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 Produits associés (36)
Produits associés (36)
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SGK Isoform Comparison
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GSK 650394
0 ImagesGSK 650394 is a novel SGK inhibitor with IC50 of 62 nM and 103 nM for SGK1 and SGK2 in the SPA assay respectively. GSK 650394 also inhibits influenza virus replication.
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EMD638683
0 ImagesEMD638683 is an orally active 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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HaloPROTAC-E
0 ImagesHaloPROTAC-E is a potent Halo PROTAC degrader that reversibly induces degradation of two Halo-tagged endoplasmic reticulum-localized proteins, SGK3 and VPS34, with a DC50 of 3-10 nM. HaloPROTAC-E significantly and selectively induces degradation of endogenous VPS34 complexes (VPS34, VPS15, Beclin1, and ATG14) labeled with Halo and inhibits autophagy.
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SGK1-IN-1
0 ImagesSGK1-IN-1 is a highly active and selective inhibitor of SGK-1, with an IC50 of 1 nM.
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PROTAC SGK3 degrader-1
0 ImagesSynonyms: SGK3-PROTAC1PROTAC SGK3 degrader-1 (SGK3-PROTAC1), a chemical probe, is a von Hippel-Lindau ligand-based SKG3 PROTAC composed of a PEG3-C4-OBn (HY-130620) alkyl linker, an SGK3 degrader (red structure), and a VHL ligand (HY-150803, blue structure). PROTAC SGK3 degrader-1 (0.3 μM) induced 50% endogenous SGK3 degradation within 2 hours, and 80% SGK3 degradation was observed at 8 hours, accompanied by loss of phosphorylation of NDRG1 (SGK3 substrate).
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SGK1-IN-9
0 ImagesCat. No.: HY-185412CAS No.: 2803840-82-4
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1-Chloro-6-methoxyhexane
0 ImagesCat. No.: HY-W260045CAS No.: 22692-46-21-Chloro-6-methoxyhexane is a target protein ligand for PROTAC. 1-Chloro-6-methoxyhexane can be used to synthesize the PROTAC HaloPROTAC-E (HY-145752).
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SGK1-IN-7
0 ImagesCat. No.: HY-182323CAS No.: 3109982-58-0SGK1-IN-7 is a blood-brain barrier-permeable SGK1 inhibitor with an IC50 of 0.72 μM. SGK1-IN-7 reduces the phosphorylation level of TAU protein at the Ser396 and Ser214 epitopes. SGK1-IN-7 antagonizes the toxicity induced by Okadaic acid (HY-N6785). SGK1-IN-7 can be used in the research of Alzheimer's disease.
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CKI-7 free base
0 ImagesCKI-7 free base is a potent and ATP-competitive casein kinase 1 (CK1) inhibitor with an IC50 of 6 μM and a Ki of 8.5 μM. CKI-7 free base is a selective Cdc7 kinase inhibitor. CKI-7 free base also inhibits SGK, ribosomal S6 kinase-1 (S6K1) and mitogen- and stress-activated protein kinase-1 (MSK1). CKI-7 free base has a much weaker effect on casein kinase II and other protein kinases.
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PT109
0 ImagesPT109 is an orally active, blood-brain barrier permeable multi-kinase inhibitor. By inhibiting PTBP1, PT109 promotes the switch of pyruvate kinase isoform from PKM2 to PKM1, thereby effectively inhibiting the proliferation and migration of glioblastoma multiforme and inducing its reprogramming into oligodendrocytes. PT109 also targets and regulates key signaling molecules such as JNK, SGK1, GSK3β to exert neuroprotective effects including promoting neurogenesis, inducing synapse formation and alleviating neuroinflammation. In Alzheimer's disease models, PT109 exhibits significant efficacy in improving spatial learning ability, along with excellent in vivo pharmacokinetic properties. PT109 can be used to investigate metabolic reprogramming of glioblastoma multiforme and neuroprotective mechanisms of Alzheimer's disease.
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CKI-7
0 ImagesCKI-7 is a potent and ATP-competitive casein kinase 1 (CK1) inhibitor with an IC50 of 6 μM and a Ki of 8.5 μM. CKI-7 is a selective Cdc7 kinase inhibitor. CKI-7 also inhibits SGK, ribosomal S6 kinase-1 (S6K1) and mitogen- and stress-activated protein kinase-1 (MSK1). CKI-7 has a much weaker effect on casein kinase II and other protein kinases.
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SGK1-IN-3 hydrochloride
0 ImagesCat. No.: HY-142686ASGK1-IN-3 hydrochloride (Compound 3a) is an ATP-competitive SGK1 inhibitor with an IC50 of <1 nM against hSGK1. SGK1-IN-3 hydrochloride blocks the activity of CDK family members. SGK1-IN-3 hydrochloride serves as a P-glycoprotein substrate. SGK1-IN-3 can be used for the research of osteoarthritis.
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EMD638683 (S-Form)
0 ImagesEMD638683 (S-Form) (Compound 1a), the S-enantiomer of EMD638683 (HY-15193), is a SGK1 inhibitor with an IC50 value > 300 nM. EMD638683 is an orally active 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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Hu7691 free base
0 ImagesCat. No.: HY-132302ACAS No.: 2241232-43-7
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