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-161024
    AC1Q3QWB
    		Inhibitor 99.39%
    AC1Q3QWB upregulates CDKN1A and SOX17 by interrupting the HOTAIR-EZH2 interaction and enhances the efficacy of Tazemetostat in endometrial cancer.
    AC1Q3QWB
  • HY-162308
    NSD-IN-3
    		Inhibitor ≥98.0%
    NSD-IN-3 (compound 3) is a potent nuclear receptor binding SET domain (NSD) inhibitor. NSD-IN-3 inhibits NSD2-SET and NSD3-SET with IC50 values of 0.81 μM and 0.84 μM, respectively. NSD-IN-3 inhibits histone H3K36 dimethylation and decreases the expression of NSDs-targeted genes in non-small cell lung cancer cells. NSD-IN-3 induces s-phase cell cycle arrest and apoptosis.
    NSD-IN-3
  • HY-A0298
    EZH2-IN-2
    		Inhibitor 99.40%
    EZH2-IN-2 is a EZH2 inhibitor extracted from patent WO2018133795A1, Compound Example 69, with an IC50 of 64 nM. EZH2-IN-2 can be used for the research of cancer or precancerous condition related to EZH2 activity.
    EZH2-IN-2
  • 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-120137
    CMP-5
    		Inhibitor 99.02%
    CMP-5 is a potent, specific, and selective PRMT5 inhibitor, while displays no activity against PRMT1, PRMT4, and PRMT7 enzymes. CMP-5 selectively blocks S2Me-H4R3 by inhibiting PRMT5 methyltransferase activity on histone preparations. CMP-5 prevents Epstein-Barr virus (EBV)-driven B-lymphocyte transformation but leaving normal B cells unaffected.
    CMP-5
  • HY-155815
    MS9715
    		Inhibitor
    MS9715 is a potent and seletive NSD3-targeting PROTAC. MS9715 is designed by BI-9321, which binds NSD3’s PWWP1 domain, with an E3 ligase VHL ligand. MS9715 has the potental for NSD3-dependent cancer treatment research.
    MS9715
  • HY-101508
    GNA002
    		Inhibitor 98.02%
    GNA002 is a highly potent, specific and covalent EZH2 (Enhancer of zeste homolog 2) inhibitor with an IC50 of 1.1 μM. GNA002 can specifically and covalently bind to Cys668 within the EZH2-SET domain, triggering EZH2 degradation through COOH terminus of Hsp70-interacting protein (CHIP)-mediated ubiquitination. GNA002 efficiently reduces EZH2-mediated H3K27 trimethylation, reactivates polycomb repressor complex 2 (PRC2)-silenced tumor suppressor genes.
    GNA002
  • 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-136188
    UNC2399
    		Inhibitor 99.62%
    UNC2399, a biotinylated UNC1999, is a selective EZH2 inhibitor, maintaining high in vitro potency for EZH2, with an IC50 of 17 nM.
    UNC2399
  • HY-107777A
    LLY-284
    		Control 99.11%
    LLY-284 is the diastereomer of LLY-283 with much less active. LLY-283 is a potent inhibitor of PRMT5. LLY-284 has the potential for the research of cancer diseases.
    LLY-284
  • HY-132970
    EED ligand 1
    		Inhibitor 99.93%
    EED ligand 1 is a diverse, potent, and efficacious inhibitor that target the EED subunit of the polycomb repressive complex 2 (PRC2) methyltransferase.
    EED ligand 1
  • HY-109963
    PR5-LL-CM01
    		Inhibitor 98.45%
    PR5-LL-CM01 is a potent protein arginine methyltransferase 5 (PRMT5) inhibitor (IC50= 7.5 μM). Anti-tumor activies.
    PR5-LL-CM01
  • HY-P2254
    H3K27(Me3) (15-34)
    H3K27(Me3) (15-34), a histone peptide, is a repressive chromatin mark derived from human histone. Polycomb Repressive Complex 2 (PRC2) is a multiprotein complex that catalyzes the methylation of H3K27(Me).
    H3K27(Me3) (15-34)
  • HY-111418
    EBI-2511
    		Inhibitor 99.81%
    EBI-2511 is a highly potent and orally active EZH2 inhibitor, with an IC50 of 6 nM in Pfeffiera cell lines, respectively.
    EBI-2511
  • HY-128717
    GSK3368715
    		Inhibitor 99.24%
    GSK3368715 (EPZ019997) is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50=3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). GSK3368715 (EPZ019997) produces a shift in arginine methylation states, alters exon usage, and has strong anti-cancer activity.
    GSK3368715
  • HY-12759A
    CARM1-IN-1 hydrochloride
    		Inhibitor
    CARM1-IN-1 (compound 7g) hydrochloride is a highly potent and selective inhibitor of CARM1 (IC50=8.6 μM, CARM1/PABP1), with low inhibitory activity against PRMT1 and SET7 (IC50 >667 μM). CARM1-IN-1 hydrochloride inhibits the methylation activity of CARM1 and the methylation levels of different substrates, such as PABP1, CA150, SmB, and H3. CARM1-IN-1 hydrochloride also inhibits the promoter activity of prostate-specific antigen (PSA) without significant cytotoxicity.
    CARM1-IN-1 hydrochloride
  • HY-121093
    DC-S239
    		Inhibitor 99.43%
    DC-S239 is a selective histone methyltransferase SET7 inhibitor with an IC50 value of 4.59 μM. DC-S239 also displays selectivity for DNMT1, DOT1L, EZH2, NSD1, SETD8 and G9a. DC-S239 has anticancer activity.
    DC-S239
  • HY-141539A
    SETDB1-TTD-IN-1 TFA
    		99.77%
    SETDB1-TTD-IN-1 TFA is a potent, selective and endogenous binder competitive ligand of SET domain bifurcated protein 1 tandem tudor domain (SETDB1-TTD) that binds to TTD, with a Kd of 88 nM. SETDB1-TTD-IN-1 TFA increases SETDB1 methyltransferase activity. SETDB1-TTD-IN-1 TFA can be used for the research of biological functions and disease associations of SETDB1-TTD.
    SETDB1-TTD-IN-1 TFA
  • HY-120444
    MS0124
    		Inhibitor 99.79%
    MS0124 is a potent selective G9a-like protein (GLP) inhibitor with IC50 values of 13±4 nM and 440±63 nM for GLP and G9a,respectively.
    MS0124
  • HY-147185
    PRMT7-IN-1
    		Inhibitor 98.70%
    PRMT7-IN-1 (Compound 14) is a PRMT7 inhibitor with an IC50 of 2.1 μM. PRMT7-IN-1 shows anticancer activity against different cancer cells.
    PRMT7-IN-1
Cat. No. Product Name / Synonyms Application Reactivity
Histone Methyltransferase Isoform Comparison

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