Information on EC 2.1.1.43 - histone-lysine N-methyltransferase

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The enzyme appears in viruses and cellular organisms

EC NUMBER
COMMENTARY hide
2.1.1.43
-
RECOMMENDED NAME
GeneOntology No.
histone-lysine N-methyltransferase
REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
S-adenosyl-L-methionine + histone L-lysine = S-adenosyl-L-homocysteine + histone N6-methyl-L-lysine
show the reaction diagram
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
methyl group transfer
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-
-
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PATHWAY
BRENDA Link
KEGG Link
MetaCyc Link
carnitine metabolism
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Lysine degradation
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SYSTEMATIC NAME
IUBMB Comments
S-adenosyl-L-methionine:histone-L-lysine N6-methyltransferase
One of a group of enzymes methylating proteins; see also EC 2.1.1.59, [cytochrome-c]-lysine N-methyltransferase and EC 2.1.1.60, calmodulin-lysine N-methyltransferase.
CAS REGISTRY NUMBER
COMMENTARY hide
9055-08-7
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ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
calf
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Manually annotated by BRENDA team
strain CAI12
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Manually annotated by BRENDA team
strain CAI12
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Manually annotated by BRENDA team
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-
-
Manually annotated by BRENDA team
2 enzyme forms: VA and VB
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-
Manually annotated by BRENDA team
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UniProt
Manually annotated by BRENDA team
strain 3D7
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-
Manually annotated by BRENDA team
strain Lister 427
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-
Manually annotated by BRENDA team
Trypanosoma brucei Lister 427
strain Lister 427
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-
Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
malfunction
physiological function
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
ARTKQTARKSTGGKAPRK(biot)G + S-adenosyl-L-methionine
ART-methyl-KQTARKSTGGKAPRK(biot)G + S-adenosyl-L-homocysteine
show the reaction diagram
-
-
-
-
?
biotinyl-MARTKQTARKSTGGKAPRKQ + S-adenosyl-L-methionine
?
show the reaction diagram
-
Dim-5 methylates the histone H3 tail at position Lys9
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-
-
MC-1alpha + S-adenosyl-L-methionine
MC-1alpha N6-methylated at lysine37 + S-adenosyl-L-homocysteine
show the reaction diagram
-
high substrate specificity
-
-
?
polylysine + S-adenosylmethionine
S-adenosyl-L-homocysteine + N6-methylpolylysine
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + biotin-aminohexanoyl-GSRAHSSHLKSKKGQSTSRH
?
show the reaction diagram
-
100% activity
-
-
?
S-adenosyl-L-methionine + biotin-ARTKQTARKST
?
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + CDYL1 protein
?
show the reaction diagram
-
target of histone lysine methyltransferase G9a (KMT1C)
-
-
?
S-adenosyl-L-methionine + chicken nucleosome
S-adenosyl-L-homocysteine + chicken nucleosome N6-methyl-L-lysine
show the reaction diagram
-
-
-
?
S-adenosyl-L-methionine + CSB protein
?
show the reaction diagram
-
target of histone lysine methyltransferase G9a (KMT1C)
-
-
?
S-adenosyl-L-methionine + dimethylated histone H3(K9)
S-adenosyl-L-homocysteine + trimethylated histone H3(K9)
show the reaction diagram
-
the activity on dimethylated histone H3(K9) peptides is several folds lower than when monomethylated histone H3(K9) peptides are used
-
-
?
S-adenosyl-L-methionine + DNA methyltransferase 1
?
show the reaction diagram
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-
-
-
?
S-adenosyl-L-methionine + estrogen receptor alpha(K302)
?
show the reaction diagram
estrogen receptor alpha is directly methylated at lysine-302 by SET-7, a K303R mutation inhibits methylation at K302 in vivo
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-
?
S-adenosyl-L-methionine + HDAC1 protein
?
show the reaction diagram
-
target of histone lysine methyltransferase G9a (KMT1C)
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-
?
S-adenosyl-L-methionine + histone (K4)
S-adenosyl-L-homocysteine + methylated histone (K4)
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + histone 3(K4)
?
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + histone 3(K79)
?
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + histone H1
?
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + histone H1.4(K121)
?
show the reaction diagram
-
less than 10% methylation at Lys-34
-
-
?
