Potent, selective and irreversible protein phosphatase methylesterase-1 (PME-1) inhibitor
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.
| Marque | Tocris Bioscience |
|---|---|
| Réf. B-LABO | BL-RE-158162 |
| Réf. fabricant | 18778606 |
| Nom chimique ou matériau | (2 E)-2-[(4-Fluorophenyl)sulfonyl]-3-[1-[(3-nitrophenyl)sulfonyl]-1 H-pyrrol-2-yl]-2-propenenitrile |
| CAS | 1313613-09-0 |
| Quantité | 10 mg |
| Cible | Hydrolase Inhibitors |
| Formule moléculaire | C<sub>19</sub>H<sub>12</sub>FN<sub>3</sub>O<sub>6</sub>S<sub>2</sub> |
| Pureté | 0.98 |
