Name: OICR-9429
Price: 254.00 USD

- Overview
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    Background
    
    IC50: 5 uMOICR-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.
- Properties
  - Categories
    
    Wdr5-MLL interaction antagonist
    
    Alternative Name
    
    N-(4-(4-methylpiperazin-1-yl)-3'-(morpholinomethyl)-[1,1'-biphenyl]-3-yl)-6-oxo-4-(trifluoromethyl)-1,6-dihydropyridine-3-carboxamide
    
    CAS Number
    
    1801787-56-3
    
    Molecular Formula
    
    C29H32F3N5O3
    
    Molecular Weight
    
    555.59
    
    Appearance
    
    A crystalline solid
    
    Purity
    
    98.00%
    
    Solubility
    
    insoluble in EtOH; insoluble in H2O; ≥21.52 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    SMILES
    
    O=C(C(C(C(F)(F)F)=C1)=CNC1=O)NC2=CC(C3=CC=CC(CN4CCOCC4)=C3)=CC=C2N5CCN(C)CC5
    
    * For Research Use Only
- Reference
  - 1. Bhattacharya U, Gutter-Kapon L, et al. "Heparanase and Chemotherapy Synergize to Drive Macrophage Activation and Enhance Tumor Growth." Cancer Res. 2020 Jan 1;80(1):57-68. PMID:31690669

Documents

COA (Certificate Of Analysis)

MSDS (Material Safety Data Sheet)

Datasheet

OICR-9429

OICR-9429

Background

Documents

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