h3k4

Sinefungin (Adenosyl-Ornithine) is an effective inhibitor of virion mRNA(guanine-7-)-methyltransferase, mRNA(nucleoside-2'-)-methyltransferase, and viral multiplication. Sinefungin is a SET7 9 inhibitor and ameliorates renal fibrosis by inhibiting H3K4 methylation.

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.

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.

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

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].

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

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.

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.

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].

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.

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.

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

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.

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].

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.

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].

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.

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.

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