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ABL127

Catalog No. T14084 CAS 1073529-41-5

ABL127 is a selective and covalent inhibitor of protein methylesterase 1 (PME-1). In HEK293T and MDA-MB-231 cells, the IC50s values are 6.4 nM and 4.2 nM , respectively.

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ABL127, CAS 1073529-41-5

Pack Size	Availability	Price/USD	Quantity
1 mg	35 days	$ 93.00
5 mg	35 days	$ 335.00

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Biological Description

Chemical Properties

Storage & Solubility Information

Description	ABL127 is a selective and covalent inhibitor of protein methylesterase 1 (PME-1). In HEK293T and MDA-MB-231 cells, the IC50s values are 6.4 nM and 4.2 nM , respectively.
Targets&IC50	PME-1 (HEK293T):6.4 nM, PME-1 (MDA-MB-231):4.2 nM
In vitro	In this study, three PME-1 inhibitor compounds were analyzed, demonstrating that ABL127, at concentrations of 100 μM, induces a thermal shift. Lower concentrations of ABL127 (25 or 50 μM) similarly affect protein melting temperature. The application of ABL127 and AMZ-30 on Ishikawa cells notably reduced cell proliferation, an effect comparable to PME-1 suppression via shRNA. Furthermore, treating ECC-1 cells with ABL127 or AMZ-30 impacted cell invasion in a dose-responsive manner. Specifically, ABL127 treatment on EC cells enhanced protein phosphatase 2A (PP2A) activity by approximately 45%, whereas AMZ-30 treatment resulted in a modest increase of around 10% in PP2A activity[1].
In vivo	In these preliminary studies, no substantial reduction in tumor size was observed[1]. Moreover, gel analysis suggests that ABL127 deactivates the brain's PME-1 enzyme. However, due to the presence of similar serine hydrolase activities, accurately determining the degree of inactivation is challenging[2].

Molecular Weight	332.35
Formula	C17H20N2O5
CAS No.	1073529-41-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Pusey M, et al. Inhibition of protein methylesterase 1 decreased cancerous phenotypes in endometrial adenocarcinoma cell lines and xenograft tumor models. Tumour Biol. 2016 Sep;37(9):11835-11842. 2. Bachovchin DA, et al. Academic cross-fertilization by public screening yields a remarkable class of protein phosphatase methylesterase-1 inhibitors. Proc Natl Acad Sci U S A. 2011 Apr 26;108(17):6811-6.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

ABL127 1073529-41-5 Others ABL-127 ABL 127 inhibitor inhibit

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