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GSK1120360A

Chemical Structure : GSK1120360A

CAS No.: 931399-19-8

GSK1120360A (GSK360A)

Catalog No.: PC-49790Not For Human Use, Lab Use Only.

GSK1120360A (GSK360A) is a potent, specific and orally active inhibitor of HIF PHD enzyme with pIC50 of 8.0/7.0/6.9 for PHD1/2/3, respectively.

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    Biological Activity

    GSK1120360A (GSK360A) is a potent, specific and orally active inhibitor of HIF PHD enzyme with pIC50 of 8.0/7.0/6.9 for PHD1/2/3, respectively.
    GSK360A acts by competing with the a-ketoglurtarate site and has little or no activity on inhibiting HIF-1 asparaginyl hydroxylase (FIH-1) or collagen 4-prolyl hydroxylase (pIC50 =5.0 and 5.7, respectively).
    GSK360A increased secreted EPO protein level by 50% at 3 uM and vascular endothelial growth factor protein level by 50% at 1 uM, respectively, in Hep3B cells.
    GSK360A exerts systemic and local effects by stabilizing HIF-1 alpha signaling and improves long-term ventricular function, remodeling, and vascularity in a model of established ventricular dysfunction.
    GSK360A enhances rotator cuff regeneration following a chronic tear.

    Physicochemical Properties

    M.Wt 348.33
    Formula C17H17FN2O5
    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-{[1-(2-cyclopropylethyl)-6-fluoro-4-hydroxy-2-oxo-1, 2-dihydro-3-quinolinyl] carbonyl} glycine

    References

    1. Weike Bao, et al. J Cardiovasc Pharmacol. 2010 Aug;56(2):147-55.

    2. J P Gumucio, et al. Bone Joint Res. 2017 Jan;6(1):57-65.

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