2. Vías de señalización
  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. Nombre del producto Efecto Pureza Chemical Structure
  • HY-174445
    C199
    		Degrader
    C199 is a PROTAC degrader targeting PRMT4 (DC50 = 106 nM). C199 shows high selectivity for PRMT4 over other protein arginile methyltransferases. C199 exhibits strong cell degradation ability. C199 induces apoptosis in MM cell lines. C199 efficiently clears PRMT4 protein via the VHL-proteasome pathway. C199 has a relatively long half-life and shows strong anti-multiple myeloma (MM) tumor activity (Pink: Target protein ligand (HY-111109); Blue: E3 ligase ligand (HY-112078), E3 ligase ligand + linker (HY-174474); black: Linker).
    C199
  • HY-110196
    (S)-PFI-2 hydrochloride
    		Inhibitor
    (S)-PFI-2 hydrochloride is an inhibitor of lysine methyltransferase SETD7 and is approximately 500-fold more active than its enantiomer (R)-PFI-2. (R)-PFI-2 is a cofactor-dependent and substrate-competitive inhibitor. (R)-PFI-2 can occupy the substrate peptide binding groove of SETD7 (including the catalytic lysine binding channel) and interact with the cofactor The donor methyl group is in direct contact. However, (S)-PFI-2 was not observed to have the same interaction as (R)-PFI-2.
    (S)-PFI-2 hydrochloride
  • HY-110158
    UNC2327
    		Inhibitor 99.70%
    UNC2327 is an allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3).
    UNC2327
  • HY-122640
    NPD13668
    		Inhibitor
    NPD13668 is an EZH2-mediated gene silencing modulator. NPD13668 inhibits EZH2/PRC2 (polycomb repressive complex 2) activity. NPD13668 reactivates the expression of silenced H3K27me3 target genes together with depletion of the H3K27me3 modification. NPD13668 can be used for the study of prostate cancer and ovarian cancer.
    NPD13668
  • HY-162939
    TB22
    		Inhibitor
    TB22 is a non-nucleoside inhibitor of DOT1LR231Q, possessing anticancer activity. TB22 inhibits the malignant phenotype of lung cancer cells carrying the R231Q mutation through the MAPK/ERK signaling pathway, and can be used for lung cancer research.
    TB22
  • HY-143616
    EZH2-IN-7
    		Inhibitor
    EZH2-IN-7 is a potent inhibitor of EZH2. EZH2 overexpression or mutations in the SET region (Y641F, Y641N, A687V, A677G point mutations) all lead to abnormal elevation of H3K27me3 and promote the growth and development of many types of tumors, such as breast cancer, prostate cancer, leukemia, etc. EZH2-IN-7 has the potential for the research of cancer diseases (extracted from patent WO2021129629A1, compound 259).
    EZH2-IN-7
  • HY-10427
    WAY-260022
    WAY-260022 is a selective norepinephrine reuptake inhibitor with potent inhibitory activity on norepinephrine reuptake. WAY-260022 exhibits excellent selectivity in inhibiting serotonin and dopamine transporters. WAY-260022 also showed oral efficacy in a rat model of thermoregulatory dysfunction.
    WAY-260022
  • HY-152775A
    RK-0133114
    		Inhibitor
    RK-0133114 is a G9a inhibitor and a R-enantiomer of RK-701 (HY-152775). RK-0133114 inhibits G9a with an IC50 value of 3.7 μM. RK-0133114 can be used for the research of sickle cell disease (SCD).
    RK-0133114
  • HY-181320
    PROTAC EZH2 Degrader-19
    		Degrader
    PROTAC EZH2 Degrader-19 (compound 6) is a is a PROTAC protein degrader targeting EZH2 with an IC50 of 15.00 nM. PROTAC EZH2 Degrader-19 induces strong degradation of all PRC2 subunits (EZH2, SUZ12, EED, RbAp48) in a concentration- and time-dependent manner.PROTAC EZH2 Degrader-19 exhibits antiproliferative effects in cancer cells.PROTAC EZH2 Degrader-19 can be used for the research of cancer.
    PROTAC EZH2 Degrader-19
  • HY-169708
    PRMT5-IN-49
    		Inhibitor
    PRMT5-IN-49 (Compound 4b16) is an inhibitor of PRMT5.
