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Submit ReviewOICR 9429 is a 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.
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.
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.
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.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 27.78 | 50 |
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 |
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.
Keywords: OICR 9429, OICR 9429 supplier, OICR9429, High, affinity, selective, WDR5, antagonists, WD, repeat-containing, proteins, 5, antagonism, sgc, WD40, Lysine, Methyltransferases, 5267, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for OICR 9429 include:
Ying et al (2023) Rewired m6A epitranscriptomic networks link mutant p53 to neoplastic transformation. Nat Commun 14 1694 PMID: 36973285
Wolfgang et al (2020) Chemical Genetics Screen Identifies Epigenetic Mechanisms Involved in Dopaminergic and Noradrenergic Neurogenesis in Zebrafish. Front Genet 11 80 PMID: 32158467
Do you know of a great paper that uses OICR 9429 from Tocris? Please let us know.
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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