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-117540
    ZLD10A
    ZLD10A is a highly potent and selective EZH2 inhibitor with the activity of inhibiting H3K27 methylation. ZLD10A can inhibit wild-type and mutant EZH2 with nanomolar potency and has more than 1000-fold selectivity for the other 10 histone methyltransferases. ZLD10A inhibited cell proliferation of DLBCL cell lines in a concentration- and time-dependent manner, showing a potential antiproliferative effect. ZLD10A can be used in the study of EZH2 mutant lymphomas.
    ZLD10A
  • HY-125090
    PHA-680626
    		Inhibitor
    PHA-680626 is an effective inhibitor of the interaction between Aurora-A and N-Myc. PHA-680626 inhibits kinase activity of AURKA and Bcr-Abl, and induces N-Myc degradation. PHA-680626 decreases phosphorylation of CrkL and histone H3. PHA-680626 shows anti-proliferative and pro-apoptotic activity on Imatinib (HY-15463)-resistant chronic myeloid leukemia cell lines and primary CD34+ cells.
    PHA-680626
  • HY-12707C
    Piribedil hydrochloride
    		Inhibitor
    Piribedil hydrochloride is a potent and orally active dopamine D2 and dopamine D3 agonist. Piribedil hydrochloride is also a α2-adrenoceptors antagonist. Piribedil hydrochloride can inhibit MLL1 methyltransferase activity (EC50: 0.18 μM). Piribedil hydrochloride has the potential for the research of parkinson's disease, circulatory disorders, cancers.
    Piribedil hydrochloride
  • HY-155020
    Antitumor agent-101
    		Inhibitor
    Antitumor agent-101 is a selective covalent inhibitor of lysine methyltransferases G9a/GLP, with IC50s of 8.5 nM and 5.5 nM for G9a and GLP, respectively. Antitumor agent-101 shows antitumor efficacy in the PANC-1 xenograft model.
    Antitumor agent-101
  • HY-168142
    YD1130
    		Inhibitor
    YD1130 is a PRMT4 inhibitor (0.5 nM, 75% inhibition rate), and its inhibitory potency against other PRMTs is not significant (PRMT5 IC50> 1 μM, PRMT1/3/6/7/8 IC50 > 10 μM)..
    YD1130
  • 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-171119
    NSD2-PWWP1-IN-1
    		Inhibitor
    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-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 (IC50 6.87 nM) and EZH2 (IC50 36.51 nM) inhibitor for triple-negative breast cancer with wild-type BRCA.
    PARP/EZH2-IN-1
  • HY-161313
    DYB-03
    		Inhibitor 99.49%
    DYB-03 is an oral active HIF-1α/EZH2 inhibitor. DYB-03 inhibits migration, invasion, and angiogenesis of lung cancer cells and HUVECs in vitro and in vivo. DYB-03 induces apoptosis in 2-ME2- and GSK126-resistant of A549 and H460 cells.
    DYB-03
  • HY-171121
    NSD2-PWWP1-IN-3
    		Inhibitor
    NSD2-PWWP1-IN-3 (compound 36) is a potent NSD2-PWWP1 inhibitor with an IC50 value of 8.05 µM. NSD2-PWWP1-IN-3 has the potential for the research of cancer.
    NSD2-PWWP1-IN-3
  • HY-170494
    AS-254s
    		Inhibitor
    AS-254s is the inhibitor for absent, small, or homeotic-like 1 protein (ASH1L) with an IC50 of 94 nM (FP assay). AS-254s exhibits antiproliferative activity against MLL1-rearranged leukemic cells with GI50 <1 μM. AS-254s induces the differentiation of MLL1-r leukemic cell.
    AS-254s
  • HY-159728
    PROTAC PRMT3 degrader 1
    		Degrader
    PROTAC PRMT3 degrader 1 (compound 11) is a PROTAC degrader targeting PRMT3. PROTAC PRMT3 degrader 1 can inhibit the growth of acute leukemia cells.
    PROTAC PRMT3 degrader 1
  • HY-126300A
    SGC6870N
    SGC6870N is inactive against PRMT6 and can be utilized as a negative control. SGC6870N is an inactive enantiomer of SGC6870 (HY-126300).
    SGC6870N
  • 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-168035
    W4275
    		Inhibitor
    W4275 (Compound 42) is a selective NSD2 inhibitor with oral activity, showing an IC50 value of 17 nM. W4275 exhibits antiproliferative activity with an IC50 of 230 nM against RS411 cells and significantly inhibits tumor growth in the RS411 tumor xenograft model. Pharmacokinetic analysis in mice demonstrates that W4275 has good oral bioavailability (F of 27.34%). W4275 holds promise for use in cancer research.
    W4275
  • 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-139611B
    (S)-MRTX-1719
    		Inhibitor
    (S)-MRTX-1719 (example 16-7) is the S-enantiomer of MRTX-1719. (S)-MRTX-1719 is a PRMT5/MTA complex inhibitor, with an IC50 of 7070 nM.
    (S)-MRTX-1719
  • HY-156152
    CARM1 degrader-1
    		Inhibitor
    PROTAC CARM1 degrader-1 (compound 3b) is a degrader (DC50=8.1 nM) of co-activator associated argininemethyltransferase (CARM1). PROTAC CARM1 degrader-1 degrades CARM1 in a VHL- and proteasome-dependent manner. Thus, PROTAC CARM1 degrader-1 inhibits methylation of CARM1 substrates such as poly(A)-binding protein PABP1 and BGR1-associated factor BAF155 and inhibits breast cancer cell migration.
    CARM1 degrader-1
Cat. No. Product Name / Synonyms Application Reactivity
Histone Methyltransferase Isoform Comparison

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