OICR 9429
Tocris Bioscience, part of Bio-Techne | Catalog # 5267
High affinity and selective WDR5 antagonist
Key Product Details
Description
High affinity and selective WDR5 antagonist
Product Description
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
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.Product Specifications
Molecular Weight
555.59
Formula
C29H32F3N5O3
Storage
Store at -20°C
Purity
≥98% (HPLC)
Chemical Name
N-[2-(4-Methylpiperazin-1-yl)-5-[3-(morpholin-4-ylmethyl)phenyl]phenyl]-6-oxo-4-(trifluoromethyl)-1,6-dihydropyridine-3-carboxamide
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.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| 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 all 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 |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
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
Product Specific Notices for OICR 9429
For research use only
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