Information on EC 2.1.1.43 - histone-lysine N-methyltransferase and Organism(s) Homo sapiens

for references in articles please use BRENDA:EC2.1.1.43
Word Map on EC 2.1.1.43
Please wait a moment until all data is loaded. This message will disappear when all data is loaded.
Specify your search results
Select one or more organisms in this record:
This record set is specific for:
Homo sapiens


The taxonomic range for the selected organisms is: Homo sapiens

The enzyme appears in selected 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
-
-
-
-
PATHWAY
BRENDA Link
KEGG Link
MetaCyc Link
carnitine metabolism
-
-
Lysine degradation
-
-
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
-
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
-
-
-
-
?
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 + DNA methyltransferase 1
?
show the reaction diagram
-
-
-
-
?
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
-
-
?
S-adenosyl-L-methionine + HDAC1 protein
?
show the reaction diagram
-
target of histone lysine methyltransferase G9a (KMT1C)
-
-
?
S-adenosyl-L-methionine + histone (K4)
S-adenosyl-L-homocysteine + methylated histone (K4)
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
-
-
?
S-adenosyl-L-methionine + histone H1.4(K34)
?
show the reaction diagram
-
10-15% methylation at Lys-34
-
-
?
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 H2B
?
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
-
-
?
S-adenosyl-L-methionine + histone H3
?
show the reaction diagram
-
-
-
-
?
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(K27)
?
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(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
-
-
preferable in vitro substrate for isoform NSD1
-
?
S-adenosyl-L-methionine + 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(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 + 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
methylated by GST-HYPB protein
-
-
?
S-adenosyl-L-methionine + histone H3(N27)
?
show the reaction diagram
methylated by GST-HYPB protein
-
-
?
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
methylated by GST-HYPB protein
-
-
?
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 + 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 L-lysine
S-adenosyl-L-homocysteine + histone N6-methyl-L-lysine
show the reaction diagram
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 + 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 + WIZ protein
?
show the reaction diagram
-
target of histone lysine methyltransferase G9a (KMT1C)
-
-
?
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 + histone L-lysine
S-adenosyl-L-homocysteine + histone 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+
-
the enzyme contains three tightly bound zinc ions that are important for maintaining the structural integrity and catalytic 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
cyclohexamide
-
decreases nuclear G9a protein but does not prevent its relative increase during hypoxic stress
eosin
-
AMI-5, numerous different substitutes of eosin synthesized and tested for inhibition
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
-
-
S-adenosyl-L-homocysteine
-
competitive inhibition
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
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
-
additional information
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.00027 - 0.0089
chicken nucleosome
-
0.0005
histone H3(peptide 21-44)
pH 9.0, 23C
-
0.00003 - 0.0081
recombinant nucleosome
-
0.00012 - 0.0055
S-adenosyl-L-methionine
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0031 - 0.0061
chicken nucleosome
-
0.0031
histone H3(peptide 21-44)
pH 9.0, 23C
-
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
0.00035
S-adenosyl-L-homocysteine
-
wild type enzyme, using p53 as cosubstrate, in 50 mM Tris pH 9.0, at 22C
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
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
9.1
-
SMYD2 activity increases dramatically from pH 8.5 to pH 9.2, peaking at pH 9.1
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
32
-
SMYD2 has maximal activity at about 32C, with activity rapidly dropping at temperatures above 37C
37
-
assay at
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
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY hide
GeneOntology No.
LITERATURE
SOURCE
additional information
-
G9a protein not detected in the cytoplasm
-
Manually annotated by BRENDA team
PDB
SCOP
CATH
ORGANISM
UNIPROT
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
45000
SDS-PAGE
49700
-
calculated from amino acid sequence
52000
-
about 52000 Da, SDS-PAGE
53000
-
x * 53000, MALDI-TOF mass spectrometry
53100
-
x * 53100, calculated from amino acid sequence
60000
-
x * 60000, GST-tagged SET8 domain, SDS-PAGE
400000 - 800000
-
the activity peak migrates at high molecular mass (400000-800000 Da), gel filtration
450000
Western analysis of Set1/CXXC finger protein 1 complex
