AMZ 30

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Description: Potent, selective and irreversible protein phosphatase methylesterase-1 (PME-1) inhibitor
Chemical Name: (2E)-2-[(4-Fluorophenyl)sulfonyl]-3-[1-[(3-nitrophenyl)sulfonyl]-1H-pyrrol-2-yl]-2-propenenitrile
Purity: ≥98% (HPLC)

Biological Activity for AMZ 30

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.

Technical Data for AMZ 30

M. Wt 461.45
Formula C19H12FN3O6S2
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1313613-09-0
PubChem ID 44607965
Smiles C(=C(/S(=O)(=O)C1=CC=C(F)C=C1)\C#N)\C=2N(S(=O)(=O)C3=CC(N(=O)=O)=CC=C3)C=CC2

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for AMZ 30

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 46.15 100

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 will affect the solvent volumes required to prepare stock solutions.

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

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References for AMZ 30

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

Elgenaidi et al (2019) Regulation of the phosphoprotein phosphatase 2A system and its modulation during oxidative stress: A potential therapeutic target? Pharmacol.Ther. 198 68 PMID: 30797822

Xia et al (2015) A LCMT1-PME-1 methylation equilibrium controls mitotic spindle size. Cell Cycle 14 1938 PMID: 25839665

Bachovchin et al (2011) Discovery and optimization of sulfonyl acrylonitriles as selective, covalent inhibitors of protein phosphatase methylesterase-1. J.Med.Chem. 54 5229 PMID: 21639134

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Keywords: AMZ 30, AMZ 30 supplier, AMZ30, potent, selective, irreversible, covalent, inhibitor, inhibits, serine, hydrolases, protein, phosphatase, methylesterase-1, PME-1, mitotic, arrest, Other, Hydrolases, Mitosis, 6923, Tocris Bioscience

Citations for AMZ 30

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