1. Epigenetics
    PI3K/Akt/mTOR
  2. AMPK

WZ4003 

Cat. No.: HY-15802 Purity: 97.26%
Data Sheet SDS Handling Instructions

WZ4003 is the first potent and highly specific NUAK kinase inhibitor with IC50 of 20 nM/100 nM for NUAK1/NUAK2, without significant inhibition on other 139 kinases.

For research use only. We do not sell to patients.
WZ4003 Chemical Structure

WZ4003 Chemical Structure

CAS No. : 1214265-58-3

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 103 In-stock
5 mg USD 94 In-stock
50 mg USD 547 In-stock
100 mg   Get quote  
200 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

WZ4003 is the first potent and highly specific NUAK kinase inhibitor with IC50 of 20 nM/100 nM for NUAK1/NUAK2, without significant inhibition on other 139 kinases.

IC50 & Target

IC50: 20 nM (NUAK1), 100 nM (NUAK2)

In Vitro

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].

References
Preparing Stock Solutions
Concentration Volume Mass 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
Please refer to the solubility information to select the appropriate solvent.
Kinase Assay
[1]

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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

496.99

Formula

C₂₅H₂₉ClN₆O₃

CAS No.

1214265-58-3

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: 24.5 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
WZ4003
Cat. No.:
HY-15802
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