AMZ30 |
| カタログ番号GC30122 |
AMZ30 は、プロテインホスファターゼメチルエステラーゼ-1 の選択的共有結合阻害剤です (PME-1; IC50=600 nM)。 PME-1 を選択的に不活性化し、生細胞の PP2A の脱メチル化型を減少させます。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1313613-09-0
Sample solution is provided at 25 µL, 10mM.
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AMZ30 is a selective, covalent inhibitors of protein phosphatase methylesterase-1(PME-1; IC50=600 nM); selectively inactivates PME-1 and reduces the demethylated form of PP2A in living cells.IC50 value: 600 nM [1]Target: PME-1 inhibitorin vitro: AMZ30 showed substantially improved inhibition of PME-1 (IC50 value of 600 nM) with more than 100-fold selectivity relative to other SHs in human cell lysates. Incubation of HEK 293T cells with a concentration range of AMZ30 generated an in situ IC50 value for PME-1 inhibition of 3.5 μM as determined by gel-based ABPP without any observed cross-reactivity with other SHs even at 100 μM compound. Treatment of HEK 293T cells stably overexpressing PME-1 with 28 (20 μM) caused an ~80% reduction in the levels of demethylated PP2A [1].
[1]. Bachovchin DA, 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.
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