Home>>Signaling Pathways>> PI3K/Akt/mTOR Signaling>> AMPK>>WZ4003

WZ4003

Catalog No.GC16549

NUAK1/2 inhibitor, potent and selective

Products are for research use only. Not for human use. We do not sell to patients.

WZ4003 Chemical Structure

Cas No.: 1214265-58-3

Size Price Stock Qty
10mM (in 1mL DMSO)
$94.00
In stock
5mg
$86.00
In stock
10mg
$131.00
In stock
50mg
$324.00
In stock

Tel:(909) 407-4943 Email: sales@glpbio.com


Customer Reviews

Based on customer reviews.

  • GlpBio Citations

    GlpBio Citations
  • Bioactive Compounds Premium Provider

    Bioactive Compounds Premium Provider

Sample solution is provided at 25 µL, 10mM.

Description of WZ4003

WZ4003 is a potent and selective inhibitor of NUAK1 and NUAK2 with IC50 values of 20 and 100 nM, respectively [1].

NUAK family SNF1-like kinase-1 (NUAK1) and the related NUAK2 belong to the AMP-activated protein kinase (AMPK) family and are activated by liver kinase B1 (LKB1) tumour suppressor protein kinase [1].

WZ4003 is a potent and selective NUAK1/2 inhibitor. In HEK-293 cells, WZ4003 inhibited the phosphorylation of myosin phosphate-targeting subunit 1 (MYPT1), which was phosphorylated by NUAK1 at Ser445. In HEK-293 cells overexpressing inhibitor-resistant NUAK1[A195T], WZ4003 didn’t inhibit the phosphorylation of MYPT1 at Ser445. In mouse embryonic fibroblasts (MEFs), WZ4003 significantly inhibited migration in a wound-healing assay and inhibited MEFs proliferation. In a cell invasion assay, WZ4003 inhibited the invasive potential of U2OS cells [1]. In U2OS cells, WZ4003 (10 μM) inhibited phosphorylation of MYPT1 and reduced the cells in S-phase by 50%. Also, WZ4003 prevented cells from entering into mitosis [2].

References:
[1].  Banerjee S, Buhrlage SJ, Huang HT, et al. Characterization of WZ4003 and HTH-01-015 as selective inhibitors of the LKB1-tumour-suppressor-activated NUAK kinases. Biochem J, 2014, 457(1): 215-225.
[2].  Banerjee S, Zagórska A, Deak M, et al. Interplay between Polo kinase, LKB1-activated NUAK1 kinase, PP1βMYPT1 phosphatase complex and the SCFβTrCP E3 ubiquitin ligase. Biochem J, 2014, 461(2): 233-245.

Protocol of WZ4003

Kinase experiment [1]:

Kinase assays

In vitro activities of purified GST–NUAK1 were measured using Cerenkov counting of incorporation of radioactive 32P from [γ-32P]ATP into Sakamototide substrate peptide. Reactions were carried out in a 50 μl reaction volume for 30 min at 30°C and reactions were terminated by spotting 40 μl of the reaction mix on to P81 paper and immediately immersing in 50 mM orthophosphoric acid. Samples were 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 was quantified by Cerenkov counting.

Cell experiment [2]:

Cell lines

U2OS cell lines

Preparation method

The solubility of this compound in DMSO is >7.85mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

10 μM for 16h

Applications

WZ4003 impaired the invasive potential of U2OS cells in a 3D cell invasion assay to the same extent as NUAK1 knockdown, which indicates that WZ4003 will serve as useful chemical probes to delineate the biological roles of the NUAK kinases.

References:

[1] Banerjee S, Buhrlage SJ, Huang HT, et al. Characterization of WZ4003 and HTH-01-015 as selective inhibitors of the LKB1-tumour-suppressor-activated NUAK kinases. Biochem J, 2014, 457(1): 215-225.

Chemical Properties of WZ4003

Cas No. 1214265-58-3 SDF
Chemical Name N-[3-[5-chloro-2-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]oxyphenyl]propanamide
Canonical SMILES CCC(=O)NC1=CC(=CC=C1)OC2=NC(=NC=C2Cl)NC3=C(C=C(C=C3)N4CCN(CC4)C)OC
Formula C25H29ClN6O3 M.Wt 496.99
Solubility ≥ 7.85mg/mL in DMSO with gentle warming Storage Store at -20° C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of WZ4003

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.0121 mL 10.0606 mL 20.1211 mL
5 mM 0.4024 mL 2.0121 mL 4.0242 mL
10 mM 0.2012 mL 1.0061 mL 2.0121 mL
  • Molarity Calculator

  • Dilution Calculator

  • Molecular Weight Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
**When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / CoA (available online).

Calculate

In vivo Formulation Calculator (Clear solution) of WZ4003

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

Product Documents

Quality Control & SDS

View current batch:

Reviews

Review for WZ4003

Average Rating: 5 ★★★★★ (Based on Reviews and 34 reference(s) in Google Scholar.)

5 Star
100%
4 Star
0%
3 Star
0%
2 Star
0%
1 Star
0%
Review for WZ4003

GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.

Required fields are marked with *

You may receive emails regarding this submission. Any emails will include the ability to opt-out of future communications.