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-179386
    PARP1/EZH2-IN-1
    		Inhibitor
    PARP1/EZH2-IN-1 is a selective PARP1 and EZH2 dual inhibitor. PARP1/EZH2-IN-1 has IC50s of 28 nM, 414 nM and 74 nM for PARP1, PARP2 and EZH2, respectively. PARP1/EZH2-IN-1 inhibits the proliferation and migration of TNBC cells (triple-negative breast Cancer cells). PARP1/EZH2-IN-1 induces PANoptosis (Apoptosis, Pyroptosis and Necroptosis), increases the level of reactive oxygen species (ROS), and activates related inflammatory pathways. PARP1/EZH2-IN-1 can be used in triple-negative breast cancer research.
    PARP1/EZH2-IN-1
  • HY-139150
    EZH2-IN-4
    		Inhibitor
    EZH2-IN-4 is an orally active, potent EZH2 inhibitor with IC50s of 0.923 nM and 2.65 nM against wild type (WT) 5-membered (5-mer) EZH2 and mutant 5-mer EZH2, respectively. EZH2-IN-4 has anti-cancer activity.
    EZH2-IN-4
  • HY-163288
    EZH2/HSP90-IN-29
    		Inhibitor
    EZH2/HSP90-IN-29 is a dual inhibitor for EZH2 and HSP90, with IC50s of 6.29 nM and 60.1 nM, for EZH2 and HSP90, respectively. EZH2/HSP90-IN-29 increases apoptosis/necrosis-related gene expression, induces cell cycle arrest at M phase and inhibits reactive oxygen species (ROS) catabolism pathway. EZH2/HSP90-IN-29 is able to cross the blood-brain-barrier (BBB).
    EZH2/HSP90-IN-29
  • HY-12707A
    Piribedil dihydrochloride
    		Inhibitor
    Piribedil dihydrochloride is a potent and orally active dopamine D2 and dopamine D3 agonist. Piribedil dihydrochloride is also a α2-adrenoceptors antagonist. Piribedil dihydrochloride can inhibit MLL1 methyltransferase activity (EC50: 0.18 μM). Piribedil dihydrochloride has the potential for the research of parkinson's disease, circulatory disorders, cancers.
    Piribedil dihydrochloride
  • HY-W699159
    Acedapsone-d8
    Acedapsone-d8 is the deuterium labeled Acedapsone (HY-B1377). Acedapsone is a compound with antimalarial and antimicrobial activities. Acedapsone is mainly used as a long-acting leprosy inhibitor.
    Acedapsone-d<sub>8</sub>
  • HY-180816
    PRMT5-MTA-IN-7
    		Inhibitor
    PRMT5-MTA-IN-7 (Compound 14) is a selective PRMT5-MTA inhibitor. PRMT5-MTA-IN-7 exhibits KD values of PRMT5-MTA-IN-7 for PRMT5-MTA and PRMT5-SAM of 236 nM and 2.84 μM respectively, and the IC50 values of 4.08 and 13.6 μM respectively. PRMT5-MTA-IN-7 can selectively inhibit the proliferation of MTAP-deficient cancer cells. PRMT5-MTA-IN-7 can be used for the study of colon cancer.
    PRMT5-MTA-IN-7
  • HY-122595
    EZH2-IN-1
    		Inhibitor
    EZH2-IN-1 (compound 3) is a selective and SAM-competitive EZH2 and EZH1 inhibitor with an IC50s of 32 nM, 197 nM and 213 nM for EZH2wt, EZH2 Y641N mutant and EZH1, respectively. EZH2-IN-1 reduces bulk H3K27me3 and H3K27me2 levels. EZH2-IN-1 has the potential for diffuse large B cell lymphoma research.
    EZH2-IN-1
  • HY-163589
    PRMT5-IN-40
    		Inhibitor
    PRMT5-IN-40 (compound 104) is a potent inhibitor of PRMT5.
    PRMT5-IN-40
  • HY-181300
    PROTAC EZH2 Degrader-17
    		Degrader
    PROTAC EZH2 Degrader-17 (compound 52) is a PROTAC protein degrader targeting EZH2 with an antiproliferative IC50 of 18.32 μM in lymphoma cells. PROTAC EZH2 Degrader-17 exhibits antiproliferative activity against lymphoma cells. PROTAC EZH2 Degrader-17 can be used for the research of lymphoma.