S-adenosyl-L-methionine + histone H1.4(K26)
?
show the reaction diagram
-
70% methylation at Lys-26, methylation of the K26A mutant of histone H1.4 is strongly reduced but not completely abolished
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-
?
S-adenosyl-L-methionine + histone H1.4(K34)
?
show the reaction diagram
-
10-15% methylation at Lys-34
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-
?
S-adenosyl-L-methionine + histone H1.4(K52)
?
show the reaction diagram
-
less than 1% methylation at Lys-34
-
-
?
S-adenosyl-L-methionine + histone H2A
?
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + histone H2A
S-adenosyl-L-homocysteine + ?
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + histone H2B
?
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + histone H2B
S-adenosyl-L-homocysteine + ?
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + histone H2B L-lysine
S-adenosyl-L-homocysteine + histone H2B N6-methyl-L-lysine
show the reaction diagram
-
about 150% activity compared to biotin-aminohexanoyl-GSRAHSSHLKSKKGQSTSRH, H2B is more efficient substrate with 3fold higher specific activity compared to H3
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?
S-adenosyl-L-methionine + histone H3
?
show the reaction diagram
S-adenosyl-L-methionine + histone H3 (1-13)
?
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + histone H3 (S10phos)
?
show the reaction diagram
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phosphorylation of the proximal amino acids impairs Lys-9 methylation via impairing enzyme-substrate interaction
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?
S-adenosyl-L-methionine + histone H3 (T11phos)
?
show the reaction diagram
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phosphorylation of the proximal amino acids impairs Lys-9 methylation via impairing enzyme-substrate interaction
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-
?
S-adenosyl-L-methionine + histone H3 L-lysine
S-adenosyl-L-homocysteine + histone H3 N6-methyl-L-lysine
show the reaction diagram
-
efficient substrate, about 40% activity compared to biotin-aminohexanoyl-GSRAHSSHLKSKKGQSTSRH
-
-
?
S-adenosyl-L-methionine + histone H3 lysine 36
?
show the reaction diagram
dimethylation
-
-
?
S-adenosyl-L-methionine + histone H3(K27)
?
show the reaction diagram
S-adenosyl-L-methionine + histone H3(K27)
S-adenosyl-L-homocysteine + ?
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + histone H3(K27)
S-adenosyl-L-homocysteine + N-methylated histone H3(K27)
show the reaction diagram
S-adenosyl-L-methionine + histone H3(K27)
S-adenosyl-L-homocysteine + N6-methylated histone H3(K27)
show the reaction diagram
-
-
isoforms NSD1, NSD2 and NSD3, mainly trimethylation
-
?
S-adenosyl-L-methionine + histone H3(K27A)
?
show the reaction diagram
-
mutation in the unstructured amino-terminal tail of histone H3 does not affect the central globular domain, but reduces the turnover numbers of the substrates
-
-
?
S-adenosyl-L-methionine + histone H3(K36)
?
show the reaction diagram
S-adenosyl-L-methionine + histone H3(K36)
S-adenosyl-L-homocysteine + histone H3(K36) N6-methyl-L-lysine
show the reaction diagram
-
-
-
?
S-adenosyl-L-methionine + histone H3(K36)
S-adenosyl-L-homocysteine + N-methylated histone H3(K36)
show the reaction diagram
S-adenosyl-L-methionine + histone H3(K36)
S-adenosyl-L-homocysteine + N6-methylated histone H3(K36)
show the reaction diagram
-
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preferable in vitro substrate for isoform NSD1
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?
S-adenosyl-L-methionine + histone H3(K36R)
?
show the reaction diagram
-
methylated by GST-mG9a
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-
?
S-adenosyl-L-methionine + histone H3(K4)
?
show the reaction diagram
S-adenosyl-L-methionine + histone H3(K4)
S-adenosyl-L-homocysteine + ?
show the reaction diagram
-
enzyme G9A exhibits a modest decrease in catalytic efficiency when assayed with an histone H3(K4)me3 peptide in comparison to an unmodified H3 peptide substrate
-
-
?
