Activators & Inhibitors

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.

UNC0321is a selective histone lysine methyltransferase (HMTase) inhibitor for G9a and GLP (also known as EHMT1), with IC50 of 9 nM and 15 nM, respectively. It is more than 10,000-fold more selective for G9a and GLP vs. SET7/9, SET8, PRMT3, or JMJD2E.

Milrinone, also known as WIN 47203 and Primacor®, is an inhibitor of PDE3. It is less effective against other PDE isoforms. Milrinone has positive inotropic and vasodilatory effects in vivo.

Milrinone, also known as WIN 47203 and Primacor®, is an inhibitor of PDE3. It is less effective against other PDE isoforms. Milrinone has positive inotropic and vasodilatory effects in vivo.

PARP1 Inhibitor

Z-VAD(OMe)-FMK is a cell permeable, irreversible pan-caspase inhibitor and anti-apoptotic agent. It has been shown to inhibit Fas-mediated apoptosis in Jurkat T cells and apoptosis in THP.1 cells induced by diverse stimuli (including cycloheximide, thapsigargin, etoposide and staurosporine). Inhibits caspases 1, 3, 4, and 7.