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AMZ30 {[allProObj[0].p_purity_real_show]}

货号:A781030 同义名: ML136;CS-2122

AMZ30 is a selective, covalent inhibitors of protein phosphatase methylesterase-1 (PME-1; IC50=600 nM), and selectively inactivates PME-1 and reduces the demethylated form of PP2A in living cells.

AMZ30 化学结构 CAS号:1313613-09-0
AMZ30 化学结构
CAS号:1313613-09-0
AMZ30 3D分子结构
CAS号:1313613-09-0
AMZ30 化学结构 CAS号:1313613-09-0
AMZ30 3D分子结构 CAS号:1313613-09-0
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AMZ30 纯度/质量文件 产品仅供科研

货号:A781030 标准纯度: {[allProObj[0].p_purity_real_show]}
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AMZ30 生物活性

描述 The serine hydrolase protein PME-1 (phosphatase methylesterase-1) regulates the methylesterification state of PP2A and has been implicated in cancer and Alzheimer’s disease. AMZ30 is a selective PME-1 inhibitor with IC50 value of 0.6μM in vitro. AMZ30 inhibited cellular PME-1 activity with IC50 value of 3.5μM and significantly reduced demethylation level and increased methylation level of PP2A, which is regulated by PME-1, at concentration of 20μM post 1h in HEK 293T cells stably overexpressing PME-1. Inhibition of PME-1 by AMZ30 at concentration of 20μM led to short mitotic spindles, an increase in the percentage of HeLa cells arrested in mitosis, an increase in the percentage of mitotic cells with spindle defects, an increase in the percentage of cells with unaligned chromosomes, a reduced PTP distance, a reduced spindle width, a reduced spindle volume and a decrease in the amount of microtubule polymer. Also it decreased cell viability and increased the time of cells spent in mitosis.

AMZ30 参考文献

[1]Bachovchin DA, Zuhl AM, et al. Discovery and optimization of sulfonyl acrylonitriles as selective, covalent inhibitors of protein phosphatase methylesterase-1. J Med Chem. 2011 Jul 28;54(14):5229-36.

[2]Xia X, Gholkar A, et al. A LCMT1-PME-1 methylation equilibrium controls mitotic spindle size. Cell Cycle. 2015;14(12):1938-47.

AMZ30 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.17mL

0.43mL

0.22mL

10.84mL

2.17mL

1.08mL

21.67mL

4.33mL

2.17mL

AMZ30 技术信息

CAS号1313613-09-0
分子式C19H12FN3O6S2
分子量 461.443
别名 ML136;CS-2122
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C

溶解度

DMSO: 105 mg/mL(227.55 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

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