Activators & Inhibitors

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.

Anagrelide is a selective thrombocytopenic agent that inhibits PDE3. It also has been used in the treatment of chronic myeloid leukemia.

Anagrelide is a selective thrombocytopenic agent that inhibits PDE3. It also has been used in the treatment of chronic myeloid leukemia.

Apoptosis Activator 2 is a small, cell permeable activator of caspase-3. Apoptosis Activator 2 induces apoptosis specifically in tumor cell lines, but not normal cell lines, with IC50 value of about 4 µM.

Apoptosis Activator 2 is a small, cell permeable activator of caspase-3. Apoptosis Activator 2 induces apoptosis specifically in tumor cell lines, but not normal cell lines, with IC50 value of about 4 µM.

Apoptosis Inhibitor is a cell-permeable inhibitor of apoptosis induction. It does not directly inhibit caspase-3, but its effects are attributable to the inhibition of caspase-3 activation.