Target type: molecularfunction
Catalysis of the reaction: N6,N6-dimethyl-L-lysyl9-[histone H3] + S-adenosyl-L-methionine = H+ + N6,N6,N6-trimethyl-L-lysyl9-[histone H3] + S-adenosyl-L-homocysteine. This reaction is the addition of a single methyl group to the dimethylated lysine residue at position 9 of histone H3, producing histone H3K9me3. [RHEA:60280]
Histone H3K9me2 methyltransferase activity is a molecular function that involves the enzymatic transfer of two methyl groups to the lysine 9 residue of histone H3. This methylation event is catalyzed by histone H3K9 methyltransferases, which belong to a family of enzymes known as SET domain-containing proteins. The addition of methyl groups to histone H3K9 alters the local chromatin structure, influencing gene expression and other cellular processes. Histone H3K9me2 methylation is associated with transcriptional repression, heterochromatin formation, and DNA repair. The mechanism of histone H3K9me2 methyltransferase activity involves the recognition of a specific histone tail sequence, the binding of S-adenosyl-L-methionine (SAM), a methyl donor, and the transfer of two methyl groups from SAM to the lysine 9 residue of histone H3. The resulting di-methylation of histone H3K9 recruits other proteins, such as HP1, that contribute to the formation of compact chromatin structures, which hinder the access of transcription factors to DNA. Histone H3K9me2 methyltransferase activity plays a crucial role in maintaining genomic stability, regulating gene expression, and orchestrating diverse cellular processes.'
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| Protein | Definition | Taxonomy |
|---|---|---|
| Histone-lysine N-methyltransferase EHMT1 | A histone-lysine N-methyltransferase, H3 lysine-9 specific 5 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9H9B1] | Homo sapiens (human) |
| Histone-lysine N-methyltransferase EHMT2 | A histone-lysine N-methyltransferase, H3 lysine-9 specific 3 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q96KQ7] | Homo sapiens (human) |
| Histone-lysine N-methyltransferase SETDB1 | A histone-lysine N-methyltransferase SETDB1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q15047] | Homo sapiens (human) |
| Compound | Definition | Classes | Roles |
|---|---|---|---|
| disulfiram | organic disulfide; organosulfur acaricide | angiogenesis inhibitor; antineoplastic agent; apoptosis inducer; EC 1.2.1.3 [aldehyde dehydrogenase (NAD(+))] inhibitor; EC 3.1.1.1 (carboxylesterase) inhibitor; EC 3.1.1.8 (cholinesterase) inhibitor; EC 5.99.1.2 (DNA topoisomerase) inhibitor; ferroptosis inducer; fungicide; NF-kappaB inhibitor | |
| ebselen | ebselen : A benzoselenazole that is 1,2-benzoselenazol-3-one carrying an additional phenyl substituent at position 2. Acts as a mimic of glutathione peroxidase. | benzoselenazole | anti-inflammatory drug; antibacterial agent; anticoronaviral agent; antifungal agent; antineoplastic agent; antioxidant; apoptosis inducer; EC 1.13.11.33 (arachidonate 15-lipoxygenase) inhibitor; EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor; EC 1.3.1.8 [acyl-CoA dehydrogenase (NADP(+))] inhibitor; EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor; EC 2.5.1.7 (UDP-N-acetylglucosamine 1-carboxyvinyltransferase) inhibitor; EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor; EC 3.1.3.25 (inositol-phosphate phosphatase) inhibitor; EC 3.4.22.69 (SARS coronavirus main proteinase) inhibitor; EC 3.5.4.1 (cytosine deaminase) inhibitor; EC 5.1.3.2 (UDP-glucose 4-epimerase) inhibitor; enzyme mimic; ferroptosis inhibitor; genotoxin; hepatoprotective agent; neuroprotective agent; radical scavenger |
