2. シグナル伝達
  3. Epigenetics
  4. Histone Methyltransferase
  5. EHMT2/G9a/KMT1C Isoform

EHMT2/G9a/KMT1C

EHMT2, also known as G9a or KMT1C, is a euchromatic histone lysine methyltransferase that primarily catalyzes mono- and dimethylation of histone H3 lysine 9 (H3K9), thereby regulating gene expression and chromatin structure[1][2][3]. Mechanistically, EHMT2 forms heteromeric complexes with EHMT1/GLP and WIZ, facilitating transcriptional repression via coordinated H3K9 methylation and interaction with H3K4 demethylases[4][3]. In addition to canonical histone substrates, EHMT2 modulates non-histone proteins, including MyoD and p53, influencing myogenic differentiation and apoptosis pathways[5][6]. Compared with its paralog EHMT1, EHMT2 exhibits distinct substrate specificity, contributing selectively to DNA methylation at CpG-rich promoters and maintaining gene silencing in embryonic and adult tissues[2][7]. In disease contexts, EHMT2 overexpression is associated with poor prognosis in acute myeloid leukemia, neuroblastoma, Ewing sarcoma, and brain tumors, reflecting its role in tumor cell proliferation, chemoresistance, and epigenetic dysregulation[8][9][10][11]. Pharmacologic inhibition of EHMT2 using small-molecule inhibitors such as BIX-01294 reactivates autophagy-related genes, reprograms cancer-associated fibroblasts, and enhances the efficacy of immunotherapy, highlighting its potential as a therapeutic target[12][13][7]. Structurally, EHMT2 contains ankyrin repeats, a SET catalytic domain, and a cysteine-rich region mediating protein-protein interactions, distinguishing it functionally from EHMT1 and enabling selective targeting in experimental applications[14].

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EHMT2/G9a/KMT1C 関連製品 (27):

