OICR 9429

Name: OICR 9429
Brand: Tocris Bioscience
SKU: 5267

Tocris Bioscience, part of Bio-Techne | Catalog # 5267

Citations (4)

COA / SDS

High affinity and selective WDR5 antagonist

Key Product Details

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)
Molecular Weight:	555.59

View Full Technical Details for OICR 9429

Technical Data
Citations

Biological Activity for OICR 9429

OICR 9429 is a high affinity WDR5 antagonist (K_d = 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.

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
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 for OICR 9429

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	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.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.5 mM	3.60 mL	18.00 mL	36.00 mL
2.5 mM	0.72 mL	3.60 mL	7.20 mL
5 mM	0.36 mL	1.80 mL	3.60 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.

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.Med.Chem. 2016 PMID: 26958703
Grebien Pharmacological targeting of the Wdr5-MLL interaction in C/EBPα N-terminal leukemia. Nat.Chem.Biol. 2015 PMID: 26167872