AMZ 30

Product Description

AMZ 30 is a potent, selective and irreversible inhibitor of protein phosphatase methylesterase-1 (PME-1; IC₅₀ = 600 nM) with > 100-fold selectivity for PME-1 over other serine hydrolases in human cell lysates. AMZ 30 inactivates PME-1 and reduces the demethylated form of serine/threonine protein phosphatase 2A (PP2A) in HEK 293T cells. AMZ 30 perturbs leucine carboxyl methyltransferase-1 (LCMT1)-PME-1 methylation equilibrium leading to shortening of mitotic spindles and mitotic arrest in HeLa cells. It also shows antiproliferative properties in an in vitro model of endometrial carcinoma.

Solubility

Preparing Stock Solutions for AMZ 30

The following data is based on the product molecular weight 461.45

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.17 mL	10.84 mL	21.67 mL
5 mM	0.43 mL	2.17 mL	4.33 mL
10 mM	0.22 mL	1.08 mL	2.17 mL
50 mM	0.04 mL	0.22 mL	0.43 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• Xia A LCMT1-PME-1 methylation equilibrium controls mitotic spindle size. Cell Cycle 2015 PMID: 25839665
• Bachovchin Discovery and optimization of sulfonyl acrylonitriles as selective, covalent inhibitors of protein phosphatase methylesterase-1. J.Med.Chem. 2011 PMID: 21639134
• Elgenaidi Regulation of the phosphoprotein phosphatase 2A system and its modulation during oxidative stress: A potential therapeutic target? Pharmacol.Ther. 2019 PMID: 30797822