WZ 4003
Chemical Name: N-3-[[5-Chloro-2-[[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]oxy]phenyl]propanamide
Purity: ≥98%
Biological Activity
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
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
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.
Background References
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Characterization of WZ4003 and HTH-01-015 as selective inhibitors of the LKB1-tumour-suppressor-activated NUAK kinases.
Banerjee et al.
Biochem J., 2014;457:215 -
Novel mutant-selective EGFR kinase inhibitors against EGFR T790M.
Zhou et al.
Nature, 2009;462:1070 -
Interplay between Polo kinase, LKB1-activated NUAK1 kinase, PP1βMYPT1 phosphatase complex and the SCFβTrCP E3 ubiquitin ligase.
Banerjee et al.
Biochem.J., 2014;461:233
Product Datasheets
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Citations for WZ 4003
The citations listed below are publications that use Tocris products. Selected citations for WZ 4003 include:
3 Citations: Showing 1 - 3
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A novel role for NUAK1 in promoting ovarian cancer metastasis through regulation of fibronectin production in spheroids.
Authors: Anne-Claude Et al.
Cancers (Basel) 2020;12
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Pharmacoproteomics Identifies Kinase Pathways that Drive the Epithelial-Mesenchymal Transition and Drug Resistance in Hepatocellular Carcinoma.
Authors: Raymond S Et al.
Cell Syst 2020;11:196-207.e7
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Development of MAP4 Kinase Inhibitors as Motor Neuron-Protecting Agents.
Authors: Sebastian Et al.
Cell Chem Biol 2019;26:1703-1715.e37
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