h3k9me3

BIX-01294 is an G9a Histone Methyltransferase inhibitor(IC50 : 1.9 μM).

BIX-01294 trihydrochloride is an inhibitor of G9a histone methyltransferase.In a cell-free assay, the IC50=2.7 μM for G9a histone methyltransferase.

NV03 is a potent and selective antagonist of the UHRF1 (Ubiquitin-like with PHD and RING finger domains 1)-H3K9me3 interaction, binding to the UHRF1 tandem tudor domain with a Kd of 2.4 μM. NV03 holds potential as an anticancer therapeutic [1].

Methylstat is a methyl ester prodrug of a Jumonji C domain-containing histone demethylase (JMJD) inhibitor that has favorable cell permeability. The free acid of methylstat inhibits JMJD2A, JMJD2C, JMJD2E, PHF8, and JMJD3 with IC50 values of approximately 4.3, 3.4, 5.9, 10, and 43 μM, respectively, in an in vitro assay. Methylstat inhibits growth of the JMJD2C-sensitive esophageal cancer cell line KYSE150 with a GI50 of 5.1 μM, whereas the free acid of methylstat did not inhibit cell growth up to 100 μM. Methylstat induces histone hypermethylation at multiple sites in a concentration-dependent manner (EC50 for H3K4me3 and H3K9me3 = 10.3 and 8.6 μM in KYSE150 cells and 6.7 ad 6.3 μM in MCF-7 cells, respectively).

F5446 is a selective small molecule SUV39H1 methyltransferase inhibitor. It promotes apoptosis in colorectal cancer cells by inhibiting the deposition of H3K9me3 on the FAS promoter to increase Fas expression, while inhibiting CTL effector gene expression.