Catalog Number: 5177
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.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 50 mM in 1eq. HCl and to 20 mM in DMSO with gentle warming
  • Purity:
  • Storage:
    Store at -20°C
  • CAS No:
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.
Background References
  1. 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
  2. Novel mutant-selective EGFR kinase inhibitors against EGFR T790M.
    Zhou et al.
    Nature, 2009;462:1070
  3. 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
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