of potent and selective SGK inhibitors support the urgent need for discovery and development of small molecules inhibitors targeting SGK for PIK3CA mutant cancers, and especially those that are resistant to AKT inhibition.
SGK Isoform Specific Products
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SGK Related Products (37)
Related Products (37)
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SGK Isoform Comparison
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SGK1-IN-5
0 ImagesSGK1-IN-5 is a SGK1 inhibitor with an IC50 of 0.003 μM. SGK1-IN-5 can be used for the research of osteoarthritis, rheumatism.
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308-R
0 ImagesCat. No.: HY-151009CAS No.: 2376724-98-8308-R is a SGK3/SGK1/S6K1 inhibitor. 308-R exhibits an IC50 of 5 nM against human SGK3, an IC50 of 10 nM against human SGK1, and an IC50 of 1 nM against human S6K1. 308-R can be used in breast cancer research. It is also applicable to studies related to PROTAC synthesis, such as serving as the target protein ligand for PROTAC SGK3 degrader-2 (HY-176823).
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SGK1-IN-6
0 ImagesCat. No.: HY-170933CAS No.: 3046378-98-4SGK1-IN-6 is a selective SGK1 inhibitor with an IC50 of 0.39 μM, showing selectivity over SGK2/3. SGK1-IN-6 inhibits cancer cell migration and invasion, improves SGK1 protein thermal stability. SGK1-IN-6 decreases SGK1 protein levels in tumor tissues, suppresses tumor growth in mouse xenograft models. SGK1-IN-6 can be used for the research of prostate cancer.
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SGK1-IN-8
0 ImagesCat. No.: HY-182342CAS No.: 3109982-48-8SGK1-IN-8 (compound 55) is a SGK1 and GSK3β inhibitor, with an IC50 of 0.11 μM against human SGK1 and an IC50 of 3.39 μM against human GSK3β. SGK1-IN-8 inhibits the catalytic activities of SGK1 and GSK3β, and reduces the phosphorylation level of TAU protein at the Ser214 site. SGK1-IN-8 is available for the research of Alzheimer's disease.
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SGK1-IN-10
0 ImagesCat. No.: HY-184333SGK1-IN-10 is an ATP-competitive SGK1 inhibitor with an IC50 of 2.53 μM against human SGK1, and it exhibits blood-brain barrier permeability. SGK1-IN-10 downregulates the phosphorylation levels of MDM2 and GSK-3β, induces apoptosis and inhibits cell migration. SGK1-IN-10 can be used in the research of prostate cancer.
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PROTAC SGK3 degrader-2
0 ImagesCat. No.: HY-176823CAS No.: 2381196-78-5PROTAC SGK3 degrader-2 is the cis epimer of PROTAC SGK3 degrader-1 (SGK3-PROTAC1) (HY-125878). PROTAC SGK3 degrader-2 exhibits inhibitory activity against SGK3, SGK1 and S6K1, with IC50 values of 0.6 μM, 1.4 μM and 1.7 μM, respectively, but fails to degrade SGK3. PROTAC SGK3 degrader-2 can serve as a control compound to investigate the specific effects of SGK3 degradation mediated by SGK3-PROTAC1.
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EMD638683 (Standard)
0 ImagesEMD638683 (Standard) is the analytical standard of EMD638683. This product is intended for research and analytical applications. EMD638683 is an orally effective SGK1 inhibitor with an IC50 of 3 μM. EMD638683 exhibits strong inhibition against SGK1, moderate inhibition against SGK2 and SGK3, and shows excellent selectivity for other AGC kinase family members. EMD638683 has antihypertensive activity by inhibiting SGK1, and independently of the blood pressure-lowering effect, it effectively prevents heart inflammation and fibrosis caused by hypertension by inhibiting the cardiac NLRP3 inflammation body/ IL-1β axis. EMD638683 promotes apoptosis of colon cancer cells and sensitizes radiotherapy. EMD638683 (S-Form) can be used in research related to hypertension, hypertensive heart damage, and colon cancer.
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