2. Signaling Pathways
  3. Epigenetics
  4. Histone Methyltransferase

Histone Methyltransferase

Histone Methyltransferase

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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-A0298
    EZH2-IN-2
    		Inhibitor 98.51%
    EZH2-IN-2 (Example 69) is a EZH2 inhibitor with an IC50 and a TR-FRET IC50 of 64 nM and 20 nM. EZH2-IN-2 can be used for the research of cancer or precancerous condition related to EZH2 activity.
    EZH2-IN-2
  • 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-139611C
    Navlimetostat hydrochloride
    		Inhibitor 99.22%
    Navlimetostat hydrochloride is a potent, orally active, selective PRMT5-MTA complex inhibitor, with IC50s of 3.6 and 20.5 nM for PRMT5-MTA and PRMT5. Navlimetostat hydrochloride binds to the PRMT5-MTA complex, with KD value of 0.14 pM. Navlimetostat shows antineoplastic activity in vitro and in vivo, and can be used for cancer study.
    Navlimetostat hydrochloride
  • 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-147230
    EZH2-IN-13
    		Inhibitor 99.72%
    EZH2-IN-13 is a potent EZH2 inhibitor, for details please refer to compound 73 in patent WO2017139404. EZH2-IN-13 can be used to study cancers or precancerous lesions associated with EZH2 activity.
    EZH2-IN-13
  • HY-151576
    PRMT5:MEP50 PPI
    		Inhibitor 98.09%
    PRMT5:MEP50 PPI is a novel PRMT5:MEP50 protein-protein interaction (PRMT5:MEP50 PPI) inhibitor, shows anti-tumor activity and anti-proliferative activity of lung and prostate cancer cells.
    PRMT5:MEP50 PPI
  • 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-135128
    Dot1L-IN-5
    		Inhibitor 99.82%
    Dot1L-IN-5 is a potent disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor with an IC50 of 0.17 nM.
    Dot1L-IN-5
  • HY-150510A
    MS8511 hydrochloride
    		Inhibitor ≥98.0%
    MS8511 (hydrochloride) is a selective G9a/GLP covalent irreversible inhibitor by targeting a cysteine residue at the substrate binding site, with IC50 values of 100 nM (G9a) and 140 nM (GLP), and Kd values of 44 nM (G9a) and 46 nM (GLP). MS8511 (hydrochloride) reduces the cellular H3K9me2 level and enhances antiproliferation activity. MS8511 (hydrochloride) can be used for the research of several types of cancers including brain, breast, ovarian, lung, bladder, melanoma, colorectal cancer, and other disease such as Alzheimer’s disease (AD), sickle cell disease, Prader−Willi syndrome (PWS).
    MS8511 hydrochloride
  • HY-147185
    PRMT7-IN-1
    		Inhibitor 98.70%
    PRMT7-IN-1 (Compound 14) is a PRMT7 inhibitor with an IC50 of 2.1 μM. PRMT7-IN-1 shows anticancer activity against different cancer cells.
    PRMT7-IN-1
  • HY-P2258
    Histone H3 (1-34)
    		99.44%
    Histone H3 (1-34) is a peptide derived from human histone isotype 3.1. Histones are the main protein components of eukaryotic chromatin. Histone variants and histone modifications modulate chromatin structure, ensuring the precise operation of cellular processes associated with genomic DNA.
    Histone H3 (1-34)
  • HY-171119
    NSD2-PWWP1-IN-1
    		Inhibitor 98.72%
    NSD2-PWWP1-IN-1 (compound 31) is a potent NSD2-PWWP1 inhibitor with an IC50 value of 0.64 µM. NSD2-PWWP1-IN-1 has the potential for the research of cancer.
    NSD2-PWWP1-IN-1
  • HY-12991A
    BIX-01338 hydrate
    		Inhibitor 98.67%
    BIX-01338 hydrate is a histone lysine methyltransferase inhibitor.
    BIX-01338 hydrate
  • HY-Q36691
    PRMT5-IN-30
    		Inhibitor 99.17%
    PRMT5-IN-30 (compound 17) is a potent and selective protein arginine methyltransferase 5 (PRMT5) inhibitor with an IC50 of 0.33 μM and a Kd of 0.987 μM. PRMT5-IN-30 exhibits a broad selectivity against a panel of other methyltransferases. PRMT5-IN-30 inhibits PRMT5 mediated SmD3 methylation.
    PRMT5-IN-30
  • HY-12759A
    CARM1-IN-1 hydrochloride
    		Inhibitor
    CARM1-IN-1 (compound 7g) hydrochloride is a highly potent and selective inhibitor of CARM1 (IC50=8.6 μM, CARM1/PABP1), with low inhibitory activity against PRMT1 and SET7 (IC50 >667 μM). CARM1-IN-1 hydrochloride inhibits the methylation activity of CARM1 and the methylation levels of different substrates, such as PABP1, CA150, SmB, and H3. CARM1-IN-1 hydrochloride also inhibits the promoter activity of prostate-specific antigen (PSA) without significant cytotoxicity.
    CARM1-IN-1 hydrochloride
  • HY-132233A
    DDO-2093 dihydrochloride
    		Inhibitor 98.79%
    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-111904
    EHMT2-IN-2
    		Inhibitor 99.0%
    EHMT2-IN-2 is a potent EHMT inhibitor, with IC50s of all <100 nM for EHMT1 peptide, EHMT2 peptide and cellular EHMT2. Used in the research of blood disease or cancer.
    EHMT2-IN-2
  • HY-108239
    BIX-01294 trihydrochloride
    		Inhibitor 99.68%
    BIX-01294 trihydrochloride is a reversible and highly selective G9a and GLP Histone Methyltransferase inhibitor, with IC50s of of 1.7 μM and 0.9 μM, respectively. BIX-01294 trihydrochloride inhibits G9a/GLP by competing for binding with the amino acids N-terminal of the substrate lysine residue. BIX-01294 trihydrochloride, a (1H-1,4-diazepin-1-yl)-quinazolin-4-yl amine derivative, induces necroptosis and autophagy. BIX-01294 trihydrochloride has antitumor activity in recurrent tumor cells.
    BIX-01294 trihydrochloride
  • HY-136188
    UNC2399
    		Inhibitor 99.16%
    UNC2399, a biotinylated UNC1999, is a selective EZH2 inhibitor, maintaining high in vitro potency for EZH2, with an IC50 of 17 nM.
    UNC2399
  • 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
Cat. No. Product Name / Synonyms Application Reactivity
Histone Methyltransferase Isoform Comparison

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