Activators & Inhibitors

Tenovin-6 is the water soluble analog of Tenovin-1 and acts as a potent SIRT1 and SIRT2 inhibitor as well as an activator of the p53 pathway. Studies show that Tenovin-6 increases p53 levels more than Tenovin-1 and is also more toxic to yeast. Tenovin-6 has also been shown to inhibit SIRT3.

UNC669 is a potent and selective MBT (malignant brain tumor) inhibitor for L3MBTL1.

UNC669 is a potent and selective MBT (malignant brain tumor) inhibitor for L3MBTL1.

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.