Selective inhibitor of NUAK1 and NUAK2 kinases with an IC50 of 20 nM for NUAK1 and an IC50 of 100 nM for NUAK2
WZ4003 helps to repress the migration of cells. It also prevents cell proliferation.[1]
WZ4003 is a potent and selective inhibitor of NUAK1 and NUAK2 kinases, members of the AMPK family that are that are activated by the LKB1 (liver kinase B1) tumour suppressor kinase and involved in development and proliferation. WZ4003 has an IC50 of 20 nM for NUAK1 and an IC50 of 100 nM for NUAK2 without significant inhibition of 139 other kinases tested, including ten AMPK-related kinase family members. Treatment with WZ4003 was found to suppress proliferation, restricting cells from entering into mitosis.
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WZ4003 has been expertly reviewed and recommended by the Chemical Probes Portal. For more information, please visit the WZ4003 probe summary on the Chemical Probes Portal website.
The Biochemical journal, 457(1), 215-225 (2013-11-01)
The related NUAK1 and NUAK2 are members of the AMPK (AMP-activated protein kinase) family of protein kinases that are activated by the LKB1 (liver kinase B1) tumour suppressor kinase. Recent work suggests they play important roles in regulating key biological
Hepatocellular carcinoma (HCC) is a complex and deadly disease lacking druggable genetic mutations. The limited efficacy of systemic treatments for advanced HCC implies that predictive biomarkers and drug targets are urgently needed. Most HCC drugs target protein kinases, indicating that
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