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Chemical Structure| 1214265-58-3 Chemical Structure| 1214265-58-3

Structure of WZ4003
CAS No.: 1214265-58-3

Chemical Structure| 1214265-58-3

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WZ4003 is a potent and selective NUAK1/2 inhibitor with IC50 values of 20 and 100 nM, respectively.

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Product Details of WZ4003

CAS No. :1214265-58-3
Formula : C25H29ClN6O3
M.W : 496.99
SMILES Code : CCC(NC1=CC=CC(OC2=NC(NC3=CC=C(N4CCN(C)CC4)C=C3OC)=NC=C2Cl)=C1)=O
MDL No. :MFCD28015100
InChI Key :SDGJBAUIGHSMRI-UHFFFAOYSA-N
Pubchem ID :72200024

Safety of WZ4003

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Related Pathways of WZ4003

epigenetics
PI3K-AKT

Isoform Comparison

Biological Activity

Target
  • AMPK

    NUAK2, IC50:100 nM

    NUAK1, IC50:20 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
U2OS cells 10 µM 1000 minutes WZ4003 markedly restricted cells from entering mitosis, similar to the effect of the RO3306 CDK1 inhibitor. Biochem J. 2014 Jul 15;461(2):233-45.
HEK-293 cells 3–10 µM 16 hours To evaluate the inhibitory effect of WZ4003 on NUAK1 activity, results showed that WZ4003 significantly inhibited MYPT1 Ser445 phosphorylation at concentrations of 3–10 μM. Biochem J. 2014 Jan 1;457(1):215-25.
Human jaw bone marrow mesenchymal stem cells 5 µM 2 hours Suppress the APN-induced overexpression of CXCL1 and CXCL8 J Cell Mol Med. 2017 Jul;21(7):1411-1419.
Human brain slice cultures (HBSCs) 10 µM 2 weeks To assess the impact of WZ4003 on p-tau Ser356 levels, it was found that WZ4003 significantly reduced p-tau Ser356 levels while increasing neuronal and synaptic protein levels. Acta Neuropathol. 2024 Jan 4;147(1):7.
WPMY-1 cells 10 µM 24 hours WZ4003 reduced the proliferation rate of WPMY-1 cells and increased the number of dead cells Front Pharmacol. 2023 Apr 28;14:1105427.
Mouse organotypic brain slice cultures (MOBSCs) 5 µM 2-4 weeks To assess the impact of WZ4003 on tau and p-tau Ser356 levels, it was found that WZ4003 significantly reduced both total tau and p-tau Ser356 levels. Acta Neuropathol. 2024 Jan 4;147(1):7.
U2OS cells 10 µM 5 days To evaluate the inhibitory effect of WZ4003 on U2OS cell proliferation, results showed that 10 μM WZ4003 significantly inhibited cell proliferation. Biochem J. 2014 Jan 1;457(1):215-25.
U2OS cells 10 µM 8 hours WZ4003 significantly reduced the population of cells in S-phase, indicating that NUAK1 inhibitors suppress proliferation by reducing S-phase cells. Biochem J. 2014 Jul 15;461(2):233-45.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice NUAK1 knockout mouse embryonic fibroblasts In vitro culture 10 μM Single dose, 15–20 hours To evaluate the inhibitory effect of WZ4003 on the migration of NUAK1 knockout mouse embryonic fibroblasts, results showed that 10 μM WZ4003 significantly inhibited cell migration. Biochem J. 2014 Jan 1;457(1):215-25.

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.01mL

0.40mL

0.20mL

10.06mL

2.01mL

1.01mL

20.12mL

4.02mL

2.01mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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