OICR-9429 Struktur

OICR-9429

Bezeichnung:OICR-9429

CAS-Nr1801787-56-3

Englisch Name:OICR-9429

CBNumberCB43133471

SummenformelC29H32F3N5O3

Molgewicht555.59

MOL-Datei1801787-56-3.mol

OICR-9429 physikalisch-chemischer Eigenschaften

Siedepunkt	693.0±55.0 °C(Predicted)
Dichte	1.325±0.06 g/cm3(Predicted)
storage temp.	2-8°C
Löslichkeit	insoluble in EtOH; insoluble in H2O; ≥21.52 mg/mL in DMSO
pka	8.84±0.10(Predicted)
Aggregatzustand	powder
Farbe	white to light brown

Gefahreninformationscode (GHS)

OICR-9429 Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden
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.
Biologische Aktivität
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
Lager
Store at -20°C
Einzelnachweise
[1] FLORIAN GREBIEN. Pharmacological targeting of the Wdr5-MLL interaction in C/EBPα N-terminal leukemia[J]. Nature chemical biology, 2015, 11 8: 571-578. DOI:10.1038/nchembio.1859.
[2] DONG A, DOMBROVSKI L, WALKER J, et al. Crystal structure of human WDR5 in complex with compound OICR-9429[C]. 2014: 0. DOI:10.2210/pdb4ql1/pdb.
[3] MATTH?US GETLIK. Structure-Based Optimization of a Small Molecule Antagonist of the Interaction Between WD Repeat-Containing Protein 5 (WDR5) and Mixed-Lineage Leukemia 1 (MLL1)[J]. Journal of Medicinal Chemistry, 2016, 59 6: 2478-2496. DOI:10.1021/acs.jmedchem.5b01630.

OICR-9429 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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