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Merck
CN

SML1445

WZ4003

≥98% (HPLC)

别名:

N-[3-[[5-Chloro-2-[[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]oxy]phenyl]-propanamide

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关于此项目

经验公式(希尔记法):
C25H29ClN6O3
化学文摘社编号:
分子量:
496.99
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
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产品名称

WZ4003, ≥98% (HPLC)

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)

SMILES string

ClC1=CN=C(NC2=C(OC)C=C(N3CCN(C)CC3)C=C2)N=C1OC4=CC(NC(CC)=O)=CC=C4

InChI key

SDGJBAUIGHSMRI-UHFFFAOYSA-N

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 5 mg/mL, clear (warmed)

storage temp.

−20°C

Quality Level

Biochem/physiol Actions

Selective inhibitor of NUAK1 and NUAK2 kinases with an IC50 of 20 nM for NUAK1 and an IC50 of 100 nM for NUAK2
WZ4003 helps to repress the migration of cells. It also prevents cell proliferation.
WZ4003 is a potent and selective inhibitor of NUAK1 and NUAK2 kinases, members of the AMPK family that are that are activated by the LKB1 (liver kinase B1) tumour suppressor kinase and involved in development and proliferation. WZ4003 has an IC50 of 20 nM for NUAK1 and an IC50 of 100 nM for NUAK2 without significant inhibition of 139 other kinases tested, including ten AMPK-related kinase family members. Treatment with WZ4003 was found to suppress proliferation, restricting cells from entering into mitosis.

Other Notes

WZ4003 has been expertly reviewed and recommended by the Chemical Probes Portal. For more information, please visit the WZ4003 probe summary on the Chemical Probes Portal website.

pictograms

Exclamation mark

signalword

Warning

hcodes

Hazard Classifications

Acute Tox. 4 Oral

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

法规信息

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分析证书(COA)

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Sourav Banerjee et al.
The Biochemical journal, 457(1), 215-225 (2013-11-01)
The related NUAK1 and NUAK2 are members of the AMPK (AMP-activated protein kinase) family of protein kinases that are activated by the LKB1 (liver kinase B1) tumour suppressor kinase. Recent work suggests they play important roles in regulating key biological
Martin Golkowski et al.
Cell systems, 11(2), 196-207 (2020-08-07)
Hepatocellular carcinoma (HCC) is a complex and deadly disease lacking druggable genetic mutations. The limited efficacy of systemic treatments for advanced HCC implies that predictive biomarkers and drug targets are urgently needed. Most HCC drugs target protein kinases, indicating that

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