WZ4003
Synonym(s):N-[3-[[5-Chloro-2-[[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]oxy]phenyl]-propanamide
- CAS NO.:1214265-58-3
- Empirical Formula: C25H29ClN6O3
- Molecular Weight: 496.99
- MDL number: MFCD28015100
- SAFETY DATA SHEET (SDS)
- Update Date: 2023-06-30 15:45:59
What is WZ4003?
The Uses of WZ4003
WZ4003 is a highly specific protein kinase inhibitor of NUAK kinases.
Biological Activity
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].
Biochem/physiol Actions
WZ4003 helps to repress the migration of cells. It also prevents cell proliferation.
storage
Store at -20°C
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.
Properties of WZ4003
Density | 1.303±0.06 g/cm3(Predicted) |
storage temp. | -20°C |
solubility | insoluble in H2O; ≥2.68 mg/mL in EtOH with gentle warming and ultrasonic; ≥7.85 mg/mL in DMSO with gentle warming |
pka | 14.27±0.70(Predicted) |
form | powder |
color | white to beige |
Safety information for WZ4003
Signal word | Warning |
Pictogram(s) |
Exclamation Mark Irritant GHS07 |
GHS Hazard Statements |
H302:Acute toxicity,oral |
Computed Descriptors for WZ4003
New Products
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