S-adenosyl-L-methionine + histone H3(K4)
S-adenosyl-L-homocysteine + N-methylated histone H3(K4)
show the reaction diagram
S-adenosyl-L-methionine + histone H3(K4)
S-adenosyl-L-homocysteine + N6-methylated histone H3(K4)
show the reaction diagram
-
-
isoforms NSD1 and NSD2, mainly trimethylation
-
?
S-adenosyl-L-methionine + histone H3(K4A)
?
show the reaction diagram
-
mutation in the unstructured amino-terminal tail of histone H3 does not affect the central globular domain, but reduces the turnover numbers of the substrates
-
-
?
S-adenosyl-L-methionine + histone H3(K76)
?
show the reaction diagram
S-adenosyl-L-methionine + histone H3(K79)
?
show the reaction diagram
S-adenosyl-L-methionine + histone H3(K79)
S-adenosyl-L-homocysteine + N6-methylated histone H3(K79)
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + histone H3(K9)
?
show the reaction diagram
S-adenosyl-L-methionine + histone H3(K9)
S-adenosyl-L-homocysteine + ?
show the reaction diagram
S-adenosyl-L-methionine + histone H3(K9)
S-adenosyl-L-homocysteine + N6-methylated histone H3(K9)
show the reaction diagram
-
-
isoforms NSD1, NSD2 and NSD3, mainly dimethylation
-
?
S-adenosyl-L-methionine + histone H3(N)
?
show the reaction diagram
S-adenosyl-L-methionine + histone H3(N27)
?
show the reaction diagram
S-adenosyl-L-methionine + histone H3(N4)
?
show the reaction diagram
methylated by GST-HYPB protein
-
-
?
S-adenosyl-L-methionine + histone H3(N9)
?
show the reaction diagram
S-adenosyl-L-methionine + histone H3(peptide 21-44)
S-adenosyl-L-homocysteine + histone H3(peptide21-44) N6-methyl-L-lysine
show the reaction diagram
-
-
-
?
S-adenosyl-L-methionine + histone H3(peptide31-50)
S-adenosyl-L-homocysteine + N6-methylated K36 in histone H3(peptide 31-50)
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + histone H3.2 L-lysine
S-adenosyl-L-homocysteine + histone H3.2 N6-methyl-L-lysine
show the reaction diagram
-
about 30% activity compared to biotin-aminohexanoyl-GSRAHSSHLKSKKGQSTSRH
-
-
?
S-adenosyl-L-methionine + histone H4
?
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + histone H4
S-adenosyl-L-homocysteine + ?
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + histone H4
S-adenosyl-L-homocysteine + N-methylated histone H4
show the reaction diagram
-
-
-
?
S-adenosyl-L-methionine + histone H4 L-lysine
S-adenosyl-L-homocysteine + histone H4 N6-methyl-L-lysine
show the reaction diagram
-
best substrate, H4 is more efficient substrate with 5fold higher specific activity compared to H3, about 240% activity compared to biotin-aminohexanoyl-GSRAHSSHLKSKKGQSTSRH
-
-
?
S-adenosyl-L-methionine + histone H4(K20)
?
show the reaction diagram
S-adenosyl-L-methionine + histone H4(K20)
S-adenosyl-L-homocysteine + N6-methylated histone H4(K20)
show the reaction diagram
-
-
isoform NSD1, mainly mono- and trimethylation, isoforms NSD2 and NSD3, mainly di-and trimethylation
-
?
S-adenosyl-L-methionine + histone H4(K344)
?
show the reaction diagram
histone H4 lysine-44 is the primary target of NSD2 in the case of octamer substrates, irrespective of the histones being native or recombinant
-
-
?
S-adenosyl-L-methionine + histone H4(peptide35-55)
S-adenosyl-L-homocysteine + N6-methylated K44 in histone H4(peptide 35-55)
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + histone K4-acetylK9
?
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + histone K4-trimethylK9
?
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + histone K4AK9
?
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + histone L-lysine
S-adenosyl-L-homocysteine + histone N6-methyl-L-lysine
show the reaction diagram
S-adenosyl-L-methionine + monomethylated histone H3(K9)
S-adenosyl-L-homocysteine + trimethylated histone H3(K9)
show the reaction diagram
-
the SUVR4 product specificity shifts from di- to trimethylation in the presence of free ubiquitin. SUVR4 in vivo specifically converts monomethylated histone H3(K9) to trimethylated histone H3(K9) at transposons and pseudogenes
-
-
?
