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-128717C
    GSK3368715 hydrochloride
    		Inhibitor
    GSK3368715 (EPZ019997) hydrochloride is an orally active, reversible, SAM-noncompetitive type I protein arginine methyltransferase (PRMT) inhibitor with IC50 values of 3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), and 1.7 nM (PRMT8). GSK3368715 hydrochloride induces a shift in arginine methylation states, alters exon usage, and exhibits potent anticancer activity.
    GSK3368715 hydrochloride
  • HY-152228
    SMYD3-IN-2
    		Inhibitor
    SMYD3-IN-2 is a SMYD3 inhibitor against gastric cancer via inducing lethal autophagy. SMYD3-IN-2 has inhibitory for SMYD3 and BGC823 cells with IC50 values of 0.81 μM and 0.75 μM, respectively. SMYD3-IN-2 can be used for the research of cancer.
    SMYD3-IN-2
  • HY-141875
    PRMT5-IN-13
    		Inhibitor
    PRMT5-IN-13 is a selective inhibitor of protein arginine methyltransferase 5 (prmt5).
    PRMT5-IN-13
  • HY-132885
    PARP/EZH2-IN-1
    		Inhibitor
    PARP/EZH2-IN-1 is a first-in-class dual PARP-1/EZH2 inhibitor with IC50 values of 6.87 nM and 36.51 nM, respectively. PARP/EZH2-IN-1 induces autophagy in cancer cells and shows potent antiproliferative activity in BRCA wild-type triple-negative breast cancer cells.
    PARP/EZH2-IN-1
  • HY-181294
    PRMT5-IN-55
    		Inhibitor
    PRMT5-IN-55 is an inhibitor of PRMT5 with a pIC50 value of 9.6 at a 10 nM enzyme.
    PRMT5-IN-55
  • HY-179650
    NSD2-PWWP1-IN-5
    		Inhibitor
    NSD2-PWWP1-IN-5 (Compound 13) is an effective NSD2-PWWP1 inhibitor with a Kd value of 78 nM. NSD2-PWWP1-IN-5 competitively blocks the recognition of H3K36me2 and DNA by NSD2-PWWP1, thereby weakening its binding ability to nucleosomes. NSD2-PWWP1-IN-5 inhibits the proliferation of U2OS osteosarcoma cells and induces cell cycle arrest and apoptosis. NSD2-PWWP1-IN-5 can be used for the study of osteosarcoma.
    NSD2-PWWP1-IN-5
  • HY-175821
    PRMT1-IN-3
    		Inhibitor
    PRMT1-IN-3 is a potent protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 4.11 μM. PRMT1-IN-3 inhibits PRMT6 and PRMT8 with IC50s of 23.3 and 30.1 μM. PRMT1-IN-3 suppresses asymmetric dimethylarginine (ADMA) levels and histone H4R3me2a modification in triple-negative breast cancer (TNBC) cells. PRMT1-IN-3 induces cell cycle arrest, apoptosis, and inhibits migration and colony formation in MDA-MB-231 cells. PRMT1-IN-3 acts as chemotherapeutic sensitizers for Paclitaxel (HY-B0015). PRMT1-IN-3 can be used for the study of TNBC.
    PRMT1-IN-3
  • HY-148641
    ZJH-16
    		Inhibitor
    ZJH-16 (Compound 11e) is an orally active EED inhibitor (IC50 = 2.72 nM, Kd = 4.4 nM). ZJH-16 inhibits the growth of lymphoma cells and reduces H3K27 trimethylation levels. ZJH-16 inhibits tumor growth in lymphoma animal models. ZJH-16 can be used for research on lymphoma and other cancers.
    ZJH-16
  • HY-168082
    Dot1L-IN-8
    		Inhibitor
    Dot1L-IN-8 (Compound 15) is a potent Dot1L inhibitor. Dot1L-IN-8 inhibits HL-60, K562, MV4-11, HH, and KG-1 cells vitality with IC50s of 0.45, 1.03, 0.68, 1.66, and 1.12 μM, respectively.
    Dot1L-IN-8
  • HY-157151
    iPRMT1
    		Inhibitor
    iPRMT1 is a potent and selective PRMT1 inhibitor for breast cancer research. iPRMT1 inhibits breast cancer cell growth in vitro and in vivo with EC50 values of 90, 70, and 9 nM in MCF7, T47D, and MDA-MB-231 cells, respectively.
    iPRMT1
  • HY-156152
    CARM1 degrader-1
    		Inhibitor
    CARM1 degrader-1 is a CARM1 PROTAC degrader (DC50 = 8.1 nM) with high selectivity over other protein arginine methyltransferases. CARM1 degrader-1 degrades CARM1 in a VHL- and proteasome-dependent manner. CARM1 degrader-1 downregulates the methylation level of CARM1 substrates in cell-based assays. CARM1 degrader-1 inhibits cancer cell migration in cell-based assays. CARM1 degrader-1 can be used for the research of breast cancer.
