WZ 4003

Pricing Availability Delivery Time Qty
Cat.No. 5177 - WZ 4003 | C25H29ClN6O3 | CAS No. 1214265-58-3
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)
Datasheet
Citations
Literature
Pathways

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.

Select a batch to recalculate based on the batch molecular weight:
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

Safety Datasheet

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


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

Citations for WZ 4003

Citations are publications that use Tocris products.

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Reviews

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Literature in this Area

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases
Programmed Cell Death

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

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

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.

Protocols

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