OICR-9429
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- CAS-Nr.
- 1801787-56-3
- Englisch Name:
- OICR-9429
- Synonyma:
- CS-2362;OICR-9429;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)-1H-pyridine-3-carboxamide;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;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)-;OICR9429,pancreatic,Histone Methyltransferase,MLL,inhibit,OICR-9429,colon,prostate cance,bladder cancer (BCa),Inhibitor,WD repeat domain 5 (WDR5),Apoptosis,leukaemia,H3K4
- CBNumber:
- CB43133471
- Summenformel:
- C29H32F3N5O3
- Molgewicht:
- 555.59
- MOL-Datei:
- 1801787-56-3.mol
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OICR-9429 Eigenschaften
- Siedepunkt:
- 693.0±55.0 °C(Predicted)
- Dichte
- 1.325±0.06 g/cm3(Predicted)
- storage temp.
- 2-8°C
- L?slichkeit
- 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
Sicherheit
- Risiko- und Sicherheitserkl?rung
- Gefahreninformationscode (GHS)
| Bildanzeige (GHS) |
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| Alarmwort |
Warnung |
| Gefahrenhinweise |
| Code |
Gefahrenhinweise |
Gefahrenklasse |
Abteilung |
Alarmwort |
Symbol |
P-Code |
| H315 |
Verursacht Hautreizungen. |
Hautreizung |
Kategorie 2 |
Warnung |
![GHS hazard pictograms]() src="/GHS07.jpg" width="20" height="20" /> |
P264, P280, P302+P352, P321,P332+P313, P362 |
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| Sicherheit |
| P264 |
Nach Gebrauch gründlich waschen. |
| P264 |
Nach Gebrauch gründlich waschen. |
| P302+P352 |
BEI BERüHRUNG MIT DER HAUT: Mit viel Wasser/... (Hersteller kann, falls zweckm??ig, ein Reinigungsmittel angeben oder, wenn Wasser eindeutig ungeeignet ist, ein alternatives Mittel empfehlen) waschen. |
| P321 |
Besondere Behandlung |
| P332+P313 |
Bei Hautreizung: ?rztlichen Rat einholen/?rztliche Hilfe hinzuziehen. |
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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.
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
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 Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
OICR-9429 Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.
Global( 90)Lieferanten
- N-(4-(4-methylpiperazin-1-yl)-3'-(morpholinomethyl)-[1,1'-biphenyl]-3-yl)-6-oxo-4-(trifluoromethyl)-1,6-dihydropyridine-3-carboxamide
- 6-hydroxy-N-(4-(4-methylpiperazin-1-yl)-3'-(morpholinomethyl)-[1,1'-biphenyl]-3-yl)-4-(trifluoromethyl)nicotinamide
- CS-2362
- OICR-9429 (OICR9429
- N-[2-(4-Methylpiperazin-1-yl)-5-[3-(morpholin-4-ylmethyl)phenyl]phenyl]-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)-
- N-[2-(4-methylpiperazin-1-yl)-5-[3-(morpholin-4-ylmethyl)phenyl]phenyl]-6-oxo-4-(trifluoromethyl)-1H-pyridine-3-carboxamide
- OICR9429,pancreatic,Histone Methyltransferase,MLL,inhibit,OICR-9429,colon,prostate cance,bladder cancer (BCa),Inhibitor,WD repeat domain 5 (WDR5),Apoptosis,leukaemia,H3K4
- OICR-9429
- N-(4-(4-Methylpiperazin-1-yl)-3'-(morpholinomethyl)-[1,1'-biphenyl]-3-yl)-6-oxo-4-(trifluoromethyl)-1,6-dihydropyridine-3-carboxamide
- 1801787-56-3
- C29H32F3N5O3
- API
