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-126256A
    PRMT5-IN-1 hydrochloride
    		Inhibitor 99.50%
    PRMT5 IN-1 hydrochloride (compound 9), a hemiaminal, is a potent, selective protein arginine methyltransferase 5 (PRMT5) inhibitor with an IC50 of 11 nM for PRMT5/MEP50. PRMT5 IN-1 hydrochloride can be converted to aldehydes and react with C449 to form covalent adducts under physiological conditions.
    PRMT5-IN-1 hydrochloride
  • HY-141429
    AS-99 free base
    		Inhibitor
    AS-99 is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 µM, Kd= 0.89 µM) with anti-leukemic activity. AS-99 blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo.
    AS-99 free base
  • HY-B1322AS
    Amodiaquine-d10
    		Inhibitor
    Amodiaquine-d10 is the deuterium labeled Amodiaquine. Amodiaquine (Amodiaquin), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC50 of ~20 μM. Anti-inflammatory effect[1][2][3][4].
    Amodiaquine-d<sub>10</sub>
  • HY-141797
    MS33
    		Inhibitor
    MS33 is a potent WDR5 degrader, with Kds of 870 nM and 120 nM for VCB and WDR5, respectively. MS33 induces WDR5 degradation in an E3 ligase VHL, and proteasome-dependent manner. MS33 can be used for the research of acute myeloid leukemia.
    MS33
  • HY-125244
    LEM-14-1189
    		Inhibitor 99.57%
    LEM-14-1189, a LEM-14 (HY-114340) derivative, is a NSDs inhibitor with IC50s of 418 μM (NSD1), 111 μM (NSD2), and 60 μM (NSD3), respectively. The NSDs, histone lysine methyltransferases (HMTases), are oncoproteins, drivers of a number of tumors. LEM-14-1189 can be used for multiple myeloma (MM) research.
    LEM-14-1189
  • 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
  • HY-111213
    PRMT5-IN-20
    		Inhibitor 99.20%
    PRMT5-IN-20 is a selective protein arginine methyltransferase 5 (PRMT5) inhibitor with anti-tumor activity.
    PRMT5-IN-20
  • HY-100869B
    MM-589 (racemic mixture ) (TFA)
    		Inhibitor 99.83%
    MM-589 (racemic mixture) TFA, is a racemic mixture of MM-589 TFA (HY-100869A). MM-589 TFA is a potent inhibitor of WD repeat domain 5 (WDR5) and mixed lineage leukemia (MLL) protein-protein interaction. MM-589 binds to WDR5 with an IC50 of 0.90 nM and inhibits the MLL H3K4 methyltransferase activity with an IC50 of 12.7 nM.
    MM-589 (racemic mixture ) (TFA)
  • HY-152242
    YEATS4-IN-1
    YEATS4-IN-1 (Compound 4d) is a potent and selective YEATS4 binder that binds to the KAc recognition site of the YEATS structural domain with a Ki value of 33 nM.
    YEATS4-IN-1
  • HY-100967
    SKF 91488 dihydrochloride
    		Inhibitor 98.62%
    SKF 91488 (Homodimaprit) dihydrochloride is a potent and noncompetitive histamine N-methyltransferase inhibitor with a Ki value of 0.9 microM. SKF 91488 dihydrochloride inhibits the methylation of labeled histamine in mice.
    SKF 91488 dihydrochloride
  • HY-157388
    CARM1/HDAC2-IN-1
    		Inhibitor
    CARM1/HDAC2-IN-1 (compound CH-1) is a dual inhibitor against CARM1 and HDAC2, with IC50 values of 3.71 nM and 4.07 nM, respectively. CARM1/HDAC2-IN-1 possesses antitumor activity.
    CARM1/HDAC2-IN-1
  • HY-117421
    CM-579
    		Inhibitor
    CM-579 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
  • HY-126327A
    UNC4976 TFA
    		Antagonist ≥98.0%
    UNC4976 TFA is a positive allosteric modulator (PAM) peptidomimetic of CBX7 chromodomain binding to nucleic acids. UNC4976 TFA simultaneously antagonizes H3K27me3-specific recruitment of CBX7 to target genes while increasing non-specific binding to DNA and RNA.
    UNC4976 TFA
  • HY-114211
    SGC8158
    		Inhibitor
    SGC8158 is an inhibitor of PRMT7 and can be used to study the cellular function of PRMT7. SGC8158 decreases monomethylarginine levels of Hsp70 (the best characterized PRMT7 substrate). SGC8158 induces growth inhibition in various cancer cells (IC50: 2-9 μM), as well as multidrug-resistant (MDR) cancer cells. SGC8158 also enhances Doxorubicin (HY-15142A) induced DNA damage and Its cytotoxicity.
    SGC8158
  • HY-146999
    YM458
    		Inhibitor 99.16%
    YM458 is a potent EZH2 and BRD4 dual inhibitor with IC50s of 490 nM and 34 nM, respectively. YM458 inhibits cell proliferation and colony formation and induces cell cycle arrest and apoptosis in solid cancer cells. YM458 can be used for researching anticancer.
    YM458
  • HY-134883
    PRMT5-IN-4
    		Inhibitor ≥99.0%
    PRMT5-IN-4 (compound AAA-1) is a PRMT5 inhibitor.
    PRMT5-IN-4
  • HY-150403
    XF067-68
    		Inhibitor 99.56%
    XF067-68 is a PROTAC for targeted degradation of WD40 repeat domain protein 5 (WDR5) (extracted from patent WO2019246570A1).
    XF067-68
  • HY-152236
    PRMT6-IN-3
    		Inhibitor 99.66%
    PRMT6-IN-3 (compound 25) is a selective PRMT6 inhibitor with an IC50 value of 192 nM. PRMT6-IN-3 can induce apoptosis in cancer cells and has anticancer activity.
    PRMT6-IN-3
  • HY-111390
    Dot1L-IN-2
    		Inhibitor
    Dot1L-IN-2 is a potent, selective and orally bioavailable inhibitor of Dot1L (a histone methyltransferase), with an IC50 and Ki of 0.4 nM and 0.08 nM, respectively.
    Dot1L-IN-2
Cat. No. Product Name / Synonyms Application Reactivity
Histone Methyltransferase Isoform Comparison

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