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WZ4003

Cat. No. M3132
WZ4003 Structure
Size Price Availability Quantity
5mg USD 50  USD50 In stock
10mg USD 80  USD80 In stock
25mg USD 155  USD155 In stock
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Quality Control & Documentation
Biological Activity

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.

Product Citations
Customer Product Validations & Biological Datas
Source APMIS.m (2017). Figure 7. WZ4003 (Abmole Bioscience Inc. Houston, TX, USA)
Method Western blot
Cell Lines HeLa cells
Concentrations
Incubation Time
Results Particularly, pifithrin-μ and WZ4003 dramatically decreased 10-G-induced activation of the p53 and p-AMPK protein, respectively.
Protocol (for reference only)
Cell Experiment
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
Animal models
Formulation
Dosages
Administration
Chemical Information
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
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Jiabin Chen, et al. WZ4003 sensitizes non-small cell lung cancer cells to gefitinib via inhibition of ARK5 and epithelial-to-mesenchymal transition

[2] Huali Yang, et al. Optimization of WZ4003 as NUAK inhibitors against human colorectal cancer

[3] Yinfei Pu, et al. Adiponectin promotes human jaw bone marrow mesenchymal stem cell chemotaxis via CXCL1 and CXCL8

[4] Sourav Banerjee, et al. Interplay between Polo kinase, LKB1-activated NUAK1 kinase, PP1βMYPT1 phosphatase complex and the SCFβTrCP E3 ubiquitin ligase

[5] Sourav Banerjee, et al. Characterization of WZ4003 and HTH-01-015 as selective inhibitors of the LKB1-tumour-suppressor-activated NUAK kinases

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Keywords: WZ4003 supplier, AMPK, inhibitors, activators


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