Catalog Number: 4904
Chemical Name: N-[(1,2-Dihydro-6-methyl-2-oxo-4-propyl-3-pyridinyl)methyl]-1-(1-methylethyl)-6-[6-[4-(1-methylethyl)-1-piperazinyl]-3-pyridinyl]-1H-indazole-4-carboxamide
Biological Activity
Potent and SAM-competitive EZH2/EZH1 lysine methyltransferase inhibitor (IC50 values are 2 and 45 nM respectively). Selective for EZH2/EZH1 over a panel of other methyltransferases and non-epigenetic targets. Reduces H3K27me3 levels in vitro. Prolongs survival of MLL-AF9 bearing mice. Orally bioavailable.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 100 mM in 1eq. HCl and to 20 mM in DMSO
  • Purity:
  • Storage:
    Store at +4°C
  • CAS No:
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.
Additional Information
Licensing Caveats:
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the UNC 1999 probe summary on the SGC website.
Other Product-Specific Information:
Background References
  1. An orally bioavailable chemical probe of the Lysine Methyltransferases EZH2 and EZH1.
    Konze et al.
    ACS Chem.Biol., 2013;8:1324
  2. Selective inhibition of EZH2 and EZH1 enzymatic activity by a small molecule suppresses MLL-rearranged leukemia.
    Xu et al.
    Blood, 2015;125:346
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