1313613-09-0

1313613-09-0 structure

Name: AMZ30
Chemical Name: AMZ30
CAS Number: 1313613-09-0
Molecular Formula: C₁₉H₁₂FN₃O₆S₂
Molecular Weight: 461.444
Catalog: Research Areas Others
Create Date: 2018-02-28 19:53:30
Modify Date: 2024-01-22 17:34:13
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].

Name	AMZ30
Synonyms	(2E)-2-[(4-Fluorophenyl)sulfonyl]-3-{1-[(3-nitrophenyl)sulfonyl]-1H-pyrrol-2-yl}acrylonitrile 2-Propenenitrile, 2-[(4-fluorophenyl)sulfonyl]-3-[1-[(3-nitrophenyl)sulfonyl]-1H-pyrrol-2-yl]-, (2E)-

Description	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].
Related Catalog	Signaling Pathways >> Others >> Others Research Areas >> Others
References	[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.