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.
MedKoo Cat#: 466264
Name: AMZ 30
CAS#: 1313613-09-0
Chemical Formula: C19H12FN3O6S2
Exact Mass: 461.0152
Molecular Weight: 461.44
Elemental Analysis: C, 49.46; H, 2.62; F, 4.12; N, 9.11; O, 20.80; S, 13.90
Solvent | mg/mL | mM | comments | |
---|---|---|---|---|
Solubility | ||||
DMSO | 46.2 | 100.00 |
The following data is based on the product molecular weight 461.44 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.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |