UPF 1069, a derivative of isoquinolinone, is a potent and selective inhibitor of poly-(ADP-ribose) polymerase 2 (PARP-2) 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 . 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.

5-phenacyloxy-2H-isoquinolin-1-one

≥98% by HPLC

UPF 1069 is a selective inhibitor of PARP2 with IC50 of 0.3 µM. It is ~27-fold selective for PARP2 vs. PARP1 (IC50 = 8 µM).

Soluble in DMSO

Store at or below –20°C. Solid form is stable at least 12 months from date of receipt, when stored as directed. Do not store aqueous solutions for more than one day.

Moroni F, et al. Br J Pharmacol. 2009;157(5):854-862

PARP Inhibitor

Inhibitor