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MM 102

5307 Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
5307/10
Lysine Methyltransferase Inhibitors Small Molecule
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Description: Potent WDR5/MLL interaction inhibitor

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

Purity: ≥98%

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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:
783.83
Formula:
C35H49F2N7O4.CF3CO2H
Solubility:
Soluble to 100 mM in DMSO
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
1883545-52-5

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

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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