Catalog Number: 5267
Chemical Name: N-[2-(4-Methylpiperazin-1-yl)-5-[3-(morpholin-4-ylmethyl)phenyl]phenyl]-6-oxo-4-(trifluoromethyl)-1,6-dihydropyridine-3-carboxamide
Biological Activity
High affinity WDR5 antagonist (Kd = 93 nM); disrupts WDR5-MLL interaction. Exhibits selectivity for WDR5 over 22 methyltransferases and a panel of kinases, GPCRs, ion channels, and transporters. Reduces viability of acute myeloid leukemia cells in vitro. Also disrupts MLL1-RbBP5 interaction.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 50 mM in DMSO
  • Purity:
  • Storage:
    Store at -20°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 OICR-9429 probe summary on the SGC website.
Background References
  1. Pharmacological targeting of the Wdr5-MLL interaction in C/EBPα N-terminal leukemia.
    Grebien et al.
    Nat.Chem.Biol., 2015;11:571
  2. Structure-Based Optimization of a Small Molecule Antagonist of the Interaction Between WD Repeat-Containing Protein 5 (WDR5) and Mixed-Lineage Leukemia 1 (MLL1).
    Getlik et al.
    J.Med.Chem., 2016;59:2478
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