| Identification | Back Directory | [Name]
WZ4003 | [CAS]
1214265-58-3 | [Synonyms]
WZ4003
CS-1174
WZ 4003;WZ4003
N-[3-[5-chloro-2-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]oxyphenyl]propanamide
N-[3-[[5-Chloro-2-[[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]oxy]phenyl]propanamide
N-(3-((5-chloro-2-((2-methoxy-4-(4-methylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)oxy)phenyl)propionamide
Propanamide, N-[3-[[5-chloro-2-[[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]oxy]phenyl]- | [Molecular Formula]
C25H29ClN6O3 | [MDL Number]
MFCD28015100 | [MOL File]
1214265-58-3.mol | [Molecular Weight]
496.989 |
| Chemical Properties | Back Directory | [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 | [form ]
powder | [pka]
14.27±0.70(Predicted) | [color ]
white to beige |
| Hazard Information | Back Directory | [Uses]
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. |
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