GSK4027

CAS No. 2079896-25-4

GSK4027 ( GSK 4027;GSK-4027 )

Catalog No. M13238 CAS No. 2079896-25-4

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

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    GSK4027
  • Note
    Research use only, not for human use.
  • Brief Description
    GSK4027 (GSK 4027, GSK-4027) is a potent, selective, cell-penetrant chemical probe of PCAF/GCN5 bromodomain with pKi of 8.9 for both.
  • Description
    GSK4027 (GSK 4027, GSK-4027) is a potent, selective, cell-penetrant chemical probe of PCAF/GCN5 bromodomain with pKi of 8.9 for both; 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.
  • Synonyms
    GSK 4027;GSK-4027
  • Pathway
    Chromatin/Epigenetic
  • Target
    Bromodomain
  • Recptor
    Bromodomain
  • Research Area
    Inflammation/Immunology
  • Indication
    ——

Chemical Information

  • CAS Number
    2079896-25-4
  • Formula Weight
    377.29
  • Molecular Formula
    C17H21BrN4O
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO : 50 mg/mL 132.53 mM
  • SMILES
    CN1C[C@@H](C2=CC=CC=C2)C[C@@H](NC3=C(Br)C(N(C)N=C3)=O)C1
  • Chemical Name
    4-Bromo-2-methyl-5-(((3R,5R)-1-methyl-5-phenylpiperidin-3-yl)amino)pyridazin-3(2H)-one

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

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