| vorinostat | vorinostat : A dicarboxylic acid diamide comprising suberic (octanedioic) acid coupled to aniline and hydroxylamine. A histone deacetylase inhibitor, it is marketed under the name Zolinza for the treatment of cutaneous T cell lymphoma (CTCL). Vorinostat: A hydroxamic acid and anilide derivative that acts as a HISTONE DEACETYLASE inhibitor. It is used in the treatment of CUTANEOUS T-CELL LYMPHOMA and SEZARY SYNDROME. | dicarboxylic acid diamide; hydroxamic acid | antineoplastic agent; apoptosis inducer; EC 3.5.1.98 (histone deacetylase) inhibitor |
| thiram | thiram : An organic disulfide that results from the formal oxidative dimerisation of N,N-dimethyldithiocarbamic acid. It is widely used as a fungicidal seed treatment. Thiram: A dithiocarbamate chemical, used commercially in the rubber processing industry and as a fungicide. In vivo studies indicate that it inactivates the enzyme GLUTATHIONE REDUCTASE. It has mutagenic activity and may induce chromosomal aberrations. | organic disulfide | antibacterial drug; antifungal agrochemical; antiseptic drug |
| cystamine dihydrochloride | |||
| cysteamine | cysteamine : An amine that consists of an ethane skeleton substituted with a thiol group at C-1 and an amino group at C-2. Cysteamine: A mercaptoethylamine compound that is endogenously derived from the COENZYME A degradative pathway. The fact that cysteamine is readily transported into LYSOSOMES where it reacts with CYSTINE to form cysteine-cysteamine disulfide and CYSTEINE has led to its use in CYSTINE DEPLETING AGENTS for the treatment of CYSTINOSIS. | amine; thiol | geroprotector; human metabolite; mouse metabolite; radiation protective agent |
| gliotoxin | gliotoxin : A pyrazinoindole with a disulfide bridge spanning a dioxo-substituted pyrazine ring; mycotoxin produced by several species of fungi. Gliotoxin: A fungal toxin produced by various species of Trichoderma, Gladiocladium fimbriatum, Aspergillus fumigatus, and Penicillium. It is used as an immunosuppressive agent. | dipeptide; organic disulfide; organic heterotetracyclic compound; pyrazinoindole | antifungal agent; EC 2.5.1.58 (protein farnesyltransferase) inhibitor; immunosuppressive agent; mycotoxin; proteasome inhibitor |
| 9,10-anthraquinone | 9,10-anthraquinone : An anthraquinone that is anthracene in which positions 9 and 10 have been oxidised to carbonyls. | anthraquinone | |
| 1,4-naphthoquinone | 1,4-naphthoquinone : The parent structure of the family of 1,4-naphthoquinones, in which the oxo groups of the quinone moiety are at positions 1 and 4 of the naphthalene ring. Derivatives have pharmacological properties. naphthoquinone : A polycyclic aromatic ketone metabolite of naphthalene. | 1,4-naphthoquinones | |
| azacitidine | 5-azacytidine : An N-glycosyl-1,3,5-triazine that is 4-amino-1,3,5-triazin-2(1H)-one substituted by a beta-D-ribofuranosyl residue via an N-glycosidic linkage. An antineoplastic agent, it is used in the treatment of myeloid leukaemia. Azacitidine: A pyrimidine analogue that inhibits DNA methyltransferase, impairing DNA methylation. It is also an antimetabolite of cytidine, incorporated primarily into RNA. Azacytidine has been used as an antineoplastic agent. | N-glycosyl-1,3,5-triazine; nucleoside analogue | antineoplastic agent |
| ninhydrin | ninhydrin : A member of the class of indanones that is indane-1,3-dione bearing two additional hydroxy substituents at position 2. Ninhydrin: 2,2-Dihydroxy-1H-indene-1,3-(2H)-dione. Reagent toxic to skin and mucus membranes. It is used in chemical assay for peptide bonds, i.e., protein determinations and has radiosensitizing properties. | aromatic ketone; beta-diketone; indanones; ketone hydrate | colour indicator; human metabolite |
| diphenyldiselenide | diphenyldiselenide: structure given in first source | ||
| benzeneseleninic acid | benzeneseleninic acid: structure given in first source | ||
