WZ 4003

Cat. No. 5177

WZ 4003 C25H29ClN6O3 [1214265-58-3]

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Chemical Name: N-3-[[5-Chloro-2-[[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]oxy]phenyl]propanamide

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
Solubility:
Soluble to 50 mM in 1eq. HCl and to 20 mM in DMSO with gentle warming
Purity:
>98 %
Storage:
Store at -20°C
CAS No:
1214265-58-3

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.

Certificate of Analysis / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

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.

Zhou et al (2009) Novel mutant-selective EGFR kinase inhibitors against EGFR T790M. Nature 462 1070. PMID: 20033049.

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Citations are publications that use Tocris products.

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

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