|N-(3-((5-氯-2-((2-甲氧基-4-(4-甲基哌嗪-1-基)苯基)氨基)嘧啶-4-基)氧基)苯基)丙酰胺|CsnPharm

CAS No.: 1214265-58-3

WZ4003 Catalog No. CSN17571

Synonyms: WZ4003

WZ4003 is a potent and selective NUAK1/2 inhibitor with IC50 values of 20 and 100 nM, respectively.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 NUAK2

IC50:100nM NUAK1

IC50:20nM
描述NUAK family SNF1-like kinase-1 (NUAK1) and NUAK2 are the members of the AMPK family that play important roles in regulating essential cellular events, such as cell invasion, proliferation, embryonic development and axon branching. WZ4003 is an inhibitor of both NUAK isoforms with IC50 values of 20 nM and 100 nM for NUAK1 and NUAK2, respectively. In HEK-293 cells, EDTA-induced phosphorylation of MYPT1 at Ser⁴⁴⁵ was suppressed by WZ4003 (0.3 - 10 mM) in a dose-dependent manner. In HEK-293 cells expressing drug-resistant NUAK1[A195T], WZ4003 at 30 μM failed to block the phosphorylation of MYPT1. However, WZ4003 at 3 - 10 μM effectively suppressed MYPT1 Ser⁴⁴⁵ phosphorylation. Treatment with 10 μM WZ4003 remarkably reduced cell migration in wild-type mouse embryonic fibroblasts (MEFs). In both U2OS cells and MEFs, WZ4003 at 10 μM suppressed cell proliferation and MYPT1 phosphorylation to the same level as shown in NUAK1 knockout cells. The invasion potential of U2OS cells was also inhibited by 10 μM WZ4003^[3]. In the Ba/F3 cell line, the IC₅₀ values of WZ4003 against L858R/T790M mutant and T790M mutant were 1.90 mM and 1.29 mM, respectively^[4].
参考文献

[1] Banerjee S, Buhrlage SJ, et al. Characterization of WZ4003 and HTH-01-015 as selective inhibitors of the LKB1-tumour-suppressor-activated NUAK kinases. Biochem J. 2014 Jan 1;457(1):215-25.
[2] Zhou W, Ercan D, et al. Novel mutant-selective EGFR kinase inhibitors against EGFR T790M. Nature. 2009 Dec 24;462(7276):1070-4.
[3] Banerjee S, Buhrlage SJ, Huang HT, Deng X, Zhou W, Wang J, Traynor R, Prescott AR, Alessi DR, Gray NS. Characterization of WZ4003 and HTH-01-015 as selective inhibitors of the LKB1-tumour-suppressor-activated NUAK kinases. Biochem J. 2014 Jan 1;457(1):215-25. doi: 10.1042/BJ20131152. PMID: 24171924; PMCID: PMC3969223.
[4] Zhou W, Ercan D, Chen L, Yun CH, Li D, Capelletti M, Cortot AB, Chirieac L, Iacob RE, Padera R, Engen JR, Wong KK, Eck MJ, Gray NS, Jänne PA. Novel mutant-selective EGFR kinase inhibitors against EGFR T790M. Nature. 2009 Dec 24;462(7276):1070-4. doi: 10.1038/nature08622. PMID: 20033049; PMCID: PMC2879581.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.0121 mL
- 10.0606 mL
- 20.1212 mL
- 5 mM
- 0.4024 mL
- 2.0121 mL
- 4.0242 mL
- 10 mM
- 0.2012 mL
- 1.0061 mL
- 2.0121 mL

技术信息

CAS号

1214265-58-3

储存条件

粉末: Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C25H29ClN6O3

运输

蓝冰

分子量

496.99

别名

WZ4003

溶解度

DMSO	7.0 mg/mL (14.1 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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靶点	Description	IC50
NUAK2		IC50:100nM
NUAK1		IC50:20nM

WZ4003 Catalog No. CSN17571

靶点选择性

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