h3k9me2

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

MS8511, a selective covalent irreversible inhibitor of G9a GLP, targets a cysteine residue at the substrate binding site, displaying IC50 values of 100 nM (G9a) and 140 nM (GLP), alongside Kd values of 44 nM (G9a) and 46 nM (GLP). This compound effectively reduces cellular H3K9me2 levels and boosts antiproliferation activity, making it applicable in cancer research involving brain, breast, ovarian, lung, bladder, melanoma, and colorectal cancers, as well as studies on Alzheimer's disease (AD), sickle cell disease, and Prader−Willi syndrome (PWS) [1].

MS8511 HCl is a selective and potent covalent inhibitor of G9a GLP that acts by targeting cysteine residues in the substrate binding site. MS8511 has anticancer activity and antiproliferative activity and reduces intracellular H3K9me2 levels.MS8511 can be used to study a wide range of cancers including brain, breast, and ovarian cancers .

D-α-Hydroxyglutaric acid disodium [Disodium (R)-2-Hydroxyglutarate] is a competitive inhibitor of α-ketoglutarate-dependent dioxygenases with a Ki of 0.628 mM.

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

5WKS also known as ZINC97756584 is a biochemical. It is a G9a protein inhibitor.G9A/EHMT2 is a nuclear histone lysine methyltransferase that catalyzes H3K9me2, a reversible modification commonly associated with transcriptional gene silencing.5WKS can be used in the study of autoimmune diseases or tumors.

UNC 0631 is a effectvie histone methyltransferase G9a inhibitor (IC50=4 nM).

G9a-IN-2 (Compound 7i) is an inhibitor of the histone methyltransferase G9a, with an IC50 of 0.024 μM. It can reduce the levels of H3K9me2 and induce the expression of γ-globin mRNA. G9a-IN-2 shows potential for improving Sickle Cell Disease (SCD).

CBB1007 trihydrochloride is a cell-permeable amidino-guanidinium compound that acts as a potent, reversible and substrate competitive LSD1 selective inhibitor (IC50 = 5.27 μM for hLSD1). IC50 Value: 5.27 uM Target: hLSD1 CBB1007 efficiently can block LSD1-mediated demethylation of H3K4Me2 and H3K4Me (IC50 ≤ 5 μM) with no effect on H3K4Me3 and H3K9Me2, and LSD2 and JARID1A activities. Increases H3K4Me2 and H3K4Me contents (IC50 ≤ 5 μM), and causes activation of epigenetically suppressed CHRM4 M4-ArchR and SCN3A genes in F9 cells (IC50 ≤ 3.74 μM). CBB1007 was Shown to preferentially arrest the growth of pluripotent tumors with minimal effect on non-pluripotent cancer or normal somatic cells (IC50 ≥ 100 μM).

MS8511 (hydrochloride) is a specific covalent and irreversible inhibitor of G9a GLP, targeting the cysteine residue at the substrate binding site. It has an IC50 of 100 nM for G9a and 140 nM for GLP, with Kd values of 44 nM for G9a and 46 nM for GLP. This compound reduces intracellular H3K9me2 levels and enhances antiproliferative activity, making it useful for studying various cancers, including brain, breast, ovarian, lung, bladder cancers, melanoma, and colorectal cancer, as well as other diseases like Alzheimer's disease (AD), sickle cell disease, and Prader-Willi syndrome (PWS).

CBB1007 HCl is a cell-permeable amidino-guanidinium compound identified as a potent, reversible, and substrate-competitive inhibitor of LSD1 (IC50 = 5.27 μM for hLSD1). It effectively inhibits LSD1-mediated demethylation of H3K4Me2 and H3K4Me (IC50 ≤ 5 μM), without affecting H3K4Me3 and H3K9Me2 demethylation, nor the activities of LSD2 and JARID1A. Moreover, CBB1007 increases the levels of H3K4Me2 and H3K4Me (IC50 ≤ 5 μM) and activates epigenetically suppressed genes CHRM4 M4-ArchR and SCN3A in F9 cells (IC50 ≤ 3.74 μM). It preferentially inhibits the growth of pluripotent tumors with minimal impact on non-pluripotent cancer or normal somatic cells (IC50 ≥ 100 μM).

RK-701, a highly selective and non-genotoxic G9a inhibitor, exhibits an IC 50 value of 23-27 nM. It selectively up-regulates HbF, γ-Globin, and BGLT3 expression while down-regulating H3K9me2 expression. Additionally, RK-701 inhibits BCL11A and ZBTB7A.

CM-272 is a dual G9a DNA methyltransferases (DNMTs) inhibitor.

Lysine-specific demethylase inhibitor (1C) (LSD inhibitor (1C)) is an inhibitor of LSD1, a repressive demethylase selective for histone H3 lysine 4 (H3K4).1,2LSD inhibitor (1C) inhibits LSD1 activity by 85.9% when used at a concentration of 10 μM.1It increases the level of H3K4 methylation, including H3K4me1 and H3K4me2 but not H3K9me2 levels, in HCT116 human colon carcinoma cells.2LSD inhibitor (1C) also induces re-expression of the Wnt signaling pathway proteins secreted frizzle-related protein 1 (SFRP1), SFRP4, and SFRP5, as well as the transcription factor GATA5, which are aberrantly silenced in HCT116 cells.

UNC0321 is an effective inhibitor of histone methyltransferase G9a with a Ki of 63 pM and with IC50s 9 nM and 6 nM in ECSD and CLOT assays. UNC0321 inhibits GLP with IC50s of 15 nM and 23 nM in ECSD and CLOT assays.

UNC0646 is a potent and selective inhibitor of the homologous protein lysine methyltransferases G9a and GLP (IC50s: 6 nM 15 nM for G9a GLP). UNC0646(UNC 0646) potently blocks G9a GLP methyltransferase activity in cells (IC50: 10 nM in MCF7 cells) and exhibits low cellular toxicity (EC50: 4.7 μM in MCF7 cells).

ZZM-1220, a covalent inhibitor of histone lysine methyltransferase G9a GLP, exhibits IC50 values of 458 nM for G9a and 924 nM for GLP. It effectively inhibits H3K9me2 in cells, induces apoptosis in triple-negative breast cancer (TNBC) cells, and arrests the cell cycle at the G2 M phase [1].