S-adenosyl-L-methionine + p300/CBP-associated factor
?
show the reaction diagram
-
K78 and K89 are preferentially methylated in full-length p300/CBP-associated factor in vitro
-
-
?
S-adenosyl-L-methionine + p53
?
show the reaction diagram
S-adenosyl-L-methionine + p53 (K382)
?
show the reaction diagram
-
SET8 activity is strongly reduced by the arginine methylation at position R379
-
-
?
S-adenosyl-L-methionine + p53 protein
S-adenosyl-L-homocysteine + N-methylated p53 protein
show the reaction diagram
-
-
-
?
S-adenosyl-L-methionine + p53(K373)
?
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + p53(K373)
S-adenosyl-L-homocysteine + ?
show the reaction diagram
-
-
-
-
?
S-adenosyl-L-methionine + recombinant nucleosome
S-adenosyl-L-homocysteine + recombinant nucleosome N6-methyl-L-lysine
show the reaction diagram
-
-
-
?
S-adenosyl-L-methionine + TAF10-K189 peptide
?
show the reaction diagram
-
-
-
?
S-adenosyl-L-methionine + transcriptional factor p53
?
show the reaction diagram
-
methylation of transcriptional factor p53 with the sequence LKSKKGQSTY occurs at Lys-4
-
-
?
S-adenosyl-L-methionine + transition protein TP2
S-adenosyl-L-homocysteine + N6-methylated transition protein TP2
show the reaction diagram
-
-
enzyme methylates TP2 at Lys88 and Lys91 residues. TP2K88me1 modifications appear in elongating to condensing spermatids and are predominantly associated with the chromatin-bound TP2
-
?
S-adenosyl-L-methionine + WIZ protein
?
show the reaction diagram
-
target of histone lysine methyltransferase G9a (KMT1C)
-
-
?
S-adenosyl-L-methionine + [primase-subunit-Pri1]-L-lysine
S-adenosyl-L-homocysteine + [primase-subunit-Pri1]-N6-methyl-L-lysine
show the reaction diagram
S-adenosyl-L-methionine + [primase-subunit-Pri2]-L-lysine
S-adenosyl-L-homocysteine + [primase-subunit-Pri2]-N6-methyl-L-lysine
show the reaction diagram
S-adenosyl-L-methionine + [protein Cren7]-L-lysine
S-adenosyl-L-homocysteine + [protein Cren7]-N6-methyl-L-lysine
show the reaction diagram
S-adenosyl-L-methionine + [protein Dpo4]-L-lysine
S-adenosyl-L-homocysteine + [protein Dpo4]-N6-methyl-L-lysine
show the reaction diagram
-
-
-
?
S-adenosyl-L-methionine + [protein FEN1]-L-lysine
S-adenosyl-L-homocysteine + [protein FEN1]-N6-methyl-L-lysine
show the reaction diagram
-
-
-
?
S-adenosyl-L-methionine + [protein GINS15]-L-lysine
S-adenosyl-L-homocysteine + [protein GINS15]-N6-methyl-L-lysine
show the reaction diagram
-
-
-
?
S-adenosyl-L-methionine + [protein PCNA1]-L-lysine
S-adenosyl-L-homocysteine + [protein PCNA1]-N6-methyl-L-lysine
show the reaction diagram
-
-
-
?
S-adenosyl-L-methionine + [protein PCNA2]-L-lysine
S-adenosyl-L-homocysteine + [protein PCNA2]-N6-methyl-L-lysine
show the reaction diagram
-
-
-
?
S-adenosyl-L-methionine + [protein PolB1]-L-lysine
S-adenosyl-L-homocysteine + [protein PolB1]-N6-methyl-L-lysine
show the reaction diagram
-
-
-
?
S-adenosyl-L-methionine + [protein Sso7d2]-L-lysine
S-adenosyl-L-homocysteine + [protein Sso7d2]-N6-methyl-L-lysine
show the reaction diagram
-
-
-
?
S-adenosyl-L-methionine + [ribosomal protein L11]-L-lysine
S-adenosyl-L-homocysteine + [ribosomal protein L11]-N6-methyl-L-lysine
show the reaction diagram
-
-
-
?
