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

SGK

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 Related Products (11):

Cat. No. Product Name Effect Purity
  • 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.
  • HY-15193
    EMD638683
    Inhibitor 99.74%
    EMD638683 is a highly selective SGK1 inhibitor, with an IC50 value of 3 μM.
  • HY-18607
    SGK1-IN-1
    Inhibitor 98.76%
    SGK1-IN-1 is a highly active and selective inhibitor of SGK-1, with an IC50 of 1 nM.
  • HY-125878
    PROTAC SGK3 degrader-1
    Inhibitor 99.32%
    PROTAC SGK3 degrader-1 (SGK3-PROTAC1), is a potent SKG3 degrader based on von Hippel-Lindau ligand. PROTAC SGK3 degrader-1 (0.3 μM) induces 50% degradation of endogenous SGK3 within 2 hours, with maximal 80% degradation observed within 8 hours, accompanied by a loss of phosphorylation of NDRG1 (an SGK3 substrate).
  • HY-133028
    CKI-7 free base
    Inhibitor 99.31%
    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.
  • 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.
  • 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.
  • HY-15193B
    EMD638683 S-Form
    Inhibitor 98.30%
    EMD638683 S-Form is the S-form of EMD638683. EMD638683 is a highly selective SGK1 inhibitor with IC50 of 3 μM.
  • HY-135893
    SGK1-IN-2
    Inhibitor 98.34%
    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.
  • HY-15193A
    EMD638683 R-Form
    Inhibitor 99.68%
    EMD638683 R-Form is the R-form of EMD638683. EMD638683 is a highly selective SGK1 inhibitor with IC50 of 3 μM.
  • 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.
Isoform Specific Products

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