h3k4

Sinefungin (Adenosyl-Ornithine) belongs to natural products and is an mRNA methyltransferase inhibitor with broad-spectrum antiviral activity. This compound possesses cell permeability and is commonly used in antiviral mechanism research and antiviral drug development.

OICR-9429 is a potent antagonist of the interaction that WDR5 effect with peptide regions of MLL and Histone 3. It reduces the viability of acute myeloid leukemia cells in vitro.

H3K4(Me) (1-20) is a histone peptide; H3K4me is a complexly regulated post-translational modification closely associated with enhancers and promoters at active transcription genomic sites.

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.

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

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.

T-448 is a specific, orally active, and irreversible inhibitor of lysine-specific demethylase 1 (LSD1, an H3K4 demethylase) with an IC50 of 22 nM.

(iso)-T 448 is a rotary isomer of T 448. T-448 is a potent lysine-specific demethylase 1 (LSD1) inhibitor that induces the methylation of H3K4 in rat neurons.

KDOAM-25 citrate is a potent and highly selective histone lysine demethylases 5 (KDM5) inhibitor, with IC50 values of 71 nM, 19 nM, 69 nM, and 69 nM for KDM5A, KDM5B, KDM5C, and KDM5D, respectively. Multiple myeloma MM1S cells treated with KDOAM-25 citrate show increased global H3K4 methylation at transcriptional start sites and impaired proliferation [1].

KDOAM-25 trihydrochloride increases global H3K4 methylation at transcriptional start sites and impairs proliferation in multiple myeloma MM1S cells. KDOAM-25 trihydrochloride is a potent and highly selective histone lysine demethylases 5 (KDM5) inhibitor

KDOAM-25, a potent and highly selective inhibitor of histone lysine demethylases 5 (KDM5) with IC50 values of 71 nM for KDM5A, 19 nM for KDM5B, 69 nM for KDM5C, and 69 nM for KDM5D, enhances global H3K4 methylation at transcriptional start sites and reduces proliferation in multiple myeloma MM1S cells.

T-448 free base, an orally active and irreversible inhibitor of lysine-specific demethylase 1 (LSD1, an H3K4 demethylase), has an IC50 of 22 nM.

LD-110 is a potent PROTAC degrader targeting LSD1 with a DC50 of 0.44 μM. It promotes LSD1 degradation via a ubiquitin-proteasome-dependent mechanism and enhances H3K4 dimethylation levels. By inducing apoptosis, LD-110 inhibits the growth and survival of various esophageal squamous cell carcinoma (ESCC) cell lines. It is applicable for research on esophageal squamous cell carcinoma.

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

MM-401 is a specific inhibitor of histone H3K4 methyltransferase MLL1 activity that acts by reprogramming mouse epiblast stem cells to naive pluripotency.

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.

E67-2, a derivative of E67, is a low-toxicity, selective inhibitor of the KIAA1718 Jumonji domain. It has an IC 50 value of 3.4 μM. E67-2 specifically inhibits the Jumonji demethylase for histone H3 lysine 9 (H3K9) and histone H3 lysine 4 (H3K4) demethylase.

cis-4-Br-2,5-F2-PCPA (S1024) inhibits LSD1 and LSD2 with Ki values of 94 nM and 8.4 μM, respectively. It inhibits LSD1 cell proliferation and increases dimethylated histone H3 at K4 (H3K4) in CCRF-CEM cells, particularly where there is aberrant expression of LSD1 in cancer stem cells [1].

KDOAM-25 trihydrochloride is a potent and highly selective inhibitor of histone lysine demethylase 5 (KDM5), targeting KDM5A (IC50: 71 nM), KDM5B (IC50: 19 nM), KDM5C (IC50: 69 nM), and KDM5D (IC50: 69 nM). It enhances overall H3K4 methylation at the transcription start site and hinders the proliferation of multiple myeloma [MM1S cells].

MRK-740 is a potent and selective inhibitor of PRDM9 histone methyltransferase.MRK-740 inhibits other histone methyltransferases and inhibits PRDM9-dependent H3K4 trimethylation.

Bomedemstat (IMG-7289) hydrochloride is an orally active, irreversible inhibitor of lysine-specific demethylase 1 (LSD1), exhibiting anticancer effects by inhibiting cancer cell proliferation and inducing apoptosis.

WDR5-0102 is a compound that inhibits the WDR5-MLL1 interface (K dis = 7 μM, K d = 4 μM), selectively reducing MLL1 HMT activity without affecting the human H3K4 methyltransferase SETD7 or other HMTs, including G9a, EHMT1, SUV39H2, SETD8, PRMT3, and PRMT5.

INCB059872, also known as INCB59872, is a potent, selective, and orally active lysine-specific demethylase 1 inhibitor. INCB059872 binds to and inhibits LSD1, a demethylase that suppresses the expression of target genes by converting the di- and mono-methylated forms of lysine at position 4 of histone H3 (H3K4) to mono- and unmethylated H3K4, respectively, through amine oxidation. LSD1 inhibition enhances H3K4 methylation and increases the expression of tumor-suppressor genes. In addition, LSD1 demethylates mono- or di-methylated H3K9 which increases gene expression of tumor promoting genes; inhibition of LSD1 promotes H3K9 methylation and decreases transcription of these genes.

MM-401 (TFA), an MLL1 H3K4 methyltransferase inhibitor, effectively impedes MLL1 activity (IC 50 = 0.32 µM) by preventing MLL1-WDR5 interaction. It can induce cell cycle arrest, apoptosis, and differentiation, offering potential for MLL leukemia research [1].