Catalog Number: 4703
Alternate Names: DZNep, NSC 617989
Chemical Name: (1S,2R,5R)-5-(4-Amino-1H-imidazo[4,5-c]pyridin-1-yl)-3-(hydroxymethyl)-3-cyclopentene-1,2-diol hydrochloride
Biological Activity
Histone methyltransferase inhibitor; decreases global histone methylation. Inhibits EZH2 histone methyltransferase and s-adenosylhomocysteine (SAH) hydrolase activity. Blocks trimethylation of lysine 27 on histone H3 and lysine 20 on histone H4 in vitro. Induces apoptosis in multiple cancer cell lines and has no apoptotic effect on normal cells. Enhances Oct4 expression in chemically induced pluripotent stem cells (CiPSCs).
Technical Data
  • M.Wt:
    298.73
  • Formula:
    C12H14N4O3.HCl
  • Solubility:
    Soluble to 10 mM in water
  • Purity:
    >98%
  • Storage:
    Store at -20°C
  • CAS No:
    120964-45-6
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Pharmacologic disruption of Polycomb-repressive complex 2-mediated gene repression selectively induces apoptosis in cancer cells.
    Tan J, Yang X, Zhuang L et al.
    Genes Dev.
  2. Pluripotent stem cells induced from mouse somatic cells by small-molecule compounds.
    Hou et al.
    , 2013;341:651
  3. DZNep is a global histone methylation inhibitor that reactivates developmental genes not silenced by DNA methylation.
    Miranda et al.
    Mol.Cancer Ther., 2009;8:1579
  4. Synthesis of 3-deazaneplanocin A, a powerful inhibitor of S-adenosylhomocysteine hydrolase with potent and selective in vitro and in vivo antiviral activities.
    Tseng et al.
    J.Med.Chem., 1989;32:1442

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