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AMZ30

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Chemical Structure| 1313613-09-0 同义名 : ML136;CS-2122
CAS号 : 1313613-09-0
货号 : A781030
分子式 : C19H12FN3O6S2
纯度 : 99%+
分子量 : 461.443
MDL号 : MFCD28900741
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(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
动物实验配方：
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.
实验方案
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
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.