OICR 9429

Pricing Availability   Qty
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)
Citations (2)
Literature (2)

Biological Activity for OICR 9429

OICR 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.

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 for OICR 9429

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.

Technical Data for OICR 9429

M. Wt 555.59
Formula C29H32F3N5O3
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1801787-56-3
PubChem ID 91623360
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 for OICR 9429

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 27.78 50

Preparing Stock Solutions for OICR 9429

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.

Select a batch to recalculate based on the batch molecular weight:
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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References for OICR 9429

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

2 Citations for OICR 9429

Citations are publications that use Tocris products. Selected citations for OICR 9429 include:

Wolfgang et al (2020) Chemical Genetics Screen Identifies Epigenetic Mechanisms Involved in Dopaminergic and Noradrenergic Neurogenesis in Zebrafish. Front Genet 11 80 PMID: 32158467

Ying et al (2023) Rewired m6A epitranscriptomic networks link mutant p53 to neoplastic transformation. Nat Commun 14 1694 PMID: 36973285

Do you know of a great paper that uses OICR 9429 from Tocris? Please let us know.

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

Epigenetics Scientific Review

Epigenetics Scientific Review

Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.

Epigenetics in Cancer Poster

Epigenetics in Cancer Poster

This poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.