製品番号 製品名 製品効果 純度
  • HY-10587
    BIX-01294 Inhibitor 98.44%
    BIX-01294 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 inhibits G9a/GLP by competing for binding with the amino acids N-terminal of the substrate lysine residue. BIX-01294, a (1H-1,4-diazepin-1-yl)-quinazolin-4-yl amine derivative, induces necroptosis and autophagy. BIX-01294 has antitumor activity in recurrent tumor cells.
  • HY-13980
    UNC0642 Inhibitor 99.86%
    UNC0642, a chemical probe, is a potent and selective lysine methyltransferases G9a and GLP inhibitor, with an IC50 of <2.5 nM for G9a.
  • HY-15273
    UNC0638 Inhibitor 99.84%
    UNC0638, a chemical probe, selectively inhibits G9a and GLP histone methyltransferases with IC50 of 15 nM and 19 nM, respectively. UNC0638 inhibits TNBC cell invasion and migration in vitro. UNC0638 is also an inhibitor of EHMT1/2 and induces fetal hemoglobin (HbF) expression in human erythroid progenitor cell culture. In addition, UNC0638 has anti-FMDV (foot-and-mouth disease virus) and anti-VSV (vesicular stomatitis virus) activities, with excellent potency and selectivity against multiple epigenetic and non-epigenetic targets.
  • HY-12583
    A-366 Inhibitor 98.13%
    A-366, a chemical probe, is a potent, highly selective, peptide-competitive histone methyltransferase G9a inhibitor with IC50s of 3.3 and 38 nM for G9a and GLP (EHMT1), respectively. A-366 shows >1000-fold selectivity over 21 other methyltransferases. A-366 is also a potent, nanomolar inhibitor of the Spindlin1-H3K4me3-interaction (IC50=182.6 nM). A-366 displays high affinity at human histamine H3 receptor (Ki=17 nM) and shows subtype selectivity among subsets of the histaminergic and dopaminergic receptor families.
  • HY-101925
    CM-272 Inhibitor 98.70%
    CM-272 is a first-in-class, potent, selective, substrate-competitive and reversible dual G9a/DNA methyltransferases (DNMTs) inhibitor with antitumor activities. CM-272 inhibits G9a, DNMT1, DNMT3A, DNMT3B and GLP with IC50s of 8 nM, 382 nM, 85 nM, 1200 nM and 2 nM, respectively. CM-272 inhibits cell proliferation and promotes apoptosis, inducing IFN-stimulated genes and immunogenic cell death.
  • HY-183058
    EZM8266 Inhibitor 98.24%
    EZM8266 is an orally active and selective G9a (EHMT2) histone methyltransferase inhibitor with a human EHMT2 IC50 of 1 pM. EZM8266 reduces repressive H3K9me2 marks at immune-stimulatory gene and endogenous retroviral element promoters. EZM8266 reduces colony formation, migration, and invasion of cancer cells. EZM8266 enhances IFN-γ response, increases MHC class I expression, and enhances CXCL10-mediated T cell recruitment in cancer cells. EZM8266 can be used for the research of hepatocellular carcinoma.
  • HY-10929
    UNC0224 Inhibitor 98.93%
    UNC0224 is a potent and selective histone methyltransferase G9a inhibitor with a Ki of 2.6 nM, an IC50 of 15 nM and a Kd of 23 nM. UNC0224 also potently inhibits b>GLP with assay-dependent IC50 values of 20-58 nM. UNC0224 is inactive against SET7/9, SET8/PreSET7, PRMT3 and JMJD2E.
  • HY-13808
    UNC 0631 Inhibitor 99.27%
    UNC 0631 is a potent histone methyltransferase G9a inhibitor with an IC50 of 4 nM. UNC 0631 potently reduces H3K9me2 levels in MDA-MB-231 cells with an IC50 of 25 nM.
  • HY-16705
    BRD4770 Inhibitor 99.79%
    BRD4770 is a histone methyltransferase G9a inhibitor. BRD4770 reduces di- and trimethylation of lysine 9 on histone H3 (H3K9) with an EC50 of 5 μM, and has less or little effect toward H3K27me3, H3K36me3, H3K4me3, and H3K79me3. BRD4770 can activate the ataxia telangiectasia mutated (ATM) pathway and induce cell senescence.
  • HY-152775
    RK-701 Inhibitor 98.01%
    RK-701 is an highly selective and non-genotoxic inhibitor of G9a with IC50 value of 23-27 nM. RK-701 selectively up-regulates HbF, γ- Globin, BGLT3 expression, down-regulates H3K9me2 expression. RK-701 also has inhibition for BCL11A and ZBTB7A.
  • HY-141877
    MS4322 Degrader 99.14%
    MS4322 (YS43-22) is a specific PRMT5 PROTAC degrader. MS4322 reduces the PRMT5 protein level with a DC50 of 1.1 μM in MCF-7 cells. MS4322 inhibits the methyltransferase activity of PRMT5 with an IC50 of 18 nM. MS4322 promotes ubiquitination and degradation of PRMT5. MS4322 can be used for the research of breast cancer, lung cancer, and hepatocellular cancer. (Pink: PRMT5 ligand (HY-173092); Blue: E3 ligase ligand HY-112078); Black: linker (HY-124780); E3+linker (HY-173093 )).
  • HY-10930
    UNC0321 Inhibitor 99.91%
    UNC0321 is a potent and selective histone methyltransferase G9a inhibitor with a Ki of 63 pM and with assay-dependent IC50 values of 6-9 nM. UNC0321 also inhibits GLP with assay-dependent IC50 values of 15-23 nM. UNC0321 has anti-apoptotic activity and has potential application in diabetic vascular complications.
  • HY-111778
    EHMT2-IN-1 Inhibitor 99.85%
    EHMT2-IN-1 is a potent EHMT inhibitor, with IC50s of all <100 nM for EHMT1 peptide, EHMT2 peptide and cellular EHMT2. Used in the research of blood disorder or cancer.
  • HY-13807
    UNC0646 Inhibitor 99.38%
    UNC0646 is a potent and selective histone methyltransferase G9a inhibitor with an IC50 of 6 nM. UNC0646 is also a potent GLP inhibitor (IC50 <15 nM) and highly selective for G9a/GLP over SETD7, SUV39H2, SETD8 and PRMT3. UNC0646 reduces H3K9me2 levels in MDA-MB-231 cells with an IC50 of 26 nM.
  • HY-111904
    EHMT2-IN-2 Inhibitor 99.0%
    EHMT2-IN-2 is a potent EHMT inhibitor, with IC50s of all <100 nM for EHMT1 peptide, EHMT2 peptide and cellular EHMT2. Used in the research of blood disease or cancer.
  • HY-141877B
    MS4322 (isomer) 99.87%
    MS4322 (YS43-22) isomer is an isomer of MS4322. MS4322 is a specific PRMT5 PROTAC degrader. MS4322 reduces the PRMT5 protein level with a DC50 of 1.1 μM in MCF-7 cells. MS4322 inhibits the methyltransferase activity of PRMT5 with an IC50 of 18 nM. MS4322 promotes ubiquitination and degradation of PRMT5. MS4322 can be used for the research of breast cancer, lung cancer, and hepatocellular cancer. (Pink: PRMT5 ligand (HY-173092); Blue: E3 ligase ligand HY-112078); Black: linker (HY-124780); E3+linker (HY-173093 )).
  • HY-121093
    DC-S239 Inhibitor 99.73%
    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.
  • HY-15647
    BRD9539 Inhibitor 99.73%
    BRD9539 is a histone methyltransferase G9a inhibitor with an IC50 of 6.3 μM. BRD9539 also inhibits PRC2 activity and is inactive against SUV39H1, NSD2 and DNMT1.
  • HY-156285
    ZZM-1220 Inhibitor 98.74%
    ZZM-1220 is a histone lysine methyltransferase G9a/GLP covalent inhibitor with IC50s of of 458 nM and 924 nM, respectively. ZZM-1220 inhibits H3K9me2 in cells and significantly induces apoptosis of triple-negative breast cancer (TNBC) cells and blocks the cell cycle in the G2/M phase.
  • HY-100757
    CPUY074020 Inhibitor 98.56%
    CPUY074020 is a potent and oral bioavailable inhibitor of histone methyltransferase G9a, with an IC50 of 2.18 μM. CPUY074020 possesses anti-proliferative activity.