    PRMT5-IN-49
  • HY-155818
    NSD2-IN-4
    		Inhibitor
    NSD2-IN-4 is a potent and selective NSD2-SET inhibitor. NSD2-IN-4 has the potential for NSD2-related diseases.
    NSD2-IN-4
  • HY-139823A
    PRMT5-IN-11
    		Inhibitor
    PRMT5-IN-11 is a promising structure-dependent inhibition of the protein methyltransferase PRMT5:MEP50 complex in the (sub)micromolar range.
    PRMT5-IN-11
  • HY-181391
    PROTAC EZH2 Degrader-34
    PROTAC EZH2 Degrader-34 (compound E7 (13)) is an EZH2-target PROTAC degrader with a human EZH2 IC50 of 6.30 μM. PROTAC EZH2 Degrader-34 can be used for the research of pfeiffer cancer, prostate cancer.
    PROTAC EZH2 Degrader-34
  • HY-155817
    UNC7096
    		Chemical
    UNC7096 (compound 53) is a biotinylated affinity reagent. The phenyl ring of UNC7096 replaces the pyrimidine ring in UNC6934 (HY-145103) and introduces biotin at the para position of the phenyl ring, which has a high binding affinity to the NSD2-PWWP1 domain (Kd=46 nM). UNC7096 blocks the interaction between NSD2-PWWP1 and nucleosomal H3K36me2 by occupying the methyl-lysine binding pocket of NSD2-PWWP1. This binding is achieved by covalent binding through the formation of hydrogen bonds and a specific aromatic cage structure. UNC7096 can be used to capture proteins that interact with the NSD2-PWWP1 domain to further analyze the biological significance of these interactions.
    UNC7096
  • HY-181306
    PROTAC EZH2 Degrader-11
    		Degrader
    PROTAC EZH2 Degrader-11 (compound 2) is a EZH2-targeting PROTAC protein degrader. PROTAC EZH2 Degrader-11 reduces tumor size and viability in 3D spheroid models. PROTAC EZH2 Degrader-11 can be used for the research of cancer.
    PROTAC EZH2 Degrader-11
  • HY-181414
    PROTAC EZH2 Degrader-45
    		Degrader
    PROTAC EZH2 Degrader-45 (compound 61) is a PROTAC protein degrader targeting EZH2 with an IC50 of 22.97 μM in SU-DHL-6 cells. PROTAC EZH2 Degrader-45 can be used for the research of diffuse large b-cell lymphoma.
    PROTAC EZH2 Degrader-45
  • HY-115619
    EPZ004777 formate
    		Inhibitor
    EPZ004777 formate is an effective and selective DOT1L inhibitor, with IC50 being 0.4 nM. EPZ004777 formate reduces the levels of H3K79me2 and H3K79me1, significantly down-regulating the expression of HOXA9 and MEIS1. EPZ004777 formate selectively inhibits the proliferation of MLL rearrangement cells and promotes the differentiation and subsequent apoptosis (apoptosis) of leukemia cells. EPZ004777 formate can be used for the study of leukemia.
    EPZ004777 formate
  • HY-172732
    PRMT5-IN-50
    		Inhibitor
    PRMT5-IN-50 is an orally active and selective inhibitor of PRMT5. PRMT5-IN-50 has good metabolic stability and low clearance rate in human liver microsomes. PRMT5-IN-50 inhibits SDMA/HCT116-MTAPdel and SDMA/HCT116-MTAPwt with IC50s value of 1.0, 536 nM for arginine symmetric methylation, 19, 1620 nM for anti-proliferation, respectively. PRMT5-IN-50 inhibits tumor growth in mice.
    PRMT5-IN-50
  • HY-182298
    PRMT1 ligand-Linker Conjugate 1
    		Ligand
    PRMT1 ligand-Linker Conjugate 1 is a target protein ligand-linker conjugate containing a PRMT1 ligand (HY-182297) and a PROTAC linker, which recruits E3 ligases. PRMT1 ligand-Linker Conjugate 1 can be used to synthesize PROTAC PRMT1 degrader-1 (HY-182275).
    PRMT1 ligand-Linker Conjugate 1
  • HY-115758
    PRMT1-IN-1
    		Inhibitor
    PRMT1-IN-1 is a PRMT1 inhibitor.
    PRMT1-IN-1
Cat. No. Nombre del producto / 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.