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-136977
    EEDi-5285
    		Inhibitor 99.87%
    EEDi-5285 is an exceptionally potent and orally active embryonic ectoderm development (EED) inhibitor with an IC50 value of 0.2 nM for binds to the EED protein. EEDi-5285 has anti-cancer activity.
    EEDi-5285
  • HY-117421A
    CM-579 trihydrochloride
    		Inhibitor
    CM-579 trihydrochloride is a first-in-class reversible, dual inhibitor of G9a and DNMT, with IC50 values of 16 nM, 32 nM for G9a and DNMT, respectively. Has potent in vitro cellular activity in a wide range of cancer cells.
    CM-579 trihydrochloride
  • HY-116804
    ZLD1039
    		Inhibitor 98.48%
    ZLD1039 is a potent, highly selective, and orally bioavailable EZH2 inhibitor. ZLD1039 shows potent and concentration-dependent inhibition of PRC2 enzymatic activity against EZH2 wild-type as well as Y641F, and A677G mutant enzymes with IC50 values of 5.6, 15, and 4.0 nM, respectively. ZLD1039 inhibits breast tumor growth and metastasis.
    ZLD1039
  • HY-122182
    OTS193320
    		Inhibitor 98.12%
    OTS193320, a imidazo[1,2-a]pyridine compound, is a SUV39H2 methyltransferase activity inhibitor. OTS193320 decreases global histone H3 lysine 9 tri-methylation levels in breast cancer cells and triggers apoptotic cell death. Combination of OTS193320 with Doxorubicin (HY-15142A) results in reduction of γ-H2AX levels as well as cancer cell viability compared to a single agent OTS193320 or DOX.
    OTS193320
  • HY-124101
    PDAT
    		Inhibitor 98.0%
    PDAT is a noncompetitive indolethylamine-N-methyltransferase (INMT) inhibitor with a Ki of 84 μM for rabbit lung INMT (rabINMT).
    PDAT
  • HY-100025A
    HLCL-61 hydrochloride
    		Inhibitor 99.87%
    HLCL-61 hydrochloride is a first-in-class inhibitor of protein arginine methyltransferase 5 (PRMT5).
    HLCL-61 hydrochloride
  • HY-100846
    JQEZ5
    		Inhibitor 98.14%
    JQEZ5 is a potent and selective EZH2 lysine methyltransferase inhibitor. JQEZ5 SAM-competitively inhibits polycomb repressive complex 2 (PRC2) with an IC50 of 80 nM. JQEZ5 has anti-tumor effects.
    JQEZ5
  • HY-100360
    MS049
    		Inhibitor 98.0%
    MS049, a chemical probe, is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively. MS049 reduces levels of Med12me2a and H3R2me2a in HEK293 cells. MS049 is not toxic and does not affect the growth of HEK293 cells.
    MS049
  • HY-135128
    Dot1L-IN-5
    		Inhibitor 99.82%
    Dot1L-IN-5 is a potent disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor with an IC50 of 0.17 nM.
    Dot1L-IN-5
  • HY-152038
    SPEN-IN-1
    		Inhibitor
    SPEN-IN-1 (compound X1) is an inhibitor of SPEN which is a protein factor with a Kd value of 47 nM. SPEN-IN-1 has high selectivity for RepA, a 431-nucleotide domain in Xist (a non-coding RNA prototype) that comprises 8.5 units of a GC-rich motif responsible for gene silencing.
    SPEN-IN-1
  • HY-138684
    MRTX9768
    		Inhibitor 99.60%
    MRTX9768 is a potent, selective, orally active, first-in-class PRMT5-MTA complex inhibitor.
    MRTX9768
  • HY-125292
    NV03
    		Antagonist 99.77%
    NV03 is a potent and selective antagonist of Ubiquitin-like with PHD and RING finger domains 1 (UHRF1)-H3K9me3 interaction by binding to UHRF1 tandem tudor domain, with a Kd of 2.4 μM. NV03 is also a ligand for E3 ligase. NV03 can be studied in anticancer research.
    NV03
  • HY-168035
    W4275
    		Inhibitor 98.93%
    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-W280124
    PRMT9-IN-1
    		Inhibitor 99.31%
    PRMT9-IN-1 is a PRMT9 inhibitor. PRMT9-IN-1 can be used in the research of hematological cancer.
    PRMT9-IN-1
  • HY-13803R
    Tazemetostat (Standard)
    		Inhibitor
    Tazemetostat (Standard) is the analytical standard of Tazemetostat. This product is intended for research and analytical applications. Tazemetostat (EPZ-6438) is a potent, selective and orally available EZH2 inhibitor. Tazemetostat inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a Ki value of 2.5 nM. Tazemetostat inhibits EZH2 with IC50s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat inhibits rat EZH2 with an IC50 of 4 nM. Tazemetostat also inhibits EZH1 with an IC50 of 392 nM. Tazemetostat induces apoptosis and differentiation specifically in SMARCB1-deleted MRT cells.
    Tazemetostat (Standard)
  • HY-12856
    GSK503
    		Inhibitor 99.52%
    GSK503 is a potent and specific inhibitor of EZH2 methyltransferase with Kiapp values of 3 to 27 nM.
    GSK503
  • HY-132309
    BRD0639
    		Inhibitor 98.04%
    BRD0639 is a first-in-class inhibitor of the PRMT5-substrate adaptor interaction. BRD0639 is a PRMT5 binding motif (PBM)-competitive agent that can support studies of PBM dependent PRMT5 activities.
    BRD0639
  • HY-108239
    BIX-01294 trihydrochloride
    		Inhibitor 99.68%
    BIX-01294 trihydrochloride is a reversible and highly selective G9a and GLP Histone Methyltransferase inhibitor, with IC50s of of 1.7 μM and 0.9 μM, respectively. BIX-01294 trihydrochloride inhibits G9a/GLP by competing for binding with the amino acids N-terminal of the substrate lysine residue. BIX-01294 trihydrochloride, a (1H-1,4-diazepin-1-yl)-quinazolin-4-yl amine derivative, induces necroptosis and autophagy. BIX-01294 trihydrochloride has antitumor activity in recurrent tumor cells.
    BIX-01294 trihydrochloride
  • HY-160924
    MS147
    		98.31%
    MS147 is a VHL-based PROTAC degrader of BMI1 and RING1B (polycomb repressive complex 1 core components). MS147 directly binds EED and VHL E3 ligase, recruiting the ligase to the EED-BMI1/RING1B complex to induce time-dependent, ubiquitination-mediated degradation of BMI1 and RING1B. MS147 reduces histone H2A Lys119 mono-ubiquitination without altering histone H3 Lys27 tri-methylation and inhibits cancer cells proliferation. MS147 can be used for the research of cancer, such as chronic myelogenous leukemia and b-cell lymphoma. (Pink: BMI1/RING1B ligand (HY-183634); Blue: VHL ligand (HY-125845); Black: linker)
    MS147
  • HY-156152A
    CARM1 degrader-1 hydrochloride
    		Degrader
    CARM1 degrader-1 hydrochloride is a CARM1 PROTAC degrader (DC50 = 8.1 nM) with high selectivity over other protein arginine methyltransferases. CARM1 degrader-1 hydrochloride degrades CARM1 in a VHL- and proteasome-dependent manner. CARM1 degrader-1 hydrochloride downregulates the methylation level of CARM1 substrates in cell-based assays. CARM1 degrader-1 hydrochloride inhibits cancer cell migration in cell-based assays. CARM1 degrader-1 hydrochloride can be used in breast cancer research.
    CARM1 degrader-1 hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
Histone Methyltransferase Isoform Comparison

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