6-[4-(diethylamino)-3-nitrophenyl]-5-methyl-2,3,4,5-tetrahydropyridazin-3-one

Uses

DNMDP, a phosphodiesterase 3A (PDE3A) inhibitor, is a potent and selective cancer cell cytotoxic agent. DNMDP binding to PDE3A promotes an interaction between PDE3A and Schlafen 12 (SLFN12). DNMDP shows clear cell-selective cytotoxicity[1].

Biological Activity

DNMDP, a phosphodiesterase 3A (PDE3A) inhibitor, is a potent and selective cancer cell cytotoxic agent. DNMDP binding to PDE3A promotes an interaction between PDE3A and Schlafen 12 (SLFN12). DNMDP shows clear cell-selective cytotoxicity[1]. DNMDP (0-1000 μM; 48 hours) shows clear cell-selective cytotoxicity[1]. HeLa cells undergo apoptosis upon DNMDP treatment, indicates by caspase activity detected by a caspase-sensitive luciferase assay and by poly ADP ribose polymerase (PARP) cleavage. At a concentration of 100 nM, DNMDP specifically inhibits both PDE3A and PDE3B, weakly inhibits PDE10, and had little or no detectable effect on other phosphodiesterases[1].

IC 50

PDE3

References

[1]. de Waal L, et al. Identification of cancer-cytotoxic modulators of PDE3A by predictive chemogenomics. Nat Chem Biol. 2016 Feb;12(2):102-8.