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.
J Agric Food Chem. 2017 Mar 15;65(10):2089-2099.
10-Gingerol, a Phytochemical Derivative from “Tongling White Ginger”, Inhibits Cervical Cancer: Insights into the Molecular Mechanism and Inhibitory Targets
WZ4003 purchased from AbMole
Cell Experiment | |
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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. |
Concentrations | ~10 μM |
Incubation time | 5 days |
Animal Experiment | |
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Animal models | |
Formulation | |
Dosages | |
Administration |
Molecular Weight | 496.99 |
Formula | C25H29ClN6O3 |
CAS Number | 1214265-58-3 |
Solubility (25°C) | DMSO ≥ 10 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
[2] Huali Yang, et al. Optimization of WZ4003 as NUAK inhibitors against human colorectal cancer
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