SUBUNITS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
monomer
1 * 45000, SDS-PAGE
additional information
-
enzyme interacts in vivo and in vitro with CCAAT displacement protein/cut homolog. Transcriptional repressor function of cut homolog is mediated through enzyme activity
Crystallization/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
in complex with BIX-01294, hanging drop vapor diffusion method, using 0.1 M HEPES pH 7.5, 18-20% (w/v) polyethylene glycol 4000 and 7-10% (v/v) isopropanol, in the absence or presence of DMSO (6-36% v/v)
-
molecular modelling and docking of 6-mer peptides H3K4 1-7, H3K9 5-11, H3K27 23-29, H3K36 32-38, H3K79 75-81, H4K20 16-22 with the catalytic domain of isoform NSD1, NSD2, NSD3
-
the ternary structures of SET7-estrogen receptor peptide-AdoMet analog are solved by molecular replacement
-
GENERAL STABILITY
ORGANISM
UNIPROT
LITERATURE
SMYD2 shows minimal activity in HEPES buffer with pH values below 7.5 and moderate activity in Tris buffer from pH 7.5 to pH 8.5
-
ORGANIC SOLVENT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
Tween-20
-
0.001% (w/v) Tween-20 enhances SMYD2 methyltransferase activity by more than 4fold. The enzyme remains stable in the presence of 0.01-0.05% (v/v) Tween-20
Purification/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
; Ni-NTA bead chromatography, glutathione bead chromatography, and Superdex 200 gel filtration
ammonium sulfateprecipitation, heparin-Sepharose column chromatography, DEAE 5PW column chromatography, Mono S column chromatography, and Superose 6 gel filtration
-
anti-FLAG antibody immunoprecipitation
-
Ni-NTA agarose column chromatography and Superdex 200 gel filtration
-
nickel-chelating column chromatography, HiTrap-Q column chromatography, and Superdex-75 and -200 gel filtration
-
Sepharose bead chromatography
-
tandem affinity purification
-
Cloned/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
; GST-SET domain fusion proteins are expressed in Escherichia coli, SET2-C is expressed in baculovirus insect cells
cotransfection of growth factor independent 1 with both HA epitope-tagged G9a and Myc epitope-tagged Suv39H1 into HeLa cells
-
expressed in Escherichia coli BL21 cells
-
expressed in Escherichia coli BL21(DE3) cells
-
expressed in HEK-293 cells
-
expressed in LNCaP, MCF-7, and A-549 cells
-
expressed in Sf21 insect cells
-
expressed in U2OS cells
-
expression in Escherichia coli and HEK-293 cell
expression of wild-type SET9 and mutants in Escherichia coli, His-tagged
-
FLAG-tagged and untagged SMYD3 proteins are expressed in HEK-293T and MCF-7 cells
-
for HMTase activity assays and glutathione S-transferase pull-down assays subcloned into pGEX-5X1 vector, for transactivation assays subcloned into pBIND vector, for coimmunoprecipitation assays subcloned into pFLAG-CMV4 vector, expressed in Escherichia coli strain BL21
-
glutathione-S-transferase-fusion protein, SET gene
into the pEGFP-C2 vector
recombinant full-length G9a is obtained using a baculoviral expression system
-
TAP-tagged protein is expressed in L929 cells
-
EXPRESSION
ORGANISM
UNIPROT
LITERATURE
RE-IIBP expression and histone methylation are increased in leukemia patients
-
the enzyme is overexpressed in human cancer cells
-
the expression of SET7/9 is not altered by tissue necrosis factor-alpha treatment
-
ENGINEERING
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
C483A
-
no activity, the SET domain cysteine 483 is a critical residue for the histone methyltransferase activity of RE-IIBP
DELTAGEE
-
the deletion mutant shows no histone methyltransferase activity
DELTANHSC
-
the deletion mutant shows no histone methyltransferase activity
G18A/G20A
-
the mutations impaire S-adenosyl-L-methionine binding and significantly decrease enzymatic activity
H2113K
-
methyltransferase-deficient mutant
H297A
-
catalytically inactive mutant
R1952W
-
mutation identifiied in Sotos patient, complete loss of activity
R1984Q
-
mutation identifiied in Sotos patient, complete loss of activity
R2017W
-
mutation identifiied in Sotos patient, complete loss of activity
R477A
-
no activity, the SET domain 477 is a critical residue for the histone methyltransferase activity of RE-IIBP
Y1997C
-
mutation identifiied in Sotos patient, complete loss of activity
Y245A
-
the mutant acts as a trimethylase
Y245F
-
the mutation converts the enzyme from a mono- to a dimethyltransferase
additional information
-
arginine 1122-to-histidine mutant of HYPB, both the HMTase activity and auto-methylation activity is significantly impaired
APPLICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
analysis
medicine
additional information
-
growth factor independent 1 interacts with G9a and recruits G9a and histone deacetylase 1 to its target promoters, including the cell cycle regulator p21Cip/WAF1 and other cell cycle regulators, in order to repress transcription through histone H3(K9) dimethylation
Show AA Sequence (126 entries)
Please use the Sequence Search for a specific query.