WD repeat-containing protein 5 (WDR5) antagonist (Kd
= 450 nM). Disrupts WDR5 interaction with MLL and inhibits MLL core complex methyltransferase activity in vitro
. Has no effect on a panel of seven other methyltransferases, including SETD7.
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Small-molecule inhibition of MLL activity by disruption of its interaction with WDR5.
Senisterra et al.