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WZ4003

Item № 19177
CAS № 1214265-58-3
Purity ≥98%
product image
                (CAS 1214265-58-3)
SIZE PRICE QUANTITY SUBTOTAL
CART TOTAL
     1 mg $25.00 0.00
     5 mg $81.00 0.00
     10 mg $150.00 0.00
     25 mg $313.00 0.00

Pricing updated 2019-05-26. Prices are subject to change without notice.

Description

NUAK1 (also known as AMPK-related kinase 5) and NUAK2 (also known as SNF1/AMPK-related kinase) are members of the AMP-activated protein kinase (AMPK) family of protein kinases that are activated by the liver kinase B1 tumor suppressor kinase. NUAK kinases are thought to have roles in regulating cell adhesion, cancer cell invasion, embryonic development, senescence, proliferation, neuronal polarity, and axon branching. 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

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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
A crystalline solid
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

Warning - this product is not for human or veterinary use.

Shipping & Storage
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Stability
≥ 2 years
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Additional Information

View the Cayman Structure Database for chemical structure definitions for many Cayman products

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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 Biochemistry Journal 457(1), 215-225 (2014).

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