Results for Activators & Inhibitors ( 70848 )
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.
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.
DBeQ is cell permeable, potent, selective and reversible inhibitor of the AAA-ATPase p97 (ATPase associated with diverse cellular activities). Ki=3.2 µM. DBeQ blocks both ubiquitin dependent and endoplasmic reticulum-associated degradation pathways, protein clearance pathways, and activates caspases -3 and -7 inducing apoptosis.
P22077 is a cell permeable inhibitor of the ubiquitin-specific protease USP7 (IC50=8.6 µM), and the closely related deubiquitinase (DUB) USP47. P22077 showed weak or no inhibition (EC50 >50µM) towards a panel of 14 isopeptidases and other proteases. Treatment of cells with P22077 (20-40 µM) causes an accumulation of K48-linked ubiquitinated species, and down regulation of the USP7 targets HDM2 and claspin.