Activators & Inhibitors

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.

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.

PYR-41 is a cell permeable, irreversible inhibitor of ubiquitin activating enzyme E1 with little or no activity against E2s or E3s (IC50 < 10 µM). It blocks degradation of p53 and inhibits NF-κappaB-dependent pathways. PYR-41 also increases SUMOylation of proteins.

Alvespimycin HCl, also known as 17-DMAG, is a potent, water-soluble HSP90 inhibitor. Alvespimycin has diverse anti-tumor actions and has potential in treating a number of different types of cancers, including ovarian, prostate, melatnoma, non-small-cell lung cancer, and several leukemias (chronic lymphocytic, acute myeloid). This compound also suppresses inflammation by interfering with signaling through the NF-κB pathway.

Alvespimycin HCl, also known as 17-DMAG, is a potent, water-soluble HSP90 inhibitor. Alvespimycin has diverse anti-tumor actions and has potential in treating a number of different types of cancers, including ovarian, prostate, melatnoma, non-small-cell lung cancer, and several leukemias (chronic lymphocytic, acute myeloid). This compound also suppresses inflammation by interfering with signaling through the NF-κB pathway.