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WZ4003

WZ4003

产品编号 T6291   CAS 1214265-58-3

WZ4003 是一种高度特异性 NUAK 激酶的有效抑制剂,能够抑制 NUAK1 和 NUAK2 的活性,IC50值分别为 20 和 100 nM。

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WZ4003 Chemical Structure
WZ4003, CAS 1214265-58-3
规格 价格/CNY 货期 数量
1 mg ¥ 283 现货
5 mg ¥ 668 现货
10 mg ¥ 1,050 现货
25 mg ¥ 1,980 现货
50 mg ¥ 2,990 现货
100 mg ¥ 4,320 现货
200 mg ¥ 6,120 现货
500 mg ¥ 8,900 现货
1 mL * 10 mM (in DMSO) ¥ 792 现货
产品目录号及名称: WZ4003 (T6291)
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 WZ4003, a highly selective NUAK kinase inhibitor, is with IC50 of 20 nM and 100 nM for NUAK1 and NUAK2, respectively. It is no significant inhibition on 139 other kinases.
靶点活性 NUAK2:100 nM, NUAK1:20 nM
体外活性 In HEK-293 cells expressing wild-type NUAK1, WZ4003 (3–10 μM) markedly suppresses NUAK1-mediated MYPT1 phosphorylation. Moreover, WZ4003 (10 μM) inhibits MYPT1 Ser445 phosphorylation as well as cell migration, invasion and proliferation to a similar extent as knock out in MEFs or knock down in U2OS cells of NUAK1. [1] WZ4003 also exhibits a high, specific affinity to the L858R/T790M mutant EGFR, while a significantly reduced cellular IC50 against T790M containing Ba/F3 cells. [2]
激酶实验 IC50 determination: Active GST–NUAK1, GST–NUAK1[A195T] and GST–NUAK2 enzymes are purified using glutathione–Sepharose from HEK-293 cell lysates 36–48 h following the transient transfection of pEBG2T mammalian constructs expressing N-terminal GSTtagged NUAK1, NUAK1[A195T] or NUAK2. For peptide kinase assays, 96-well plates are used, and each reaction is performed in triplicate. Each reaction is set up in a total volume of 50 μL containing 100 ng of NUAK1 (wild-type or A195T mutant) or NUAK2 in 50 mM Tris/HCl (pH 7.5), 0.1 mM EGTA, 10 mM magnesium acetate, 200 μM Sakamototide, 0.1 mM [γ -32P]ATP (450–500 c.p.m./pmol) and the indicated concentrations of inhibitors dissolved in DMSO. After incubation for 30 min at 30°C, reactions are terminated by adding 25 mM (final) EDTA to chelate the magnesium. Then, 40 μL of the reaction mix is spotted on to P81 paper and immersed in 50 mM orthophosphoric acid. Samples are washed three times in 50 mM orthophosphoric acid followed by a single acetone rinse and air drying. The incorporation of [γ -32P]ATP into Sakamototide is quantified by Cerenkov counting. The values are expressed as a percentage of the DMSO control. IC50 curves are developed and IC50 values are calculated using GraphPad Prism software.
细胞实验 Cell proliferation assays are carried out colorimetrically in 96-well plates using the CellTiter 96 AQueous Non-Radioactive Cell Proliferation Assay kit following the manufacturer's protocol. Initially, 2000 cells per well are seeded for U2OS cells and 3000 cells per well are seeded for MEFs. The proliferation assays are carried out over 5 days in the presence or absence of 10 μM WZ4003.(Only for Reference)
分子量 496.99
分子式 C25H29ClN6O3
CAS No. 1214265-58-3

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 7 mg/mL (14.08 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0121 mL 10.0606 mL 20.1211 mL 50.3028 mL
5 mM 0.4024 mL 2.0121 mL 4.0242 mL 10.0606 mL
10 mM 0.2012 mL 1.0061 mL 2.0121 mL 5.0303 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Banerjee S, et al. Biochem J. 2014, 457(1), 215-225. 2. Zhou W, et al. Nature. 2009, 462(7276), 1070-1074.
1-HEXACOSANOL YLF-466D 4-Hydroxycinnamamide Mogroside V Ginkgolide K Danthron Ligupurpuroside A Metformin hydrochloride

相关化合物库

该产品包含在如下化合物库中:
抑制剂库 抗高血压化合物库 脂代谢化合物库 自噬库 抗前列腺癌化合物库 抗结直肠癌化合物库 抗癌化合物库 激酶抑制剂库 糖代谢化合物库 氧化还原化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
% Tween 80
% ddH2O
计算 重置

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

WZ4003 1214265-58-3 Chromatin/Epigenetic PI3K/Akt/mTOR signaling AMPK inhibit AMP-activated protein kinase WZ 4003 WZ-4003 Inhibitor inhibitor

 

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