1214265-58-3

Basic information

• Product Name: WZ4003
• Synonyms: WZ4003;N-[3-[[5-Chloro-2-[[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]oxy]phenyl]propanamide;Propanamide, N-[3-[[5-chloro-2-[[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]oxy]phenyl]-;N-(3-((5-chloro-2-((2-methoxy-4-(4-methylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)oxy)phenyl)propionamide;N-[3-[5-chloro-2-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]oxyphenyl]propanamide
• CAS NO: 1214265-58-3
• Molecular Formula: C25H29ClN6O3
• Molecular Weight: 496.98916
• Product Categories: Inhibitors
• Mol File: 1214265-58-3.mol
• Article Data: 0

Chemical Properties

• Appearance: /
• 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)
• CAS DataBase Reference: WZ4003(CAS DataBase Reference)
• NIST Chemistry Reference: WZ4003(1214265-58-3)
• EPA Substance Registry System: WZ4003(1214265-58-3)

Safety Data

• Hazardous Substances Data: 1214265-58-3(Hazardous Substances Data)

Usage

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.

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.