WDR5-0103

890190-22-4

C21H25N3O4

DMSO : >= 40 mg/mL (104.32 mM)

Epigenetics

WDR5-0103 is a potent and selective WD repeat-containing protein 5 (WDR5) antagonist with Kd of 450 nM. IC50 value: 450 nM (Kd) Target: WDR5 in vitro: WDR5-0103 inhibits MLL catalytic activity with an IC50 value of 39+/-10 uM. An increase in MLL complex concentration resulted in proportional increase in IC50 values for WDR5-0103 (83+/-10 and 280+/-12 uM at concentrations of 500 and 1000 nM of the core trimeric MLL complex respectively). These data are consistent with a mechanism of action in which WDR5-0103 antagonizes the interaction of WDR5 with MLL by competing with MLL for their mutual binding site on WDR5.