h3k9me3

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

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

Histone H3K9me3 (1-15) (H3(1-15)K9me3) TFA is used as a substrate. This post-translational modification (PTM) of histone H3K9me3 is indicative of heterochromatin surrounding the centromere.

NV03 is a selective antagonist of the UHRF1-H3K9me3 interaction (Kd=2.4 μM), binding to the UHRF1 tandem Tudor domain (TTD) to form a complex. It is suitable for cancer research. NV03 also functions as a ligand for E3 ligases in PROTAC synthesis.

HP1-IN-2 (Compound (R)-18) is an inhibitor of the interaction between HP1 and H3K9me3, with an IC50 of 18.1 μM. It is useful for studying various cancers characterized by the overexpression of HP1.

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.