2. Signaling Pathways
  3. Epigenetics
  4. Histone Methyltransferase

Histone Methyltransferase

Histone Methyltransferase

Related Products

PDF 2.85 MB

Histone modifications play critical roles in regulating both global and stage-specific gene expression. Methylation on histones H3K4, H3K36 and H3K79 is generally associated with gene activation, whereas methylation on histones H3K9 and H3K27 is generally associated with gene repression. Histone lysine methylation is dynamically regulated by site-specific methyltransferases and demethylases. EZH2 (the catalytic subunit of PRC2) is responsible for the methylation of H3K27 in cells.

DOT1L is a histone H3 lysine 79 methyltransferase whose inhibition increases the yield of induced pluripotent stem cells (iPSCs). EPZ-5676 is a potent and selective DOT1L inhibitor.

Crucial to PRC2 activity, the histone methyltransferase enhancer of zeste homolog 2 (EZH2) tri-methylates lysine 27 of histone 3 (H3K27me3), leading to chromatin condensation and transcriptional repression.

Histone Methyltransferase Isoform Specific Products:

Histone Methyltransferase Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-141716
    SW2_110A
    		Inhibitor 99.19%
    SW2_110A is a selective chromobox 8 chromodomain (CBX8 ChD) inhibitor with a Kd of 800 nM. SW2_110A shows minimal 5-fold selectivity for CBX8 ChD over all other CBX paralogs in vitro.
    SW2_110A
  • HY-153728
    WM-586
    		Inhibitor 98.74%
    WM-586 is a covalent WDR5 inhibitor that disrupts the binding of WDR5 to MYC. WM-586 specifically decreases cellular WDR5 and MYC interaction with the IC50 of 101 nM in HTRF assay.
    WM-586
  • HY-161024
    AC1Q3QWB
    		Inhibitor 99.39%
    AC1Q3QWB upregulates CDKN1A and SOX17 by interrupting the HOTAIR-EZH2 interaction and enhances the efficacy of Tazemetostat in endometrial cancer.
    AC1Q3QWB
  • HY-162308
    NSD-IN-3
    		Inhibitor ≥98.0%
    NSD-IN-3 (compound 3) is a potent nuclear receptor binding SET domain (NSD) inhibitor. NSD-IN-3 inhibits NSD2-SET and NSD3-SET with IC50 values of 0.81 μM and 0.84 μM, respectively. NSD-IN-3 inhibits histone H3K36 dimethylation and decreases the expression of NSDs-targeted genes in non-small cell lung cancer cells. NSD-IN-3 induces s-phase cell cycle arrest and apoptosis.
    NSD-IN-3
  • HY-157164
    PROTAC EZH2 Degrader-2
    		Degrader 99.78%
    PROTAC EZH2 Degrader-2 (compound E-3P-MDM2), an EZH2 inhibitor, is a PROTAC composed of Tazemetostat (EPZ6438) and an E3 ligase system ligand. PROTAC EZH2 Degrader-2 degrades EZH2 in SU-DHL-6 cells in a dose-dependent manner, inhibits the expression of H3K27me3, and simultaneously degrades EED and SUZ12 proteins without affecting their mRNA levels. PROTAC EZH2 Degrader-2 has anti-cancer and anti-proliferative activity.
    PROTAC EZH2 Degrader-2
  • HY-A0298
    EZH2-IN-2
    		Inhibitor 99.40%
    EZH2-IN-2 is a EZH2 inhibitor extracted from patent WO2018133795A1, Compound Example 69, with an IC50 of 64 nM. EZH2-IN-2 can be used for the research of cancer or precancerous condition related to EZH2 activity.
    EZH2-IN-2
  • HY-101508
    GNA002
    		Inhibitor 98.02%
    GNA002 is a highly potent, specific and covalent EZH2 (Enhancer of zeste homolog 2) inhibitor with an IC50 of 1.1 μM. GNA002 can specifically and covalently bind to Cys668 within the EZH2-SET domain, triggering EZH2 degradation through COOH terminus of Hsp70-interacting protein (CHIP)-mediated ubiquitination. GNA002 efficiently reduces EZH2-mediated H3K27 trimethylation, reactivates polycomb repressor complex 2 (PRC2)-silenced tumor suppressor genes.
    GNA002
  • HY-132233A
    DDO-2093 dihydrochloride
    		Inhibitor 98.52%
    DDO-2093 dihydrochloride is a potent MLL1-WDR5 protein-protein interaction inhibitor (IC50=8.6 nM; Kd=11.6 nM) with antitumor activity. DDO-2093 dihydrochloride selectively inhibits the catalytic activity of MLL complex.
    DDO-2093 dihydrochloride
  • HY-154847
    WM-662
