Catalog Number: 5307
Chemical Name: 1-[[(2S)-5-[(Aminoiminomethyl)amino]-2-[[2-ethyl-2-[(2-methyl-1-oxopropyl)amino]-1-oxobutyl]amino]-1-oxopentyl]amino]-N-[bis(4-fluorophenyl)methyl]-cyclopentanecarboxamide trifluoroacetate
Biological Activity
Potent WDR5/MLL interaction inhibitor (IC50 = 2.4 nM). Inhibits MLL1 methyltransferase activity and MLL-1-induced HoxA9 and Meis-1 gene expression in leukemia cells expressing the MLL1-AF9 fusion gene. Also inhibits cell growth and induces apoptosis in leukemia cells harbouring MLL1 fusion proteins.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 100 mM in DMSO
  • Purity:
  • Storage:
    Store at -20°C
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. High-affinity, small-molecule peptidomimetic inhibitors of MLL1/WDR5 protein-protein interaction.
    Karatas et al.
    J.Am.Chem.Soc., 2013;135:669
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