- OICR-9429
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- $31.00
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2026-08-19
- CAS:1801787-56-3
- Purity: 97.07%
- Supply Ability: 10g
- OICR-9429
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2026-08-15
- CAS:1801787-56-3
- Min. Order: 1KG
- Purity: 98
- Supply Ability: 1000 KG
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| | OICR-9429 Basic information |
| Product Name: | OICR-9429 | | Synonyms: | 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 | | CAS: | 1801787-56-3 | | MF: | C29H32F3N5O3 | | MW: | 555.59 | | EINECS: | | | Product Categories: | API | | Mol File: | 1801787-56-3.mol |  |
| | OICR-9429 Chemical Properties |
| 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 | | InChI | 1S/C7H5FN2O2/c1-2-3-10-4-5(8)6(11)9-7(10)12/h1,4H,3H2,(H,9,11,12) | | InChIKey | DJOVLOYCGXNVPI-UHFFFAOYSA-N | | SMILES | C1NC(=O)C=C(C(F)(F)F)C=1C(NC1C(N2CCN(C)CC2)=CC=C(C2=CC=CC(CN3CCOCC3)=C2)C=1)=O |
| WGK Germany | WGK 3 | | Storage Class | 11 - Combustible Solids | | Hazard Classifications | Skin Irrit. 2 |
| | OICR-9429 Usage And Synthesis |
| 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] MATTHUS 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 |
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