AZ3146 | Kinesin | Mps1 | AmBeed-信号通路专用抑制剂

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AZ3146 {[allProObj[0].p_purity_real_show]}

货号：A174095

AZ3146 is a selective and potent Mps1 inhibitor with IC50 value of 35 nM.

AZ3146 化学结构
CAS号：1124329-14-1

AZ3146 3D分子结构
CAS号：1124329-14-1

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AZ3146 纯度/质量文件产品仅供科研

货号：A174095 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • JACS Au, 2024. Ambeed. [ A148168 ]; • JMC, 2024. Ambeed. [ A187643 ]; • JMC, 2024. Ambeed. [ A341145 , A633512 , A607865 , A167774 ]; • Biomacromolecules, 2024. Ambeed. [ A110759 ]; • Biomacromolecules, 2024. Ambeed. [ A203543 ]; 更多 >

驱动蛋白亚型比较

产品名称	Kinesin ↓ ↑	纯度
SB-743921 HCl	++++ KSP (P388 cells), IC50: 14.4 nM KSP, Ki: 0.07 nM	{[allProObj[0].p_purity_real_show]}
GSK-923295	++ CENP-E, Ki: 3.2 nM	{[allProObj[0].p_purity_real_show]}
Ispinesib	+++ KSP (HsEg5), Ki app: 1.7 nM	{[allProObj[0].p_purity_real_show]}
AZ3146	+ Mps1, IC50: ~35 nM	{[allProObj[0].p_purity_real_show]}
MPI-0479605	++ Mps1, IC50: 1.8 nM	{[allProObj[0].p_purity_real_show]}
BAY1217389	+++ Mps1, IC50: 0.63 nM	{[allProObj[0].p_purity_real_show]}
ARQ 621	✔	{[allProObj[0].p_purity_real_show]}
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

AZ3146 生物活性

靶点	Kinesin Mps1, IC50:~35 nM
描述	Monopolar spindle 1 (Mps1) is a spindle assembly checkpoint kinase that plays an essential role in the regulation of mitosis. AZ3146 inhibits human Mps1 with an IC50 value of 35 nM. In nocodazole-arrested Hela cells, AZ3146 at 1 – 30 μM inhibited the autophosphorylation of full-length Mps1. AZ3146 at 2 µM reduced the time for Hela cells to complete mitosis from 90 min to 32 min. Nearly 90% of AZ3146-treated Hela cells underwent abnormal mitoses with around 50% entering anaphase without aligning all the chromosomes and almost 30% exiting mitosis without chromosome segregation. AZ3146 at 2 µM also decreased the levels of Mad1 and Mad2 to 60% and 15%, respectively. The kinetochore recruitment of O-Mad2 in Hela cells was also blocked by at 2 µM AZ3146^[3]. The exposure of GSK923295, an inhibitor targeting the mitotic kinesin Cenp-E, combined with 2 µM AZ3146 induced whole chromosome aneuploidies in cells without causing DNA damage and significant disruption to the spindle^[4]. In AZ3146-resistent HCT116 cells created by long-term exposure of AZ3146, 24-hour incubation of 1 and 2 µM AZ3146 abolished the G₁ and G₂ - M peaks in the parental cell line and made them rapidly exit from mitosis^[5].
作用机制	AZ3146 might inhibit Mps1 by promoting its kinetochore localization^[3].

AZ3146 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
human HCT116 cells		Function assay		Inhibition of Myc-tagged wild type MPS1 autophosphorylation in human HCT116 cells after 2 hrs in presence of proteosome inhibitor MG132, IC50=0.72 μM	24256217
human HCT116 cells		Growth inhibition assay	72 h	Growth inhibition in human HCT116 cells after 72 hrs by MTT assay, GI50=1.2 μM	24256217
sf9 insect cells		Function assay		Inhibition of N-terminal 6XHis-tagged/GST-tagged full length human MPS1 expressed in recombinant baculovirus infected sf9 insect cells using 5FAM-DHTGFLTEYVATRCONH2 as substrate after 60 to 90 mins by fluorescence assay, IC50=7 nM	24256217

AZ3146 动物研究

Dose	Mice: 50 mg/kg^[3] (i.p.)
Administration	i.p.

AZ3146 参考文献

[1]Liu X, Liao W, et al. TTK activates Akt and promotes proliferation and migration of hepatocellular carcinoma cells. Oncotarget. 2015 Oct 27;6(33):34309-20.

[2]Hewitt L, Tighe A, et al. Sustained Mps1 activity is required in mitosis to recruit O-Mad2 to the Mad1-C-Mad2 core complex. J Cell Biol. 2010 Jul 12;190(1):25-34.

[3]Hewitt L, Tighe A, Santaguida S, White AM, Jones CD, Musacchio A, Green S, Taylor SS. Sustained Mps1 activity is required in mitosis to recruit O-Mad2 to the Mad1-C-Mad2 core complex. J Cell Biol. 2010 Jul 12;190(1):25-34.

[4]Bennett A, Bechi B, Tighe A, Thompson S, Procter DJ, Taylor SS. Cenp-E inhibitor GSK923295: Novel synthetic route and use as a tool to generate aneuploidy. Oncotarget. 2015 Aug 28;6(25):20921-32.

[5]Gurden MD, Westwood IM, Faisal A, Naud S, Cheung KM, McAndrew C, Wood A, Schmitt J, Boxall K, Mak G, Workman P, Burke R, Hoelder S, Blagg J, Van Montfort RL, Linardopoulos S. Naturally Occurring Mutations in the MPS1 Gene Predispose Cells to Kinase Inhibitor Drug Resistance. Cancer Res. 2015 Aug 15;75(16):3340-54.

AZ3146 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.21mL

0.44mL

0.22mL

11.05mL

2.21mL

1.10mL

22.10mL

4.42mL

2.21mL

AZ3146 技术信息

CAS号	1124329-14-1
分子式	C₂₄H₃₂N₆O₃
分子量	452.549

别名
运输	蓝冰

存储条件

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 105 mg/mL(232.02 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验配方

AZ3146 {[allProObj[0].p_purity_real_show]}

AZ3146 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

AZ3146 质控信息

AZ3146 生物活性

AZ3146 细胞研究

AZ3146 动物研究

AZ3146 参考文献

AZ3146 实验方案

AZ3146 技术信息

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AZ3146 {[allProObj[0].p_purity_real_show]}

AZ3146 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

AZ3146 质控信息

AZ3146 生物活性

AZ3146 细胞研究

AZ3146 动物研究

AZ3146 参考文献

AZ3146 实验方案

AZ3146 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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AZ3146 纯度/质量文件产品仅供科研