2. Signaling Pathways
  3. Metabolic Enzyme/Protease
  4. SGK

SGK

Serum-glucocorticoid regulated kinase; Serum and glucocorticoid-regulated kinase

SGK

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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:

SGK Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-15192
    GSK 650394
    		Inhibitor 99.76%
    GSK 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.
    GSK 650394
  • HY-15193
    EMD638683
    		Inhibitor 99.89%
    EMD638683 is a highly selective SGK1 inhibitor, with an IC50 value of 3 μM.
    EMD638683
  • HY-145752
    HaloPROTAC-E
    		Inhibitor 99.62%
    HaloPROTAC-E is a potent Halo PROTAC degrader that reversibly induces degradation of two 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.
    HaloPROTAC-E
  • HY-125878
    PROTAC SGK3 degrader-1
    		Inhibitor 99.02%
    PROTAC SGK3 degrader-1 (SGK3-PROTAC1) 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).
    PROTAC SGK3 degrader-1
  • HY-133028
    CKI-7 free base
    		Inhibitor 99.80%
    CKI-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.
    CKI-7 free base
  • HY-167832
    PT109
    		Inhibitor
    PT109 is a multi-kinase inhibitor. PT109 inhibits JNK (JNK1: IC50=0.143 μM; JNK2: IC50=0.831 μM; JNK3: IC50=0.285 μM) and other kinases (SGK1: IC50=1.34 μM; SGK2: IC50=5.6 μM; SGK3: IC50=26.4 μM; ROCK2: IC50=34 μM) and plays an important role in anti-inflammation, anti-oxidation, neurogenesis, synaptogenesis, etc. In addition, PT109 also reprograms glioblastoma multiforme (GBM) into oligodendrocytes through the PTBP1/PKM1/2 pathway and changes the metabolic pattern of GBM, exerting anti-glioma activity.
    PT109
  • HY-128221
    SGK1-IN-5
    		Inhibitor
    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.
    SGK1-IN-5
  • HY-142686A
    SGK1-IN-3 hydrochloride
    		Inhibitor
    SGK1-IN-3 hydrochloride (compound 3a) is a potent and orally active inhibitor of SGK1. The serine/threonine kinase SGK1 is an activator of the β-catenin pathway and a powerful stimulator of cartilage degradation that is found to be upregulated under genomic control in diseased osteoarthritic cartilage. SGK1-IN-3 hydrochloride has the potential for the research of osteoarthritis.
    SGK1-IN-3 hydrochloride
  • HY-18607
    SGK1-IN-1
    		Inhibitor 99.67%
    SGK1-IN-1 is a highly active and selective inhibitor of SGK-1, with an IC50 of 1 nM.
    SGK1-IN-1
  • HY-142687
    SGK1-IN-4
    		Inhibitor
    SGK1-IN-4 (compound 17a) is a highly selective, orally active SGK1 inhibitor. SGK1-IN-4 can be used for osteoarthritis research.
    SGK1-IN-4
  • HY-135893
    SGK1-IN-2
    		Inhibitor 98.36%
    SGK1-IN-2 (14h) is a selective SGK1 (serum and glucocorticoid regulated kinase 1) inhibitor, with an IC50 of 5 nM at 10 μM ATP concentration.
    SGK1-IN-2
  • HY-117357
    SI-113
    		Inhibitor 98.02%
    SI-113 is a SGK1 inhibitor, with an IC50 of 600 nM. SI113 induces autophagy.
    SI-113
  • HY-15193B
    EMD638683 S-Form
    		Inhibitor 99.95%
    EMD638683 S-Form is the S-form of EMD638683. EMD638683 is a highly selective SGK1 inhibitor with IC50 of 3 μM.
    EMD638683 S-Form
  • HY-132302
    Hu7691
    		Inhibitor
    Hu7691 is an orally active, selective Akt inhibitor with IC50s of 4.0 nM, 97.5 nM, 28 nM for Akt1, Akt2 and Akt3, respectively. Hu7691 inhibits tumor growth and enables decrease of cutaneous toxicity in mice.
    Hu7691
  • HY-15193A
    EMD638683 R-Form
    		Inhibitor 99.86%
    EMD638683 R-Form is the R-form of EMD638683. EMD638683 is a highly selective SGK1 inhibitor with IC50 of 3 μM.
    EMD638683 R-Form
  • HY-142686
    SGK1-IN-3
    		Inhibitor
    SGK1-IN-3 (compound 3a) is a potent and orally active inhibitor of SGK1. The serine/threonine kinase SGK1 is an activator of the β-catenin pathway and a powerful stimulator of cartilage degradation that is found to be upregulated under genomic control in diseased osteoarthritic cartilage. SGK1-IN-3 has the potential for the research of osteoarthritis.
    SGK1-IN-3
  • HY-132302A
    Hu7691 free base
    		Inhibitor
    Hu7691 free base is an orally active, selective Akt inhibitor with IC50s of 4.0 nM, 97.5 nM, 28 nM for Akt1, Akt2 and Akt3, respectively. Hu7691 free base inhibits tumor growth and enables decrease of cutaneous toxicity in mice.
    Hu7691 free base
  • HY-W011109
    CKI-7
    		Inhibitor
    CKI-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.
    CKI-7
  • HY-122011
    PF-4950834
    		Inhibitor
    PF-4950834 is a potent, selective, orally bioavailable, ATP-competitive rho kinase inhibitor with IC50 values of 8.35 nM and 33.12 nM against ROCK2 and ROCK1, respectively. PF-4950834 inhibits neutrophil migration.
    PF-4950834
SGK Isoform Comparison

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