WDR5 0103

WDR5-0103 is a small molecule that binds a peptide-binding pocket on WDR5 (Kd = 450 nM). It inhibits the catalytic activity of MLL core complex in in vitro experiments with IC₅₀ of 39 µM. WDR5 is a component of mixed lineage leukemia (MLL) that targets histone-3 and in vitro data shows interaction of WDR5-0103 with MLL inhibits MLL core complex methyltransferase activity. However WDR5-0103 has no effect on other methyltransferases.