    CARM1 degrader-1
  • HY-100832A
    UNC3866 TFA
    		Inhibitor
    UNC3866 TFA is a potent antagonist of the CBX7-H3 interaction as determined by AlphaScreen (IC50=66±1.2 nM) and is more than 100-fold selective for CBX7 over the other nine members of this methyl-lysine (Kme) reader panel.
    UNC3866 TFA
  • HY-158158
    CARM1-IN-5
    		Inhibitor
    CARM1-IN-5 (Compound 17e) is a potent and selective inhibitor of CARM1 (IC50= 2 nM). CARM1-IN-5 effectively prevents CARM1 from methylating substrate proteins by directly interacting with CARM1. CARM1-IN-5 exhibits significant antiproliferative effects on melanoma cell lines.
    CARM1-IN-5
  • HY-162989
    PRMT5-MTA-IN-2
    		Inhibitor
    PRMT5-MTA-IN-2 (compund 1) is a MTA co-inhibitor of PRMT5 with IC50 less than 1.5 nM.
    PRMT5-MTA-IN-2
  • HY-181787
    DOT1L705
    		Inhibitor
    DOT1L705 is a PROTAC degrader that targets DOT1L. DOT1L705 recruits the VHL E3 ubiquitin ligase to induce proteasomal degradation of DOT1L. DOT1L705 reduces the viability of leukemia cells. DOT1L705 inhibits H3K79 methylation. DOT1L705 can be used in studies related to MLL-rearranged leukemia.
    DOT1L705
  • HY-W657887
    GSK-3β/G9a-IN-1
    		Inhibitor
    GSK-3β/G9a-IN-1 (Compound T2) is an orally active, selective, blood-brain-barrier permeable, competitive G9a (substrate-competitive, IC50: 1.1 μM) and GSK-3β (ATP competitive, IC50: 0.8 μM) inhibitor. GSK-3β/G9a-IN-1 is a potent H3K9me2 inhibitor that reshapes chromatin landscape. GSK-3β/G9a-IN-1 lowers tau phosphorylation, reduces Aβ aggregation. GSK-3β/G9a-IN-1 displays inhibition toward glucocorticoid receptor, androgen receptor, and alpha-2A adrenergic receptor. GSK-3β/G9a-IN-1 also upregulates SAGA complex members such as Eny2 and Sgf29. GSK-3β/G9a-IN-1 markedly improves memory, restores social behaviors, and increases synaptic complexity in late-onset Alzheimer’s disease.
    GSK-3β/G9a-IN-1
  • HY-168263
    PRMT5-IN-45
    		Inhibitor
    PRMT5-IN-45 (compound 36) is a potent and selective PRMT5 inhibitor with an IC50 of 3 nM. PRMT5-IN-45 potently reduces the level of symmetric dimethylarginines (sDMA) and inhibits the proliferation of MOLM-13 cell lines by inducing apoptosis and cell cycle arrest.
    PRMT5-IN-45
  • HY-153422
    PRMT5-IN-29
    		Inhibitor 98.01%
    PRMT5-IN-29 is a potent and orally active PRMT5 Inhibitor with an IC50 of 1.5 μΜ. PRMT5-IN-29 has the potential for advanced cancers research.
    PRMT5-IN-29
  • HY-168497
    C-MS023
    		Inhibitor
    C-MS023 is a photo-activatable MS023 (HY-19615) prodrug, achieving spatiotemporal inhibition of Histone Arginine Asymmetric Dimethylation. C-MS023 inhibits PRMT6 mediated asymmetric dimethylation of H3 arginine 2 (H3R2me2a), with an estimate IC50 of 0.2224 μM. The photolysis of C-MS023 could be triggered by visible light irradiation at 420 nm, thereby liberating MS023 for effective downregulation of histone arginine asymmetric dimethylation and DNA replication-related transcriptomic activities.
    C-MS023
  • HY-122746
    E67-2
    		Inhibitor
    E67-2, as the E67 derivative, is a low-toxicity, selective KIAA1718 Jumonji domain inhibitor with an IC50 value of 3.4 µM. E67-2 selectively inhibits histone H3 lysine 9 (H3K9) Jumonji demethylase as well as histone H3 lysine 4 (H3K4) demethylase.
    E67-2
Cat. No. Product Name / Synonyms Application Reactivity
Histone Methyltransferase Isoform Comparison

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