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-100565A
    SGC2085 hydrochloride
    		Inhibitor
    SGC2085 hydrochloride is a potent and selective inhibitor of coactivator associated arginine methyltransferase 1 (CARM1) with an IC50 of 50 nM. SGC2085 hydrochloride also selectively inhibits PRMT6 with an IC50 value of 5.2 μM, but not other PRMT proteins.
    SGC2085 hydrochloride
  • HY-142094
    NSD3-IN-2
    		Inhibitor
    NSD3-IN-2 is a potent NSD3 inhibitor with an IC50 value of 17.97 μM. NSD3-IN-2 inhibits the growth and proliferation of non-small cell lung cancer cell lines H460, H1299 and H1650 with anti-cancer activity.
    NSD3-IN-2
  • HY-44062
    G9a-IN-1
    		Inhibitor 98.12%
    G9a-IN-1 (Compound 113) is a G9a protein inhibitor. G9A/EHMT2 is a nuclear histone lysine methyltransferase that catalyzes histone H3 lysine 9 dimethylation (H3K9me2), which is a reversible modification generally associated with transcriptional gene silencing. G9a-IN-1 can be used for the research of autoimmune disorders or cancer.
    G9a-IN-1
  • HY-160865
    PRMT5-IN-35
    		Inhibitor 99.63%
    PRMT5-IN-35 (Compound 87) is a potent, selective and orally active PRMT5 inhibitor with an IC50 value of 1 nM . PRMT5-IN-35 can be used in cancer research.
    PRMT5-IN-35
  • HY-145452
    5-Octyl-α-ketoglutarate
    5-Octyl-α-ketoglutarate (5-Octyl 2-oxopentanedioate) is a cell-permeable substrate for lysine demethylase. 5-Octyl-α-ketoglutarate is related to protein demethylation, inhibits cell proliferation of wtCRBN expressing cells, and also enhances Lenalidomide (HY-A0003)-induced sensitivity and inhibits myeloma (MM) ) drug resistance of cells. When myeloma (MM) cells undergo glutamine-dependent proliferation, α-ketoglutarate increases glutamine catabolism to promote protein demethylation.
    5-Octyl-α-ketoglutarate
  • HY-158157
    ZL-28-6
    		Inhibitor
    ZL-28-6 is a type I PRMT inhibitor (IC50: 18 nM). ZL-28-6 effectively targets CARM1 (a member of PRMT) within cells and can be used for cancer research.
    ZL-28-6
  • HY-173092
    PRMT5 ligand 1
    		Ligand
    PRMT5 ligand 1 (compound 3) is the ligand for PRMT5 that can be used as target protein ligand for synthesis of PROTAC degrader MS4322 (HY-141877).
    PRMT5 ligand 1
  • HY-B1322R
    Amodiaquine (dihydrochloride dihydrate) (Standard)
    		Inhibitor
    Amodiaquine (dihydrochloride dihydrate) (Standard) is the analytical standard of Amodiaquine (dihydrochloride dihydrate). This product is intended for research and analytical applications. Amodiaquine dihydrochloride dihydrate (Amodiaquin dihydrochloride dihydrate), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine dihydrochloride dihydrate is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC50 of ~20 μM. Anti-inflammatory effect.
    Amodiaquine (dihydrochloride dihydrate) (Standard)
  • HY-118715
    Setin-1
    		Inhibitor
    Setin-1 is one of the most potent inhibitors of Set7, acting by inhibiting KMTase G9a.
    Setin-1
  • HY-103641C
    Octyl-α-hydroxyglutarate
    		Agonist
    Octyl-α-hydroxyglutarate (octyl-2-HG) increases histone methylation and enhances viability of LMP1-negative NPC cells.
    Octyl-α-hydroxyglutarate
  • HY-117927
    EPZ0025654
    		Inhibitor
    EPZ0025654 (GSK3536023) is an inhibitor for protein arginine methyltransferases 4 (PRMT4) (which is also known as coactivator associated arginine methyltransferase 1 CARM1), with IC50 of 3 nM.
    EPZ0025654
  • HY-113846A
    CMP-5 dihydrochloride
    		Inhibitor
    CMP-5 dihydrochloride is a potent, specific, and selective PRMT5 inhibitor, while displays no activity against PRMT1, PRMT4, and PRMT7 enzymes. CMP-5 dihydrochloride selectively blocks S2Me-H4R3 by inhibiting PRMT5 methyltransferase activity on histone preparations. CMP-5 dihydrochloride prevents EBV-driven B-lymphocyte transformation but leaving normal B cells unaffected.
    CMP-5 dihydrochloride
  • HY-165496
    KAT-IN-2
    		Inhibitor
    KAT-IN-2 (7) is a potent and selective kynurenine aminotransferase II (KATII) inhibitor.
    KAT-IN-2
  • HY-157251A
    UNC8153
    		Inhibitor
    UNC8153 is a potent and selective nuclear receptor-binding SET domain-containing 2 (NSD2)-targeted degrader with a Kd of 24 nM. UNC8153 reduces the cellular levels of both NSD2 protein and the H3K36me2 chromatin mark. UNC8153 contains a simple warhead that confers proteasome-dependent degradation of NSD2.
    UNC8153
  • HY-12707B
    Piribedil maleate
    		Inhibitor
    Piribedil maleate is a potent and orally active dopamine D2 and dopamine D3 agonist. Piribedil maleate is also a α2-adrenoceptors antagonist. Piribedil maleate can inhibit MLL1 methyltransferase activity (EC50: 0.18 μM). Piribedil maleate has the potential for the research of parkinson's disease, circulatory disorders, cancers.
    Piribedil maleate
  • HY-169761
    WIZ-IN-1
    		Degrader
    WIZ-IN-1 (Example 2) is a Wiz inhibitor (DC50: 0.36 μM). WIZ-IN-1 can be used for research of inherited blood disorders (e.g., hemoglobinopathies, e.g., beta- hemoglobinopathies), such as sickle cell disease and beta-thalassemia.
    WIZ-IN-1
  • HY-111085
    CPI-905
    		Inhibitor
    CPI-905 is a potent, selective, and cell-active EZH2 inhibitor.
    CPI-905
  • HY-116605
    GSK926
    		Inhibitor
    GSK926 (compound 3) is a selective histone lysine methyltransferase EZH2 inhibitor (IC50=0.02 μM; Ki=7.9 nM), with SAM-competitive and cell-active properties. GSK926 can be used in cancer research.
    GSK926
  • HY-114206
    SKI-73
    SKI-73 is a chemical probe for CARM1 with prodrug properties. SKI-73 can rapidly penetrate cell membranes and be processed into active inhibitors. SKI-73 inhibits the invasion of breast cancer cells and can be used in the study of cancer.
    SKI-73
  • HY-154812
    Gintemetostat
    		Inhibitor
    Gintemetostat (KTX-1001) is a potent NSD2 inhibitor with an IC50 ranging from 0.001 μM to 0.01 μM. As a piperidinyl-methyl-purineamine derivative, gintemetostat has potential applications in cancer research.
    Gintemetostat
Cat. No. Product Name / Synonyms Application Reactivity
Histone Methyltransferase Isoform Comparison

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