S-adenosyl-L-methionine + [Topo-III]-L-lysine
S-adenosyl-L-homocysteine + [Topo-III]-N6-methyl-L-lysine
show the reaction diagram
-
-
-
?
additional information
?
-
NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
S-adenosyl-L-methionine + dimethylated histone H3(K9)
S-adenosyl-L-homocysteine + trimethylated histone H3(K9)
show the reaction diagram
-
the activity on dimethylated histone H3(K9) peptides is several folds lower than when monomethylated histone H3(K9) peptides are used
-
-
?
S-adenosyl-L-methionine + histone H3(K36)
?
show the reaction diagram
-
SDG724 mediates histone H3(K36)me2/3 deposition at MADS50 and RFT1
-
-
?
S-adenosyl-L-methionine + histone L-lysine
S-adenosyl-L-homocysteine + histone N6-methyl-L-lysine
show the reaction diagram
S-adenosyl-L-methionine + monomethylated histone H3(K9)
S-adenosyl-L-homocysteine + trimethylated histone H3(K9)
show the reaction diagram
-
the SUVR4 product specificity shifts from di- to trimethylation in the presence of free ubiquitin. SUVR4 in vivo specifically converts monomethylated histone H3(K9) to trimethylated histone H3(K9) at transposons and pseudogenes
-
-
?
S-adenosyl-L-methionine + [protein Cren7]-L-lysine
S-adenosyl-L-homocysteine + [protein Cren7]-N6-methyl-L-lysine
show the reaction diagram
additional information
?
-
COFACTOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
S-adenosyl-L-methionine
-
-
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
Zn2+
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the enzyme contains three tightly bound zinc ions that are important for maintaining the structural integrity and catalytic activity
additional information
the enzyme requires no divalent cations for its activity
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
2-chloro-6,7-dimethoxyquinazoline
-
less than 30% inhibition at 0.001 mM
5-(6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-4-(1-methylpiperidin-4-ylamino)quinazolin-7-yloxy)pentanamide
-
less than 30% inhibition at 0.001 mM
6,7-dimethoxy-2-(4-methyl-1,4-diazepan-1-yl)-4-(1-methylpiperidin-4-yloxy)quinazoline
-
less than 30% inhibition at 0.001 mM
6,7-dimethoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine
-
-
6,7-dimethoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpyrrolidin-3-yl)quinazolin-4-amine
-
-
6,7-dimethoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(piperidin-4-yl)quinazolin-4-amine
-
less than 30% inhibition at 0.001 mM
6,7-dimethoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(tetrahydro-2H-pyran-4-yl)quinazolin-4-amine
-
less than 30% inhibition at 0.001 mM
6,7-dimethoxy-2-(4-methylpiperazin-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine
-
-
6,7-dimethoxy-N-(1-methylpiperidin-4-yl)-2-(piperidin-1-yl)-quinazolin-4-amine
-
-
6,7-dimethoxy-N-(1-methylpiperidin-4-yl)-2-morpholinoquinazolin-4-amine
-
-
6,7-dimethoxy-N-methyl-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine
-
less than 30% inhibition at 0.001 mM
6,7-dimethoxy-N-methyl-2-(4-methyl-1,4-diazepan-1-yl)quinazolin-4-amine
-
less than 30% inhibition at 0.001 mM
6,7-dimethoxy-N2,N2-dimethyl-N4-(1-methylpiperidin-4-yl)-quinazoline-2,4-diamine
-
-
6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-7-(3-(methylamino)-propoxy)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine
-
-
6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-7-(4-methylpentyloxy)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine
-
-
6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)-7-(2-(2-(pyrrolidin-1-yl)ethoxy)ethoxy)quinazolin-4-amine
-
-
6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)-7-(3-(piperidin-1-yl)propoxy)quinazolin-4-amine
-
-
6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)-7-(3-(pyrrolidin-1-yl)propoxy)quinazolin-4-amine
