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CAS No.: 1313613-09-0

AMZ30 Catalog No. CSN17683

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.

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400-920-2911

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靶点选择性

生物活性

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技术信息

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.
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.

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
- 2.1671 mL
- 10.8356 mL
- 21.6711 mL
- 5 mM
- 0.4334 mL
- 2.1671 mL
- 4.3342 mL
- 10 mM
- 0.2167 mL
- 1.0836 mL
- 2.1671 mL

技术信息

CAS号

1313613-09-0

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H12FN3O6S2

运输

蓝冰

分子量

461.44

别名

溶解度

DMSO	86.0 mg/mL (186.4 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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