OICR-9429
目录号 : GC16397A probe for WDR5
Cas No.:1801787-56-3
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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.
Cas No. | 1801787-56-3 | SDF | |
化学名 | N-(4-(4-methylpiperazin-1-yl)-3'-(morpholinomethyl)-[1,1'-biphenyl]-3-yl)-6-oxo-4-(trifluoromethyl)-1,6-dihydropyridine-3-carboxamide | ||
Canonical SMILES | O=C(C(C(C(F)(F)F)=C1)=CNC1=O)NC2=CC(C3=CC=CC(CN4CCOCC4)=C3)=CC=C2N5CCN(C)CC5 | ||
分子式 | C29H32F3N5O3 | 分子量 | 555.59 |
溶解度 | DMSO: 0.5 mg/ml (with gentle warming),Methanol: 0.5 mg/ml (with gentle warming) | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg | |
1 mM | 1.7999 mL | 8.9994 mL | 17.9989 mL |
5 mM | 0.36 mL | 1.7999 mL | 3.5998 mL |
10 mM | 0.18 mL | 0.8999 mL | 1.7999 mL |
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2.
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