    PROTAC EZH2 Degrader-17
  • HY-110137A
    Furamidine
    		Inhibitor
    Furamidine (DB75) is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 9.4 μM. Furamidine is selective for PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) (IC50s of 166 µM, 283 µM, and >400 µM, respectively). Furamidine is a potent, reversible and competitive tyrosyl-DNA phosphodiesterase 1 (TDP-1) inhibitor. Inhibition of TDP-1 by Furamidine is effective both with single- and double-stranded DNA substrates but is slightly stronger with the duplex DNA. Furamidine is also an antiparasite agent.
    Furamidine
  • HY-12970B
    EPZ020411 dihydrochloride
    		Inhibitor
    EPZ020411 dihydrochloride is a selective, blood-brain barrier-permeable PRMT6 inhibitor with an IC50 of 0.010 μM. EPZ020411 dihydrochloride blocks PRMT6-mediated histone H3R2 methylation, reduces ROS production, and inhibits Apoptosis. EPZ020411 dihydrochloride is applicable to research related to neuropathic pain, colorectal cancer, ototoxicity, hearing loss and glioblastoma.
    EPZ020411 dihydrochloride
  • HY-149463
    EZH2-IN-16
    		Inhibitor
    EZH2-IN-16 (Compound 24) is an inhibitor for histone methyltransferase (EZH2). EZH2-IN-16 inhibits EZH2 and EZH2 Y641F, with IC50 of 37.6 and 79.1 nM. EZH2-IN-16 inhibits proliferation of WSU-DLCL2, with GI50 of 0.2 μM.
    EZH2-IN-16
  • HY-P5922
    PTD2
    		Inhibitor
    PTD2 (Ac-Gly-Val-Nle-Arg-Ile-NH2) is a potent, selective inhibitor of WHSC1. PTD2 exhibits micromolar affinity towards WHSC1.
    PTD2
  • HY-182297
    PRMT1 ligand-1
    PRMT1 ligand-1 is a PRMT1 ligand. PRMT1 ligand-1 can be used as a target protein ligand to develop and design degraders of PROTAC PRMT1, such as PROTAC PRMT1 degrader-1 (HY-182275). PROTAC PRMT1 degrader-1 inhibits the growth of various cancer cells.
    PRMT1 ligand-1
  • HY-180846
    NT32
    		Modulator
    NT32 is a selective METTL13 stabilizer with a Kd value of 14 μM. NT32 could occupy both the SAM/SAH-binding pocket and the peptide substrate-binding site of METTL13 simultaneously. NT32 specifically targets and stabilizes METTL13. NT32 shows no inhibitory activity against non-small cell lung cancer.
    NT32
  • HY-168083
    Dot1L-IN-9
    		Inhibitor
    Dot1L-IN-9 (Compound 12) is a DOT1L inhibitor (IC50: 125 nM). Dot1L-IN-9 reduces H3K79 dimethylation. Dot1L-IN-9 can be used for anti-leukemia research.
    Dot1L-IN-9
  • HY-163585
    PRMT5-IN-36
    		Inhibitor
    PRMT5-IN-36 (compound 4) is an orally active PRMT5 inhibitor and can be used for study of cancer.
    PRMT5-IN-36
  • HY-179351
    EZH2 ligand-1
    		Ligand
    EZH2 ligand-1 (Compound E) is an EZH2 ligand that can be used for the synthesis of PORTAC.
    EZH2 ligand-1
  • HY-181333
    PROTAC EZH2 Degrader-38
    		Degrader
    PROTAC EZH2 Degrader-38 (Compound 17) is a EZH2 PROTAC degrader with an IC50 of 165.00 nM. PROTAC EZH2 Degrader-38 functionally inhibits the methyltransferase activity of EZH2 and competitively binds to the SAM-binding pocket of the EZH2 SET domain.
    PROTAC EZH2 Degrader-38
  • HY-168131
    PROTAC EZH2 Degrader-3
    		Degrader
    PROTAC EZH2 Degrader-3 (compound ZJ-20) is a EZH2 PROTAC degrader. PROTAC EZH2 Degrader-3 (5 μM, 24 h) not only potently inhibits the expression of EZH2 protein, but also had a strong inhibits effect on the expression levels of other subunits of PRC2 as well as H3k27me3 protein. PROTAC EZH2 Degrader-3 shows anti-proliferative activity and blocks the cell cycle in the G0-G1 phase and induces cell apoptosis((Blue: cereblon ligand Pomalidomide (HY-10984), Black: linker HY-W361751；Pink: EZH2 inhibitor Tazemetostat (HY-13803)).
    PROTAC EZH2 Degrader-3
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.