AMZ30

Modify Date: 2024-01-22 17:34:13

AMZ30 Structure
AMZ30 structure
Common Name AMZ30
CAS Number 1313613-09-0 Molecular Weight 461.444
Density 1.5±0.1 g/cm3 Boiling Point 724.3±70.0 °C at 760 mmHg
Molecular Formula C19H12FN3O6S2 Melting Point N/A
MSDS N/A Flash Point 391.9±35.7 °C

 Use of AMZ30


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].

 Names

Name AMZ30
Synonym More Synonyms

 AMZ30 Biological Activity

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
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.

 Chemical & Physical Properties

Density 1.5±0.1 g/cm3
Boiling Point 724.3±70.0 °C at 760 mmHg
Molecular Formula C19H12FN3O6S2
Molecular Weight 461.444
Flash Point 391.9±35.7 °C
Exact Mass 461.015167
LogP 3.58
Vapour Pressure 0.0±2.3 mmHg at 25°C
Index of Refraction 1.655
Storage condition 2-8℃

 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)-