    		Inhibitor 99.48%
    WM-662 is a WDR5-MYC interaction inhibitor, with an IC50 of 18 μM. WM-662 has potential for the research of cancer, aging, and neurodegenerative disorders.
    WM-662
  • HY-12991A
    BIX-01338 hydrate
    		Inhibitor 98.81%
    BIX-01338 hydrate is a histone lysine methyltransferase inhibitor.
    BIX-01338 hydrate
  • HY-124101
    PDAT
    		Inhibitor ≥98.0%
    PDAT is a noncompetitive indolethylamine-N-methyltransferase (INMT) inhibitor with a Ki of 84 μM for rabbit lung INMT (rabINMT).
    PDAT
  • HY-111418
    EBI-2511
    		Inhibitor 99.81%
    EBI-2511 is a highly potent and orally active EZH2 inhibitor, with an IC50 of 6 nM in Pfeffiera cell lines, respectively.
    EBI-2511
  • HY-120137
    CMP-5
    		Inhibitor 99.02%
    CMP-5 is a potent, specific, and selective PRMT5 inhibitor, while displays no activity against PRMT1, PRMT4, and PRMT7 enzymes. CMP-5 selectively blocks S2Me-H4R3 by inhibiting PRMT5 methyltransferase activity on histone preparations. CMP-5 prevents Epstein-Barr virus (EBV)-driven B-lymphocyte transformation but leaving normal B cells unaffected.
    CMP-5
  • HY-100869A
    MM-589 TFA
    		Inhibitor 98.67%
    MM-589 TFA is a potent inhibitor of WD repeat domain 5 (WDR5) and mixed lineage leukemia (MLL) protein-protein interaction. MM-589 binds to WDR5 with an IC50 of 0.90 nM and inhibits the MLL H3K4 methyltransferase activity with an IC50 of 12.7 nM.
    MM-589 TFA
  • HY-141539A
    SETDB1-TTD-IN-1 TFA
    		99.77%
    SETDB1-TTD-IN-1 TFA is a potent, selective and endogenous binder competitive ligand of SET domain bifurcated protein 1 tandem tudor domain (SETDB1-TTD) that binds to TTD, with a Kd of 88 nM. SETDB1-TTD-IN-1 TFA increases SETDB1 methyltransferase activity. SETDB1-TTD-IN-1 TFA can be used for the research of biological functions and disease associations of SETDB1-TTD.
    SETDB1-TTD-IN-1 TFA
  • HY-128352
    SMYD3-IN-1
    		Inhibitor 98.01%
    SMYD3-IN-1 (compound 29) is an irreversible and selective inhibitor of SMYD3 (SET and MYND domain containing 3), with an IC50 of 11.7 nM.
    SMYD3-IN-1
  • HY-107777A
    LLY-284
    		Control 99.11%
    LLY-284 is the diastereomer of LLY-283 with much less active. LLY-283 is a potent inhibitor of PRMT5. LLY-284 has the potential for the research of cancer diseases.
    LLY-284
  • HY-162384
    EPIC-0628
    		Inhibitor 98.93%
    EPIC-0628 is an inhibitor of the HOTAIR-EZH2 interaction and promotes ATF3 expression. The long noncoding RNA HOTAIR has been found to regulate glioblastoma (GBM) progression and mediate DNA damage repair (DDR) by interacting with the catalytic subunit EZH2 of PRC2. EPIC-0628 also inhibits the ATF3-p38-E2F1 DDR pathway to inhibit the HR pathway and upregulates CDKN1A (p21) expression, causing cell cycle arrest. EPIC-0628 also synergizes with Temozolomide (TMZ) (HY-17364) to enhance its in vivo potency.
    EPIC-0628
  • HY-122936
    Tanshindiol C
    		Inhibitor 98.47%
    Tanshindiol C is a S-adenosylmethionine-competitive EZH2 (Histone Methyltransferase) inhibitor with an IC50 of 0.55 μM for inhibiting the methyltransferase activity. Tanshindiol C is also an activator of both Nrf2 and Sirtuin 1 (Sirt1) in macrophages. Tanshindiol C possesses anti-cancer activity, and can be used for atherosclerosis research.
    Tanshindiol C
  • HY-119198
    NSC745885
    		Inhibitor ≥98.0%
    NSC745885 an effective anti-tumor agent, shows selective toxicity against multiple?cancer?cell lines but not normal cells.?NSC745885 is an effective?down-regulator of EZH2 via proteasome-mediated degradation. NSC745885 provides possibilities for the study of advanced?bladder?and oral squamous cell carcinoma (OSCC) cancers.
    NSC745885
Cat. No. Product Name / Synonyms Application Reactivity
Histone Methyltransferase Isoform Comparison

Your Search Returned No Results.

Sorry. There is currently no product that acts on isoform together.

Please try each isoform separately.