WZ 4003

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Description: Potent and selective NUAK1/2 inhibitor
Chemical Name: N-3-[[5-Chloro-2-[[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]oxy]phenyl]propanamide
Purity: ≥98% (HPLC)
Citations (3)
Literature (1)
Pathways (1)

Biological Activity for WZ 4003

WZ 4003 is a 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 for WZ 4003

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 for WZ 4003

M. Wt 496.99
Formula C25H29ClN6O3
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1214265-58-3
PubChem ID 72200024
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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for WZ 4003

Solvent Max Conc. mg/mL Max Conc. mM
1eq. HCl 24.85 50
DMSO 9.94 20 with gentle warming

Preparing Stock Solutions for WZ 4003

The following data is based on the product molecular weight 496.99. 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 4.02 mL 20.12 mL 40.24 mL
2.5 mM 0.8 mL 4.02 mL 8.05 mL
5 mM 0.4 mL 2.01 mL 4.02 mL
25 mM 0.08 mL 0.4 mL 0.8 mL

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References for WZ 4003

References are publications that support the biological activity of the product.

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

If you know of a relevant reference for WZ 4003, please let us know.

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Keywords: WZ 4003, WZ 4003 supplier, WZ4003, potent, selective, NUAK1, inhibitors, inhibits, NUAK2, NUAK, MYPT1, kinases, 5177, Tocris Bioscience

3 Citations for WZ 4003

Citations are publications that use Tocris products. Selected citations for WZ 4003 include:

Sebastian et al (2019) Development of MAP4 Kinase Inhibitors as Motor Neuron-Protecting Agents. Cell Chem Biol 26 1703-1715.e37 PMID: 31676236

Raymond S et al (2020) Pharmacoproteomics Identifies Kinase Pathways that Drive the Epithelial-Mesenchymal Transition and Drug Resistance in Hepatocellular Carcinoma. Cell Syst 11 196-207.e7 PMID: 32755597

Anne-Claude et al (2020) A novel role for NUAK1 in promoting ovarian cancer metastasis through regulation of fibronectin production in spheroids. Cancers (Basel) 12 PMID: 32429240

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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.

Programmed Cell Death Poster

Programmed Cell Death Poster

There are two currently recognized forms of programmed cell death: apoptosis and necroptosis. This poster summarizes the signaling pathways involved in apoptosis, necroptosis and cell survival following death receptor activation, and highlights the influence of the molecular switch, cFLIP, on cell fate.

Pathways for WZ 4003

AMPK Signaling Pathway

AMPK Signaling Pathway

AMPK signaling pathway plays an important role in the cellular reponse to low levels of available ATP, often caused by stresses such as heat shock, ischemia or hypoxia.
Akt Signaling Pathway

Akt Signaling Pathway

The Akt signaling pathway plays a key role in the mediation of protein synthesis, metabolism, proliferation and cell cycle progression. It may be referred to as a 'prosurvival' pathway.