-
-
6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)-7-(3-morpholinopropoxy)quinazolin-4-amine
-
-
6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)-7-(piperidin-3-ylmethoxy)quinazolin-4-amine
-
-
6-methoxy-7-(3-(methyl(propyl)amino)propoxy)-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine
-
-
6-methoxy-7-(4-methoxybutoxy)-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine
-
less than 30% inhibition at 0.001 mM
7-(2-(2-(dimethylamino)ethoxy)ethoxy)-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine
-
UNC0321, G9a inhibitor with picomolar potency and the most potent G9a inhibitor
7-(2-(dimethylamino)ethoxy)-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine
-
-
7-(3-(diethylamino)propoxy)-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine
-
-
7-(3-(dimethylamino)propoxy)-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine
-
UNC0224, potent G9a inhibitor
7-(4-(dimethylamino)butoxy)-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine
-
-
7-(5-(dimethylamino)pentyloxy)-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine
-
-
7-(5-aminopentyloxy)-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine
-
-
7-(6-(dimethylamino)hexyloxy)-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine
-
-
aldosterone
BIX-01294
BIX-01338
chaetocin
Cu2+
-
-
CXXC finger protein 1
-
restricts the activity of the Set1 histone methyltransferase complex
-
cyclohexamide
-
decreases nuclear G9a protein but does not prevent its relative increase during hypoxic stress
DNA
-
-
E72
-
inhibits enzyme form GLP
eosin
-
AMI-5, numerous different substitutes of eosin synthesized and tested for inhibition
Hg2+
-
-
N-(1-benzylpiperidin-4-yl)-6,7-dimethoxy-2-(4-methyl-1,4-diazepan-1-yl)quinazolin-4-amine
-
BIX01294, selective small molecule inhibitor of enzyme forms G9a and GLP
N-cyclohexyl-6,7-dimethoxy-2-(4-methyl-1,4-diazepan-1-yl)-quinazolin-4-amine
-
less than 30% inhibition at 0.001 mM
N-cyclopropyl-6,7-dimethoxy-2-(4-methyl-1,4-diazepan-1-yl)-quinazolin-4-amine
-
less than 30% inhibition at 0.001 mM
N-isopropyl-6,7-dimethoxy-2-(4-methyl-1,4-diazepan-1-yl)-quinazolin-4-amine
-
less than 30% inhibition at 0.001 mM
N1-(2-(6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-4-(1-methylpiperidin-4-ylamino)quinazolin-7-yloxy)ethyl)-N1,N2,N2-trimethylethane-1,2-diamine
-
-
N2,N2-diethyl-6,7-dimethoxy-N4-(1-methylpiperidin-4-yl)quinazoline-2,4-diamine
-
-
RNA
-
-
S-adenosyl-L-cysteine
-
-
S-adenosyl-L-ethionine
-
-
S-adenosyl-L-homocysteine
sinefungin
TCEP
-
suppresses activity in a dose-dependent manner
tert-butyl 4-(6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-4-(1-methylpiperidin-4-ylamino)quinazolin-7-yloxy)butylcarbamate
-
less than 30% inhibition at 0.001 mM
trimethylated histone H3(K4)
-
-
-
UNC0224
-
picomolar inhibition of enzyme form G9A
Zn2+
-
-
additional information
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
deferoxamine
-
increases G9a protein and activity in A549 cells, moreover, increases the methyltransferase activity of overexpressed GFP-hG9a fusion proteins
dimethyloxalylglycine
-
increases G9a protein and activity in A549 cells
heat shock protein 90alpha
-
the interaction of SMYD2 with heat shock protein 90alpha enhances SMYD2 histone methyltransferase activity and specificity for histone H3 at lysine 4 by 10fold, histone H3K36 methyltransferase activity is independent of ist interaction with heat shock protein 90alpha
-
Sulfhydryl reducing agent
-
required for optimal activity
-
additional information
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0074
biotinyl-MARTKQTARKSTGGKAPRKQ
-
-
0.00027 - 0.0089
chicken nucleosome
0.00031 - 0.00044
histone H1
0.00026 - 0.0009
Histone H3
0.0011
histone H3 (1-13)
-
