Biological Activity
WD repeat-containing protein 5 (WDR5) antagonist (Kd = 450 nM). Disrupts WDR5 interaction with MLL and inhibits MLL core complex methyltransferase activity in vitro. Has no effect on a panel of seven other methyltransferases, including SETD7.
Compound Libraries
WDR5 0103 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 383.44 |
| Formula | C21H25N3O4 |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 890190-22-4 |
| PubChem ID | 6457069 |
| InChI Key | ZPLBXOVTSNRBFB-UHFFFAOYSA-N |
| Smiles | O=C(OC)C1=CC(NC(C3=CC=CC(OC)=C3)=O)=C(N2CCN(C)CC2)C=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 38.34 | 100 | |
| ethanol | 19.17 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 383.44. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.61 mL | 13.04 mL | 26.08 mL |
| 5 mM | 0.52 mL | 2.61 mL | 5.22 mL |
| 10 mM | 0.26 mL | 1.3 mL | 2.61 mL |
| 50 mM | 0.05 mL | 0.26 mL | 0.52 mL |
Molarity Calculator
Reconstitution Calculator
Dilution Calculator
Product Datasheets
References
References are publications that support the products' biological activity.
Senisterra et al (2013) Small-molecule inhibition of MLL activity by disruption of its interaction with WDR5. Biochem.J. 449 151 PMID: 22989411
Keywords: WDR5 0103, supplier, WDR50103, WDR5, antagonists, MLL, methyltransferases, epigenetics, WD, repeat-containing, Lysine, Methyltransferases, Lysine, Methyltransferases, Lysine, Methyltransferases, Tocris Bioscience
