WZ4003
Based on 8 publication(s) in Google Scholar
WZ4003 is the first potent and highly specific NUAK kinase inhibitor with IC50 of 20 nM/100 nM for NUAK1 (ARK5)/NUAK2, without significant inhibition on other 139 kinases.
For research use only. We do not sell to patients.
- Purity: 98.22%
- CAS No.: 1214265-58-3
- Formula: C25H29ClN6O3
- Molecular Weight:496.99
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) WZ4003
More- Cancer Discov. 2018 May;8(5):632-647. [Abstract]
- Nat Commun. 2026 Feb 12;17(1):1214. [Abstract]
- Cell Rep. 2025 Mar 21;44(4):115456. [Abstract]
- J Cell Biol. 2019 Apr 1;218(4):1369-1389. [Abstract]
- Cell Biosci. 2023 Dec 22;13(1):232. [Abstract]
- Commun Biol. 2021 Mar 25;4(1):399. [Abstract]
- Technical University of Dresden. 2025.
- University of Texas. 2025.
Customer Validation & Images
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WB
All AMPK Isoforms
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Biological Activity
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NUAK1 20 nM (IC50) |
NUAK2 100 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | IC50 |
1.29 μM
Compound: WZ4003
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Antiproliferative activity against mouse BaF3 cells harboring EGFR E746_A750/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay
Antiproliferative activity against mouse BaF3 cells harboring EGFR E746_A750/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay
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[PMID: 20033049] |
| BaF3 | IC50 |
1.9 μM
Compound: WZ4003
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Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M double mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay
Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M double mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay
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[PMID: 20033049] |
WZ4003 (3-10 μM) markedly suppresses NUAK1-mediated MYPT1 phosphorylation, in HEK-293 cells expressing wild-type NUAK1. Moreover, WZ4003 (10 μM) inhibits MYPT1 Ser445 phosphorylation as well as cell migration, invasion and proliferation to a similar extent as knock out in MEFs or knock down in U2OS cells of NUAK1[1]. WZ4003 also exhibits a high, specific affinity to the L858R/T790M mutant EGFR, while a significantly reduced cellular IC50 against T790M containing Ba/F3 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1214265-58-3
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Appearance Solid
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Molecular Weight 496.99
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Formula C25H29ClN6O3
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Color White to off-white
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SMILES
O=C(NC1=CC=CC(OC2=NC(NC3=C(OC)C=C(N4CCN(C)CC4)C=C3)=NC=C2Cl)=C1)CC
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (8)
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Journal Impact Factor
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Most Recent
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Cancer Discov
2018 May;8(5):632-647. PMID: 29500295
WZ4003 purchased from MedChemExpress. Usage Cited in: Cancer Discov. 2018 May;8(5):632-647. [Abstract]
Apoptosis is induced in U2OS cells 48hrs after treatment with 10μM HTH-01-015 or WZ4003.
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Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
Cell Rep
2025 Mar 21;44(4):115456. PMID: 40120107 -
J Cell Biol
YAP and TAZ limit cytoskeletal and focal adhesion maturation to enable persistent cell motility. [Abstract]2019 Apr 1;218(4):1369-1389. PMID: 30737263 -
Cell Biosci
2023 Dec 22;13(1):232. PMID: 38135881 -
Commun Biol
A genome-scale CRISPR Cas9 dropout screen identifies synthetically lethal targets in SRC-3 inhibited cancer cells. [Abstract]2021 Mar 25;4(1):399. PMID: 33767353 -
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Solvent & Solubility
DMSO : 33.33 mg/mL (67.06 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.03 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
In vitro activities of purified GST-NUAK1 and GST-NUAK1[A195T] are measured using Cerenkov counting of incorporation of radioactive 32P from [γ-32P]ATP into Sakamototide substrate peptide. Reactions are carried out in a 50 μL reaction volume for 30 min at 30°C and reactions are terminated by spotting 40 μL of the reaction mix on to P81 paper and immediately immersing in 50 mM orthophosphoric acid. Samples are washed three times in 50 mM orthophosphoric acid followed by a single acetone rinse and air drying. The kinase-mediated incorporation of [γ-32P]ATP into Sakamototide is quantified by Cerenkov counting. One unit of activity is defined as that which catalysed the incorporation of 1 nmol of [32P]phosphate into the substrate over 1 h.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Cell proliferation assays are carried out colorimetrically in 96-well plates. 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 HTH-01-015 or WZ4003.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (273 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Banerjee S, et al. Characterization of WZ4003 and HTH-01-015 as selective inhibitors of the LKB1-tumour-suppressor-activated NUAK kinases. Biochem J. 2014 Jan 1;457(1):215-25. [Content Brief]
[2]. Zhou W, et al. Novel mutant-selective EGFR kinase inhibitors against EGFR T790M. Nature. 2009 Dec 24;462(7276):1070-4 [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0121 mL | 10.0606 mL | 20.1211 mL | 50.3028 mL |
| 5 mM | 0.4024 mL | 2.0121 mL | 4.0242 mL | 10.0606 mL | |
| 10 mM | 0.2012 mL | 1.0061 mL | 2.0121 mL | 5.0303 mL | |
| 15 mM | 0.1341 mL | 0.6707 mL | 1.3414 mL | 3.3535 mL | |
| 20 mM | 0.1006 mL | 0.5030 mL | 1.0061 mL | 2.5151 mL | |
| 25 mM | 0.0805 mL | 0.4024 mL | 0.8048 mL | 2.0121 mL | |
| 30 mM | 0.0671 mL | 0.3354 mL | 0.6707 mL | 1.6768 mL | |
| 40 mM | 0.0503 mL | 0.2515 mL | 0.5030 mL | 1.2576 mL | |
| 50 mM | 0.0402 mL | 0.2012 mL | 0.4024 mL | 1.0061 mL | |
| 60 mM | 0.0335 mL | 0.1677 mL | 0.3354 mL | 0.8384 mL |
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