Biological Activity
Potent and selective NUAK1/2 inhibitor (IC50 values are 20 and 100 nM respectively). Exhibits no significant inhibition against a panel of 139 kinases, including ten AMPK family members. Inhibits NUAK1-mediated MYPT1 phosphorylation. Also inhibits cell proliferation in U2OS cells.
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 WZ 4003 is reviewed on the chemical probes website.
Technical Data
| M. Wt | 496.99 |
| Formula | C25H29ClN6O3 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1214265-58-3 |
| PubChem ID | 72200024 |
| InChI Key | SDGJBAUIGHSMRI-UHFFFAOYSA-N |
| Smiles | CN(CC3)CCN3C(C=C2)=CC(OC)=C2NC1=NC=C(Cl)C(OC4=CC(NC(CC)=O)=CC=C4)=N1 |
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 | |||
| 1eq. HCl | 24.85 | 50 | |
| DMSO | 9.94 | 20mM with gentle warming |
Preparing Stock Solutions
The following data is based on the product molecular weight 496.99. 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 | 2.01 mL | 10.06 mL | 20.12 mL |
| 5 mM | 0.4 mL | 2.01 mL | 4.02 mL |
| 10 mM | 0.2 mL | 1.01 mL | 2.01 mL |
| 50 mM | 0.04 mL | 0.2 mL | 0.4 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Zhou et al (2009) Novel mutant-selective EGFR kinase inhibitors against EGFR T790M. Nature 462 1070 PMID: 20033049
Banerjee et al (2014) Interplay between Polo kinase, LKB1-activated NUAK1 kinase, PP1βMYPT1 phosphatase complex and the SCFβTrCP E3 ubiquitin ligase. Biochem.J. 461 233 PMID: 24785407
Banerjee et al (2014) Characterization of WZ4003 and HTH-01-015 as selective inhibitors of the LKB1-tumour-suppressor-activated NUAK kinases. Biochem.J. 457 215 PMID: 24171924
Keywords: WZ 4003, supplier, WZ4003, potent, selective, NUAK1, inhibitors, inhibits, NUAK2, NUAK, MYPT1, kinases, NUAK, NUAK, Tocris Bioscience
