h3k4me3

A-366 is a highly selective peptide-competitive histone methyltransferase G9a inhibitor with IC50s of 3.3 and 38 nM for G9a and GLP, respectively.It is more than 1,000-fold selective for G9a and GLP over the other 21 methyltransferases. It is an inhibitor of the Spindlin1-H3K4me3 interaction with an IC50 of 182.6 nM.It exhibits high affinity for human H3R with a Ki value of 17 nM, and shows subtype selectivity between subgroups of the histaminergic and dopaminergic receptor families.

KDM4-IN-4 (compound 47) is a potent inhibitor of histone lysine demethylase 4 (KDM4), with a binding constant of approximately 80 μM for the KDM4A-Tudor domain. It inhibits H3K4Me3 binding to the Tudor domain in cellular contexts with an EC50 value of 105 μM, holding potential for anticancer research applications [1].

KDM5-C70 is an ethyl ester derivative of KDM5-C49 and functions as an effective, cell-permeable, pan-KDM5 histone demethylase inhibitor. It exhibits an antiproliferative effect in myeloma cells and induces a genome-wide elevation of H3K4me3 levels.

CPI-455 is a specific KDM5 inhibitor.

JQKD82 trihydrochloride, a cell-permeable and selective inhibitor of KDM5, enhances H3K4me3 levels and is utilized in multiple myeloma research.

KDM5-IN-1 is an effective and selective inhibitor of KDM5 with an IC50 of 15.1 nM.

KDM5A-IN-1 is an orally available, potent and selective inhibitor of the pan-histidine lysine demethylase 5 KDM5, inhibiting KDM5A, KDM5B, and KDM5C with IC50 values of 45 nM, 56 nM, and 55 nM, respectively.KDM5A-IN-1 inhibits PC9 H3K4Me3, and may be useful in cancer research.

YUKA1, a cell-permeable KDM5A inhibitor (IC50=2.66 μM) with a weak effect on KDM5C (IC50=7.12 μM) and no effect on other KDM isoforms, was able to increase the level of H3K4me3 in human cells and inhibit the proliferation of cancer cells, and also prevented the emergence of drug-resistant cells.

CPI-455 is a specific KDM5 inhibitor with IC50 value of 10 ± 1 nM for full-length KDM5A in enzymatic assays, elevating global levels of H3K4 trimethylation (H3K4me3) and decreased the number of DTPs in multiple cancer cell line models treated with target

JQKD82 is a selective inhibitor of KDM5 and increases H3K4me3. JQKD82 can be used in studies about the treatment of multiple myeloma.

MS31 trihydrochloride is a selective, high-affinity, fragment-like inhibitor of the methyl-lysine read-write protein spindlin 1 (SPIN1). MS31 trihydrochloride effectively disrupts the interaction of SPIN1 with H3K4me3 protein (IC50: 77 nM, AlphaLISA; 243 nM, FP). MS31 trihydrochloride effectively inhibits the binding of trimethyl lysine containing peptides to SPIN1 and is not toxic to non-tumorigenic cells.

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).

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).

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).

JQKD82 (JADA82) dihydrochloride, a cell-permeable and selective inhibitor of KDM5, enhances H3K4me3 levels, making it effective for multiple myeloma research [1].

MM-102 TFA (HMTase Inhibitor IX TFA) is a potent WDR5 MLL interaction inhibitor with an IC50 of 2.4 nM. This compound prevents the interaction between mixed lineage leukemia 1 (MLL1) and WD Trp-Asp repeat domain 5 (WDR5), inhibiting MLL1 H3K4 histone methyltransferase (HMT) activity and down-regulating H3K4me3, which facilitates the epigenetic reprogramming of porcine somatic cell nuclear transfer embryos.