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Biological Activity:

WDR5-0103 is a potent and selective WD repeat-containing protein 5 (WDR5) antagonist with Kd of 450 nM. It has no effect on a panel of seven other methyltransferases, including SETD7. It binds in the WDR5 peptide-binding pocket and inhibits the catalytic activity of the MLL core complex in vitro. WDR5-0103 is a good chemical probe to demonstrate inhibition of an important protein-protein interaction and form the basis for further development of inhibitors of WDR5-dependent enzymes implicated in MLL-rearranged leukaemias or other cancers.

How to Use:

In vitro: WDR5-0103 was used at 10 µM final concentration in various in vitro assays.
In vivo: n/a

Reference:

• 1. Senisterra G, et al. Small-molecule inhibition of MLL activity by disruption of its interaction with WDR5. (2013) Biochem J. 449(1):151-9.