Background:

UPF 1069, a derivative of isoquinolinone, is a potent and selective inhibitor of poly-(ADP-ribose) polymerase 2 (PARP-2), with the value of 50% inhibition concentration IC₅₀of 0.3 μmol/L, that is capable of reducing PAR formation both in recombinant enzyme preparations and in nuclear extracts from PARP^-1-/-fibroblasts. Although its inhibition towards PARP-2 is most selective among other PARP-2 inhibitors, UPF 1069 also inhibits PARP-1 with a lesser potency (the value of IC₅₀of 8 μmol/L). Having been used to investigate the role of PARP-1 and PARP-2 in post-ischaemic brain damage, UPF 1069 enhances oxygen-glucose deprivation (OGD) injury in hippocampal slices.

Reference

?[1].Moroni F, Formentini L, Gerace E, Camaioni E, Pellegrini-Giampietro DE, Chiarugi A, Pellicciari R. Selective PARP-2 inhibitors increase apoptosis in hippocampal slices but protect cortical cells in models of post-ischaemic brain damage. Br J Pharmacol. 2009;157(5):854-862