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WZ4003 is a potent and selective inhibitor of NUAK1 and NUAK2 with IC50 values of 20 and 100 nM, respectively [1].

NUAK family SNF1-like kinase-1 (NUAK1) and the related NUAK2 belong to the AMP-activated protein kinase (AMPK) family and are activated by liver kinase B1 (LKB1) tumour suppressor protein kinase [1].

WZ4003 is a potent and selective NUAK1/2 inhibitor. In HEK-293 cells, WZ4003 inhibited the phosphorylation of myosin phosphate-targeting subunit 1 (MYPT1), which was phosphorylated by NUAK1 at Ser445. In HEK-293 cells overexpressing inhibitor-resistant NUAK1[A195T], WZ4003 didn’t inhibit the phosphorylation of MYPT1 at Ser445. In mouse embryonic fibroblasts (MEFs), WZ4003 significantly inhibited migration in a wound-healing assay and inhibited MEFs proliferation. In a cell invasion assay, WZ4003 inhibited the invasive potential of U2OS cells [1]. In U2OS cells, WZ4003 (10 μM) inhibited phosphorylation of MYPT1 and reduced the cells in S-phase by 50%. Also, WZ4003 prevented cells from entering into mitosis [2].

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