OICR-9429 |
| Catalog No.GC16397 |
OICR-9429 es un inhibidor del dominio 5 de repeticiÓn de WD de alta afinidad (WDR5), bloquea de forma competitiva la interacciÓn de WDR5 con la proteÍna MLL mediante la uniÓn al bolsillo central de uniÓn de péptidos de WDR5. OICR-9429 puede suprimir la trimetilaciÓn de la histona H3K4 y puede usarse para la investigaciÓn de varios tipos de cÁncer, incluida la leucemia sin reordenamiento MLL, cÁncer de colon, pÁncreas, prÓstata y cÁncer de vejiga (BCa).
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Cas No.: 1801787-56-3
Sample solution is provided at 25 µL, 10mM.
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IC50: 5 uM
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.
In vitro: 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].
In vivo: So far, there is no animal in vivo data reported.
Clinical trial: Up to now, OICR-9429 is still in the preclinical development stage.
Reference:
[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.
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