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AMZ30 is a selective, covalent inhibitors of protein phosphatase methylesterase-1(PME-1; IC50=600 nM); selectively inactivates PME-1 and reduces the demethylated form of PP2A in living cells. IC50 value: 600 nM Target: PME-1 inhibitor in vitro: AMZ30 showed substantially improved inhibition of PME-1 (IC50 value of 600 nM) with more than 100-fold selectivity relative to other SHs in human cell lysates. Incubation of HEK 293T cells with a concentration range of AMZ30 generated an in situ IC50 value for PME-1 inhibition of 3.5 μM as determined by gel-based ABPP without any observed cross-reactivity with other SHs even at 100 μM compound. Treatment of HEK 293T cells stably overexpressing PME-1 with 28 (20 μM) caused an ~80% reduction in the levels of demethylated PP2A.
| Molecular Weight | 461.44 |
| CAS Number | 1313613-09-0 |
| Solubility (25°C) | DMSO 90 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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