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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.
OICR-9429-N-C2-NH2 is a selective ligand for WDR5, a key protein involved in the regulation of gene expression and crucial in oncogenic pathways. This compound facilitates the design and synthesis of PROTACs (Proteolysis Targeting Chimeras), allowing for targeted protein degradation. Its unique properties make it a valuable tool for cancer research and the development of innovative therapeutic strategies.
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.
Z88418521 is a ligand targeting the WDR5-MLL1 complex, acting to disrupt its interaction. This compound demonstrates potential inhibitory effects on pathways associated with oncogenesis, particularly in leukemia research. Z88418521 serves as a valuable tool for investigating the molecular mechanisms underlying various cancer pathologies.
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WDR5 ligand 2 is a specific ligand for the WDR5 protein, which plays a crucial role in regulating gene expression and chromatin dynamics. This compound can be utilized in the synthesis of PROTAC WDR5 degrader 1, facilitating targeted protein degradation studies. Its application is valuable in research focusing on epigenetic regulation and cancer biology.
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Dimethyl-F-OICR-9429-COOH is a potent ligand for the WD40 repeat domain protein 5 (WDR5), functioning as a critical component in the synthesis of proteolysis-targeting chimeras (PROTACs). Its specific binding to WDR5 facilitates the targeted degradation of associated proteins, making it a valuable tool in chemical biology research. This compound is instrumental in the exploration of protein interactions and the development of innovative therapeutic strategies.
