AMZ30

1313613-09-0

C19H12FN3O6S2

H2O : < 0.1 mg/mL (insoluble); DMSO : 4.8 mg/mL (10.40 mM; Need ultrasonic and warming)

Others

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 [1] 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 uM as determined by gel-based ABPP without any observed cross-reactivity with other SHs even at 100 uM compound. Treatment of HEK 293T cells stably overexpressing PME-1 with 28 (20 uM) caused an ca.80% reduction in the levels of demethylated PP2A [1].