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WDR5 inhibitors and degraders act on WD repeat domain 5 (WDR5), a chromatin scaffold protein. WDR5 is a core subunit of the mixed-lineage leukemia (MLL) complexes that methylate lysine 4 of histone H3 (H3K4). A 2005 study showed that WDR5 binds methylated H3K4 and is required for this methylation and for vertebrate development. In 2015 WDR5 was also shown to help the transcription factor c-Myc recognize its target genes. OICR-9429, MM-589 and WDR5-0103 block the interaction between WDR5 and MLL. MS67 and MS33 are degraders that remove WDR5 protein from cells instead of only occupying a binding site.
WDR5-0103 is a small molecule that binds a peptide-binding pocket on WDR5 (Kd = 450 nM), inhibiting the catalytic activity of the MLL core complex in vitro (IC50 = 39 M).
OICR-9429 is a novel small-molecule antagonist of the Wdr5-MLL interaction with IC50 of 5 uM. inhibit proliferation and induce differentiation .
OICR-0547 is a closely related derivative of OICR-9429. OICR-9429 is a novel small-molecule antagonist of the Wdr5-MLL interaction, while OICR-0547 cannot bind to WDR5.
WDR5-47 is a potent WDR5 antagonist that specifically disrupts the WDR5-MLL1 interaction. This compound demonstrates significant biological activity with a dissociation constant (Kd) of 0.3 μM, showcasing its effectiveness in inhibiting WDR5-mediated functions. WDR5-47 is ideal for research applications focusing on epigenetic regulation and will aid in the investigation of oncogenic processes involving the MLL1 complex.
