WZ4003 is a highly specific NUAK kinase inhibitor with IC50 of 20 nM and 100 nM for NUAK1 and NUAK2, respectively, without significant inhibition on 139 other kinases.
|Cell lines||U2OS cells, and MEFs|
|Preparation method||Following the manufacturer’s protocol ,to carry out cell proliferation assays colorimetrically in 96-well plates using the CellTiter 96 AQueous Non-Radioactive Cell Proliferation Assay kit . Initially, 2000 cells per well are seeded for U2OS cells and 3000 cells per well are seeded for MEFs. The proliferation assays are carried out over 5 days in the presence or absence of 10 μM WZ4003.|
|Incubation time||5 days|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Source||APMIS.m (2017). Figure 7. WZ4003 (Abmole Bioscience Inc. Houston, TX, USA)|
|Cell Lines||HeLa cells|
|Results||Particularly, pifithrin-μ and WZ4003 dramatically decreased 10-G-induced activation of the p53 and p-AMPK protein, respectively.|
J Agric Food Chem. 2017 Mar 15;65(10):2089-2099.
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