A selective NUAK1 and NUAK2 inhibitor
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WZ4003

Item No. 19177

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[3-[[5-chloro-2-[[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]oxy]phenyl]-propanamide
CAS Number
1214265-58-3
Molecular Formula
C25H29ClN6O3
Formula Weight
497.0
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 14 mg/mlDMF:PBS(pH 7.2)(1:1): 0.5 mg/mlDMSO: 14 mg/ml
λmax
241, 283, 311 nm
SMILES
CN1CCN(C2=CC=C(NC3=NC=C(Cl)C(OC4=CC=CC(NC(CC)=O)=C4)=N3)C(OC)=C2)CC1
InChi Code
InChI=1S/C25H29ClN6O3/c1-4-23(33)28-17-6-5-7-19(14-17)35-24-20(26)16-27-25(30-24)29-21-9-8-18(15-22(21)34-3)32-12-10-31(2)11-13-32/h5-9,14-16H,4,10-13H2,1-3H3,(H,28,33)(H,27,29,30)
InChi Key
SDGJBAUIGHSMRI-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    5 mg

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    10 mg

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    25 mg

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    Product Description

    WZ4003 is a selective inhibitor of NUAK1 and NUAK2 (IC50s = 20 and 100 nM, respectively).1 It does not affect the activity of a panel of 139 other kinases, including additional AMPK family members.1 At 3-10 µM, WZ4003 has been shown to inhibit the phosphorylation of the NUAK1 substrate, myosin phosphate-targeting subunit 1 at Ser445.1 When administered to mouse embryonic fibroblasts in vitro, 10 µM WZ4003 inhibits proliferation and migration in a wound-healing assay.1 It has also been shown to impair the invasive potential of U2OS cells at similar concentrations in a 3D cell invasion assay.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

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