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OICR-9429 is a chemical probe which inhibits the interaction of WDR5 (WD-repeat Protein 5) with peptide regions of MLL and Histone 3 with high selectivity. WDR5 is a part of the mixed-lineage leukemia (MLL) transferase complex that targets histone 3.

oicr-9429 is an antagonist of wdr5-mll interaction.wdr5 has been identified as a component of the mll complex, which is required for histone h3 tri-methylation by its binding of histone h3. thus, wdr5 is reported to be a presenter component of mll, suggesting that wdr5 can bind substrates of methylated histone h3 to the mll complex for further methylation.

OICR-9429 is a cell penetrant, potent and selective antagonist of the interaction of WDR5 (WD repeat domain 5) with peptide regions of MLL and Histone 3 that potently binds to WDR5. OICR-9429 inhibits the interaction of WDR5 with MLL1 and RbBP5 in cells. For full characterization details, please see OICR-9429 on the Structural Genomics Consortium (SGC) website.OICR-0547 is the negative control for the active probe, OICR-9429. To request a sample of the negative control from the SGC, click here.To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc

previous study found that wdr5 could be detected readily in c/ebpα immunoprecipitates from lysates of cebpap30/p30 cells by the treatment of oicr-9429, indicating that the wdr5-mll interaction could not influence p30 binding. moreover, the gene expression profiling of oicr-9429-treated cebpap30/p30 cells showed that wdr5 antagonism could result in the upregulation of myeloid-specific transcripts. in addition, the gene set enrichment analyses demonstrated a close correlation between oicr-9429–induced genes and genes that were upregulated after wdr5 knockdown. furthermore, the gene profile of cebpap30/p30 lics6 was downregulated due to the wdr5 antagonism caused by oicr-9429. further treatment of oicr-9429 to cebpap30/p30 cells was found to be associated with myeloid differentiation and loss of progenitor morphology [1].

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[1] grebien f et al. pharmacological targeting of the wdr5-mll interaction in c/ebpα n-terminal leukemia. nat chem biol.2015 aug;11(8):571-8.