Name: GSK 650394
Price: 274.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    GSK 650394 is a small molecule inhibitor of serum and glucocorticoid-regulated kinase 1 (SGK1) with IC50 value of 13nM [1].
    Sgk1 gene is a target gene of androgen. Knockdown of SGK1 expression attenuates androgen-mediated growth of the prostate cancer cell line. Thus, the inhibition of SGK1 is a novel mechanism for the treatment of prostate cancer. GSK 650394 is a competitive inhibitor of SGK1. It shows potent inhibitory activity against the purified SGK1 with IC50 value of 13nM in a fluorescence polarization assay. In the activity-based scintillation proximity assay, GSK 650394 prevents the phosphorylation activity of SGK1 and SGK2 with IC50 values of 62nM and 103nM, respectively. Moreover, GSK 650394 suppresses the androgen-mediated increase of Nedd4-2 phosphorylation in LNCaP cells. It also significantly inhibits cell growth stimulated by androgen with IC50 value of about 1μM [1].
    
    [1] Sherk A B, Frigo D E, Schnackenberg C G, et al. Development of a small-molecule serum-and glucocorticoid-regulated kinase-1 antagonist and its evaluation as a prostate cancer therapeutic. Cancer research, 2008, 68(18): 7475-7483.
- Properties
  - Alternative Name
    
    2-cyclopentyl-4-(5-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)benzoic acid
    
    CAS Number
    
    890842-28-1
    
    Molecular Formula
    
    C25H22N2O2
    
    Molecular Weight
    
    382.45
    
    Appearance
    
    A solid
    
    Purity
    
    98.36%
    
    Solubility
    
    insoluble in EtOH; insoluble in H2O; ≥19.1 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Rong Li, Xiaoqiu Wang, et al. "The role of epithelial Progesterone Receptor Isoforms in embryo implantation." iScience. 2021 Nov 20;24(12):103487. PMID:34934913
    2. Koesema E, Kodadek T. "Global analysis of gene expression mediated by OX1 orexin receptor signaling in a hypothalamic cell line." PLoS One. 2017 Nov 16;12(11):e0188082. PMID:29145494
    3. Dr.Alvaro Diaz. "Condicionamiento de células dendríticas por la capa laminar de Echinococcus granulosus: búsqueda de agonistas y mecanismos a nivel de señalizacón." colibri.udelar.edu.uy.2016.

GSK 650394

GSK 650394

Background

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