| Identification | Back Directory | [Name]
N-(4-(4-methylpiperazin-1-yl)-3'-(morpholinomethyl)-[1,1'-biphenyl]-3-yl)-6-oxo-4-(trifluoromethyl)-1,6-dihydropyridine-3-carboxamide | [CAS]
1801787-56-3 | [Synonyms]
CS-2362
OICR-9429 (OICR9429
6-hydroxy-N-(4-(4-methylpiperazin-1-yl)-3'-(morpholinomethyl)-[1,1'-biphenyl]-3-yl)-4-(trifluoromethyl)nicotinamide
N-[2-(4-Methylpiperazin-1-yl)-5-[3-(morpholin-4-ylmethyl)phenyl]phenyl]-6-oxo-4-(trifluoromethyl)-1,6-dihydropyridine-3-carboxamide
N-(4-(4-methylpiperazin-1-yl)-3'-(morpholinomethyl)-[1,1'-biphenyl]-3-yl)-6-oxo-4-(trifluoromethyl)-1,6-dihydropyridine-3-carboxamide
3-Pyridinecarboxamide, 1,6-dihydro-N-[4-(4-methyl-1-piperazinyl)-3'-(4-morpholinylmethyl)[1,1'-biphenyl]-3-yl]-6-oxo-4-(trifluoromethyl)- | [Molecular Formula]
C29H32F3N5O3 | [MDL Number]
MFCD28411621 | [MOL File]
1801787-56-3.mol | [Molecular Weight]
555.59 |
| Chemical Properties | Back Directory | [Boiling point ]
693.0±55.0 °C(Predicted) | [density ]
1.325±0.06 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
insoluble in EtOH; insoluble in H2O; ≥21.52 mg/mL in DMSO | [form ]
powder | [pka]
8.84±0.10(Predicted) | [color ]
white to light brown |
| Hazard Information | Back Directory | [Uses]
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. | [Biological Activity]
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. | [Biochem/physiol Actions]
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 | [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]. | [IC 50]
5 um | [storage]
Store at -20°C | [References]
[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. |
|
|