wild-type substrate
-
0.0006
histone H3 (T11phos)
-
wild-type substrate
-
0.2762 - 3.9
histone H3(K27)
0.00017
histone H3(K27A)
-
recombinant substrate
-
0.00023
histone H3(K4A)
-
recombinant substrate
-
0.0005
histone H3(peptide 21-44)
pH 9.0, 23C
-
0.0022
histone K4-acetylK9
-
-
-
0.0006
histone K4-trimethylK9
-
-
-
0.0015
histone K4AK9
-
-
-
0.00003 - 0.0081
recombinant nucleosome
0.00012 - 0.0345
S-adenosyl-L-methionine
additional information
additional information
-
-
-
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.038
biotinyl-MARTKQTARKSTGGKAPRKQ
Neurospora crassa
-
-
0.0031 - 0.0061
chicken nucleosome
0.02167 - 0.024
Histone H3
0.02056
histone H3 (1-13)
Mus musculus
-
wild-type substrate
-
0.001806
histone H3 (S10phos)
Mus musculus
-
wild-type substrate
-
0.005
histone H3 (T11phos)
Mus musculus
-
wild-type substrate
-
1.32 - 1.36
histone H3(K27)
0.0161
histone H3(K27A), histone H3(K4A)
Mus musculus
-
recombinant substrate
-
0.0031
histone H3(peptide 21-44)
Homo sapiens
Q9NR48
pH 9.0, 23C
-
0.0089
histone K4-acetylK9, histone K4-trimethylK9
Mus musculus
-
-
-
0.01194
histone K4AK9
Mus musculus
-
-
-
0.0001 - 0.0013
recombinant nucleosome
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.00000063
7-(2-(2-(dimethylamino)ethoxy)ethoxy)-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine
-
enzyme form G9a, in PBS buffer, pH 7.4, at 22C
0.04 - 0.044
S-adenosyl-L-ethionine
0.00035 - 0.071
S-adenosyl-L-homocysteine
0.0015 - 0.0019
sinefungin
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.00033
6,7-dimethoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine
Homo sapiens
-
enzyme form G9a, in PBS buffer, pH 7.4, at 22C
0.00091
6,7-dimethoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpyrrolidin-3-yl)quinazolin-4-amine
Homo sapiens
-
enzyme form G9a, in PBS buffer, pH 7.4, at 22C
0.00015
6,7-dimethoxy-2-(4-methylpiperazin-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine
Homo sapiens
-
enzyme form G9a, in PBS buffer, pH 7.4, at 22C
0.00055
6,7-dimethoxy-N-(1-methylpiperidin-4-yl)-2-(piperidin-1-yl)-quinazolin-4-amine
Homo sapiens
-
enzyme form G9a, in PBS buffer, pH 7.4, at 22C
0.0016
6,7-dimethoxy-N-(1-methylpiperidin-4-yl)-2-morpholinoquinazolin-4-amine
Homo sapiens
-
enzyme form G9a, in PBS buffer, pH 7.4, at 22C
0.0011
6,7-dimethoxy-N2,N2-dimethyl-N4-(1-methylpiperidin-4-yl)-quinazoline-2,4-diamine
Homo sapiens
-
enzyme form G9a, in PBS buffer, pH 7.4, at 22C
0.00012
6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-7-(3-(methylamino)-propoxy)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine
Homo sapiens
-
enzyme form G9a, in PBS buffer, pH 7.4, at 22C
0.0034
6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-7-(4-methylpentyloxy)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine
Homo sapiens
-
enzyme form G9a, in PBS buffer, pH 7.4, at 22C
0.000057
6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)-7-(2-(2-(pyrrolidin-1-yl)ethoxy)ethoxy)quinazolin-4-amine
Homo sapiens
-
enzyme form G9a, in PBS buffer, pH 7.4, at 22C
0.000025
6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)-7-(3-(piperidin-1-yl)propoxy)quinazolin-4-amine
Homo sapiens
-
enzyme form G9a, in PBS buffer, pH 7.4, at 22C
0.000008
6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)-7-(3-(pyrrolidin-1-yl)propoxy)quinazolin-4-amine
Homo sapiens
-
enzyme form G9a, in PBS buffer, pH 7.4, at 22C
0.00088
6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)-7-(3-morpholinopropoxy)quinazolin-4-amine
Homo sapiens
-
enzyme form G9a, in PBS buffer, pH 7.4, at 22C
0.0015
6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)-7-(piperidin-3-ylmethoxy)quinazolin-4-amine
Homo sapiens
-
enzyme form G9a, in PBS buffer, pH 7.4, at 22C
0.00051
