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Submit ReviewOICR 9429
Description: High affinity and selective WDR5 antagonist
Chemical Name: N-[2-(4-Methylpiperazin-1-yl)-5-[3-(morpholin-4-ylmethyl)phenyl]phenyl]-6-oxo-4-(trifluoromethyl)-1,6-dihydropyridine-3-carboxamide
Purity: ≥98% (HPLC)
Biological Activity
High affinity WDR5 antagonist (Kd = 93 nM; IC50 = 64 nM); disrupts WDR5-MLL interaction. Exhibits selectivity for WDR5 over 22 methyltransferases and a panel of kinases, GPCRs, ion channels, and transporters. Reduces viability of acute myeloid leukemia cells in vitro. Also disrupts MLL1-RbBP5 interaction.
To request the negative control for OICR 9429, please fill out the OICR 0547 request form on the SGC website.
Licensing Information
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the OICR-9429 probe summary on the SGC website.
External Portal Information
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of OICR 9429 is reviewed on the chemical probes website.
Compound Libraries
OICR 9429 is also offered as part of the Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 555.59 |
| Formula | C29H32F3N5O3 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1801787-56-3 |
| PubChem ID | 91623360 |
| InChI Key | DJOVLOYCGXNVPI-UHFFFAOYSA-N |
| Smiles | CN(CC4)CCN4C1=C(NC(C5=CNC(C=C5C(F)(F)F)=O)=O)C=C(C2=CC(CN3CCOCC3)=CC=C2)C=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 27.78 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 555.59. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.5 mM | 3.6 mL | 18 mL | 36 mL |
| 2.5 mM | 0.72 mL | 3.6 mL | 7.2 mL |
| 5 mM | 0.36 mL | 1.8 mL | 3.6 mL |
| 25 mM | 0.07 mL | 0.36 mL | 0.72 mL |
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Product Datasheets
References
References are publications that support the biological activity of the product.
Grebien et al (2015) Pharmacological targeting of the Wdr5-MLL interaction in C/EBPα N-terminal leukemia. Nat.Chem.Biol. 11 571 PMID: 26167872
Getlik et al (2016) 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.Med.Chem. 59 2478 PMID: 26958703
If you know of a relevant reference for OICR 9429, please let us know.
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Keywords: OICR 9429, OICR 9429 supplier, OICR9429, High, affinity, selective, WDR5, antagonists, WD, repeat-containing, proteins, 5, antagonism, sgc, Lysine, Methyltransferases, 5267, Tocris Bioscience
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Epigenetics in Cancer Poster
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