| sodium selenate | sodium selenate : An inorganic sodium salt having selenate as the counterion. | inorganic sodium salt | anticonvulsant; EC 3.1.3.48 (protein-tyrosine-phosphatase) inhibitor; fertilizer |
| 2,2'-dipyridyl disulfide | 2,2'-dipyridyl disulfide: disulfide is an important moiety in this cpd aldrithiol : A member of the class of pyridines that is pyridine which is substituted by a pyridin-2-yldisulfanediyl group at position 2. It is a reagent used in molecular biology as an oxidizing agent. Also used in peptide synthesis and for detecting thiols. | organic disulfide; pyridines | oxidising agent |
| glutathione disulfide | Glutathione Disulfide: A GLUTATHIONE dimer formed by a disulfide bond between the cysteine sulfhydryl side chains during the course of being oxidized. | glutathione derivative; organic disulfide | Escherichia coli metabolite; mouse metabolite |
| sinefungin | adenosines; non-proteinogenic alpha-amino acid | antifungal agent; antimicrobial agent | |
| bisdethiobis(methylthio)gliotoxin | bisdethiobis(methylthio)gliotoxin: structure given in first source; a platelet activating factor antagonist | ||
| s-adenosylhomocysteine | S-adenosyl-L-homocysteine : An organic sulfide that is the S-adenosyl derivative of L-homocysteine. S-Adenosylhomocysteine: 5'-S-(3-Amino-3-carboxypropyl)-5'-thioadenosine. Formed from S-adenosylmethionine after transmethylation reactions. | adenosines; amino acid zwitterion; homocysteine derivative; homocysteines; organic sulfide | cofactor; EC 2.1.1.72 [site-specific DNA-methyltransferase (adenine-specific)] inhibitor; EC 2.1.1.79 (cyclopropane-fatty-acyl-phospholipid synthase) inhibitor; epitope; fundamental metabolite |
| decitabine | 2'-deoxyribonucleoside | ||
| ditiocarb sodium | organic molecular entity | ||
| verticillins | verticillins: 3 antibiotics isolated from imperfect fungus Verticillium: verticillin A, verticillin B (mono-3-hydroxymethyl analog of verticillin A), & verticillin C (differs from verticillin B in that 1 of dioxopiperazine rings has a trisulfide rather than a disulfide bridge; active against gram-positive bacteria & mycobacteria but not against gram-negative bacteria & fungi; RN given refers to cpd with unknown MF; structure (verticillins A & B)) | ||
| azodicarbonamide | organic molecular entity | ||
| chetomin | |||
| sgi-1027 | SGI-1027: inhibits DNA methyltransferase 1; structure in first source | ||
| bix 01294 | piperidines | ||
| unc 0638 | UNC 0638: inhibits lysine methyltransferases G9a and GLP; structure in first source | quinazolines | |
| unc 0321 | 7-(2-(2-(dimethylamino)ethoxy)ethoxy)-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine: a G9a antagonist; structure in first source | quinazolines | |
| unc 0631 | N-(1-(cyclohexylmethyl)piperidin-4-yl)-2-(4-isopropyl-1,4-diazepan-1-yl)-6-methoxy-7-(3-(piperidin-1-yl)propoxy)quinazolin-4-amine: inhibits protein lysine methyltransferase G9a; structure in first source | ||
| gsk343 | GSK343 : A member of the class of indazoles that is 1-isopropyl-1H-indazole-4-carboxamide in which the nitrogen of the carboxamide group is substituted by a (6-methyl-2-oxo-4-propyl-1,2-dihydropyridin-3-yl)methyl group and in which the indazole ring is substituted at position 6 by a 2-(4-methylpiperazin-1-yl)pyridin-4-yl group. A highly potent and selective EZH2 inhibitor (IC50 = 4 nM). GSK343: an EZH2 methyltransferase inhibitor | aminopyridine; indazoles; N-alkylpiperazine; N-arylpiperazine; pyridone; secondary carboxamide | antineoplastic agent; apoptosis inducer; EC 2.1.1.43 (enhancer of zeste homolog 2) inhibitor |
| brd4770 | benzimidazoles | ||
| 6,7-dimethoxy-2-(pyrrolidin-1-yl)-n-(5-(pyrrolidin-1-yl)pentyl)quinazolin-4-amine | 6,7-dimethoxy-2-(pyrrolidin-1-yl)-N-(5-(pyrrolidin-1-yl)pentyl)quinazolin-4-amine: a SETD8 inhibitor; structure in first source |