Activators & Inhibitors

(R)-MG132 is a potent, cell permeable and reversible inhibitor of proteasomes. It can inhibit proteasome activity in lysates of J558L multiple myeloma cells and EMT6 breast cancer cells. In comparison to (S)-MG132, the (R)-MG132 stereoisomer is a more effective inhibitor of chymotrypsin-like (ChTL), trypsin-like (TL), and peptidylglutamyl peptide hydrolyzing proteasome (PGPH) activities.

IU1 is a small molecule, reversible inhibitor of deubiquitination by USP14. It selectively stimulates ubiquitin-dependent protein degradation in vitro at 34 µM and in MEF cells at 50 µM. IU1 can also reduce accumulation of oxidized proteins in HEK293 cells, which alleviates cytotoxicity induced by oxidative stress.

AGK2 is a selective, cell-permeable inhibitor of SIRT2. It has minimal effects SIRT1 and SIRT3 at 10-fold higher levels compared to SIRT2. Useful for studing SIRT2 in neurodegeneration and aging, as well as cell cycle progression and tumorigenesis.

BAY-11-7082 is a selective and irreversible inhibitor of NF-κB activation by blocking TNF-α-induced phosphorylation of IκB-α without affecting constitutive IκB-α phosphorylation. It also inhibits the TNF-α-induced surface expression of adhesion molecules ICAM-1, VCAM-1, and E-selectin in human endothelial cells.

(S)-MG132, also known as Z-Leu-Leu-Leu-CHO, is a potent, reversible and cell-permeable inhibitor of proteasomes that inhibits cell growth in B16 and IPC227F cells. It also inhibits NF-κB activation, sensitizing a variety of carcinoma cell lines to apoptosis.

Aliskiren Hydrochloride is an orally active, synthetic nonpeptide Renin inhibitor that has been shown to work as an antihypertensive.

CP 80633 is a selective inhibitor of PDE4, which does not display significant isozyme selectivity. It also inhibits hydrolysis of cAMP in isolated monocytes, eosinophils, human peripheral blood and T-cells. It has been shown to exhibit anti-inflammatory and bronchodilatory activity in vivo.

UNC0224 is a potent and selective inhibitor of G9a, a histone methyltransferase (HMT). It also inhibits GLP, a closely-related H3K9 HMT, but is more than 1,000-fold selective against SET7/9 and SET8.

Tranylcypromine (2-PCPA) is an irreversible inhibitor of LSD1 histone demethylase and monoamine oxidases (MAO). The inhibitor targets monoamine oxidases A and B and has been used as a chemical scaffold to design new demethylase inhibitors. Tranylcypromine has been shown to increase Histone H3 lysine 4 (H3K4) methylation in P19 embryonal carcinoma cell.