6-methoxy-7-(3-(methyl(propyl)amino)propoxy)-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine
Homo sapiens
-
enzyme form G9a, in PBS buffer, pH 7.4, at 22C
0.000009
7-(2-(2-(dimethylamino)ethoxy)ethoxy)-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine
Homo sapiens
-
enzyme form G9a, in PBS buffer, pH 7.4, at 22C
0.00011
7-(2-(dimethylamino)ethoxy)-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine
Homo sapiens
-
enzyme form G9a, in PBS buffer, pH 7.4, at 22C
0.000052
7-(3-(diethylamino)propoxy)-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine
Homo sapiens
-
enzyme form G9a, in PBS buffer, pH 7.4, at 22C
0.000043
7-(3-(dimethylamino)propoxy)-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine
Homo sapiens
-
enzyme form G9a, in PBS buffer, pH 7.4, at 22C
0.00014
7-(4-(dimethylamino)butoxy)-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine
Homo sapiens
-
enzyme form G9a, in PBS buffer, pH 7.4, at 22C
0.000095
7-(5-(dimethylamino)pentyloxy)-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine
Homo sapiens
-
enzyme form G9a, in PBS buffer, pH 7.4, at 22C
0.000235
7-(5-aminopentyloxy)-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine
Homo sapiens
-
enzyme form G9a, in PBS buffer, pH 7.4, at 22C
0.0015
7-(6-(dimethylamino)hexyloxy)-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine
Homo sapiens
-
enzyme form G9a, in PBS buffer, pH 7.4, at 22C
0.0007 - 0.0027
BIX-01294
0.005
BIX-01338
Homo sapiens
-
histone lysine methyltransferase G9a
0.00018
N-(1-benzylpiperidin-4-yl)-6,7-dimethoxy-2-(4-methyl-1,4-diazepan-1-yl)quinazolin-4-amine
Homo sapiens
-
enzyme form G9a, in PBS buffer, pH 7.4, at 22C
0.000345
N1-(2-(6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-4-(1-methylpiperidin-4-ylamino)quinazolin-7-yloxy)ethyl)-N1,N2,N2-trimethylethane-1,2-diamine
Homo sapiens
-
enzyme form G9a, in PBS buffer, pH 7.4, at 22C
0.00091
N2,N2-diethyl-6,7-dimethoxy-N4-(1-methylpiperidin-4-yl)quinazoline-2,4-diamine
Homo sapiens
-
enzyme form G9a, in PBS buffer, pH 7.4, at 22C
0.02
sinefungin
Homo sapiens
-
pH 9.8, 37C
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
0.000285
-
isozyme VA
0.00202
-
isozyme VB
0.0027
-
-
additional information
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
8.5 - 9
-
-
9.1
-
SMYD2 activity increases dramatically from pH 8.5 to pH 9.2, peaking at pH 9.1
pH RANGE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
5.5 - 9.5
-
at pH 5.5 and pH 9.5 about 50% of activity maximum
7.5 - 9.9
-
about 50% of activity maximum at pH 7.5 and 9.9
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
30
-
assay at
32
-
SMYD2 has maximal activity at about 32C, with activity rapidly dropping at temperatures above 37C
TEMPERATURE RANGE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
25 - 40
-
-
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
-
interaction between growth factor independent 1 and G9a in vivo
Manually annotated by BRENDA team
-
myeloma cell, derived from KMS-11 cell
Manually annotated by BRENDA team
-
myeloma cell, derived from KMS-11 cell
Manually annotated by BRENDA team
-
PRDM8 is expressed most prominently in striated skeletal muscle from the tongue
Manually annotated by BRENDA team
additional information
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY hide
GeneOntology No.
LITERATURE
SOURCE
-
Dpy-30 functions in the endosome to trans-Golgi network transport of cation-independent mannose 6-phosphate receptor
Manually annotated by BRENDA team
-
subcellular distribution is not definitely determined
-
Manually annotated by BRENDA team
-
subcellular distribution is not definitely determined
Manually annotated by BRENDA team
additional information
-
G9a protein not detected in the cytoplasm
-
Manually annotated by BRENDA team