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GSK716

Chemical Structure : GSK716

CAS No.: 2406205-61-4

GSK716 (GSK-716)

Catalog No.: PC-38247Not For Human Use, Lab Use Only.

GSK716 (GSK-716) is a potent inhibitor of Z α1-antitrypsin polymerisation, binds to Zα1-antitrypsin with a high-affinity (pKD=8.5).

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    Biological Activity

    GSK716 (GSK-716) is a potent inhibitor of Z α1‐antitrypsin polymerisation, binds to Zα1‐antitrypsin with a high‐affinity (pKD=8.5).
    GSK716 completely blocked the intracellular formation of Zα1‐antitrypsin polymers as measured by staining with the 2C1 anti‐Z α1‐antitrypsin polymer monoclonal antibody (pIC50=6.3).
    GSK716 also increased the secretion of Z α1‐antitrypsin (pEC50=6.2). GSK716 exhibited a good level of selectivity over the off‐target panel and over other serpins.
    GSK716 binds to a cryptic binding pocket, negate the local effects of the Z mutation and stabilise the bound state against progression along the polymerisation pathway.
    GSK716 reduces intracellular polymerisation and increases the secretion of Z α1‐antitrypsin threefold in a transgenic mouse model of Z α1‐antitrypsin deficiency.

    Physicochemical Properties

    M.Wt 370.424
    Formula C21H23FN2O3
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20°C 12 Months; 4°C 6 Months
    In Solvent
    -80°C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    N-((1S,2R)-1-(3-fluoro-2-methylphenyl)-1-hydroxypentan-2-yl)-2-oxoindoline-4-carboxamide

    References

    1. Lomas DA, et al. EMBO Mol Med. 2021 Mar 5;13(3):e13167.

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