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Merck
CN

SML1445

Sigma-Aldrich

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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About This Item

经验公式(希尔记法):
C25H29ClN6O3
分子量:
496.99
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77

质量水平

检测方案

≥98% (HPLC)

形式

powder

颜色

white to beige

溶解性

DMSO: 5 mg/mL, clear (warmed)

储存温度

−20°C

SMILES字符串

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

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

生化/生理作用

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.

其他说明

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.

象形图

Exclamation mark

警示用语:

Warning

危险声明

危险分类

Acute Tox. 4 Oral

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

法规信息

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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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