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GSK4027

Chemical Structure : GSK4027

CAS No.: 2079896-25-4

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GSK4027 (GSK 4027;GSK-4027)

Catalog No.: PC-35554Not For Human Use, Lab Use Only.

GSK4027 (GSK 4027, GSK-4027) is a potent, selective, cell-penetrant chemical probe inhibitor of PCAF/GCN5 bromodomain with pKi of 8.9 for both.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    GSK4027 (GSK 4027, GSK-4027) is a potent, selective, cell-penetrant chemical probe inhibitor of PCAF/GCN5 bromodomain with pKi of 8.9 for both.
    GSK4027 displays exceptional selectivity over the BET bromodomain family (>18000-fold selectivity over the BET family, >70-fold selectivity over the wider bromodomain families) and proof of cellular target engagement.
    GSK4027 is a useful chemical tool in elucidating the biological phenotype of PCAF/GCN5 bromodomain inhibition.

    Physicochemical Properties

    M.Wt 377.286
    Formula C17H21BrN4O
    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

    4-Bromo-2-methyl-5-(((3R,5R)-1-methyl-5-phenylpiperidin-3-yl)amino)pyridazin-3(2H)-one

    References

    1. Humphreys PG, et al. J Med Chem. 2017 Jan 26;60(2):695-709.

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