OICR-9429

ChemicalBook > CAS DataBase List > OICR-9429

Product Name: OICR-9429
CAS No.: 1801787-56-3
Chemical Name: OICR-9429
Synonyms: 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
Molecular Formula: C29H32F3N5O3
Formula Weight: 555.59
MOL File: 1801787-56-3.mol

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OICR-9429 Property

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

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H315Causes skin irritation

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P321Specific treatment (see … on this label).

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: SML1209
Product name: OICR-9429
Purity: ≥98% (HPLC)
Packaging: 5MG
Price: $191
Updated: 2023/06/20

Sigma-Aldrich

Product number: SML1209
Product name: OICR-9429
Purity: ≥98% (HPLC)
Packaging: 25MG
Price: $696
Updated: 2022/05/15

Cayman Chemical

Product number: 16095
Product name: OICR-9429
Purity: ≥98%
Packaging: 1mg
Price: $57
Updated: 2024/03/01

Cayman Chemical

Product number: 16095
Product name: OICR-9429
Purity: ≥98%
Packaging: 5mg
Price: $152
Updated: 2024/03/01

Cayman Chemical

Product number: 16095
Product name: OICR-9429
Purity: ≥98%
Packaging: 10mg
Price: $220
Updated: 2024/03/01

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OICR-9429 Chemical Properties,Usage,Production

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] 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 Preparation Products And Raw materials

Raw materials

Preparation Products

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1801787-56-3, OICR-9429Related Search:

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

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

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

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