Activators & Inhibitors

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.

I-CBP112 (Hydrochloride) is a selective inhibitor of cAMP responsive-element binding protein (CREBBP) and E1A binding protein p3000 (EP3000). The inhibitor has been shown to decrease EZH2 activity and to inhibit trimethylation of lysine 27 on histone H3 in cultured human AML HL-60 and OCI-AML3 cells. It has the same effect on primary AML cells in a dose-dependent manner.

Telotristat is the active metabolite of LX1606 (Telotristat etiprate), which is an orally bioavailable, small-molecule, tryptophan hydroxylase (TPH) inhibitor with potential antiserotonergic activity.