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Literature summary for 2.1.1.355 extracted from

  • Xiong, Y.; Li, F.; Babault, N.; Dong, A.; Zeng, H.; Wu, H.; Chen, X.; Arrowsmith, C.H.; Brown, P.J.; Liu, J.; Vedadi, M.; Jin, J.
    Discovery of potent and selective inhibitors for G9a-like protein (GLP) lysine methyltransferase (2017), J. Med. Chem., 60, 1876-1891 .
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.1.1.355

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Escherichia coli BL21(DE3) cells Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
in complex with S-adenosyl-L-methionine and either 6,7-dimethoxy-N-(1-methylpiperidin-4-yl)-2-morpholinoquinazolin-4-amine or N2-hexyl-6,7-dimethoxy-N4-(1-methylpiperidin-4-yl)quinazoline-2,4-diamine, hanging drop vapor diffusion method, using 20% (w/v) PEG 20,000, 2% (v/v) 1,4-dioxane, 0.1 M bicine (pH 9.0) Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
2-(4,4-difluoropiperidin-1-yl)-6,7-dimethoxy-N-(1-methylpiperidin-4-yl)quinazolin-4-amine
-
 Homo sapiens
2-(4,4-difluoropiperidin-1-yl)-6-methoxy-N-[1-(propan-2-yl)piperidin-4-yl]-7-[3-(pyrrolidin-1-yl)propoxy]quinazolin-4-amine
-
 Homo sapiens
2-(azepan-1-yl)-6,7-dimethoxy-N-(1-methylpiperidin-4-yl)-quinazolin-4-amine
-
 Homo sapiens
2-cyclohexyl-6,7-dimethoxy-N-(1-methylpiperidin-4-yl)-quinazolin-4-amine
-
 Homo sapiens
2-cyclohexyl-6-methoxy-N-[1-(propan-2-yl)piperidin-4-yl]-7-[3-(pyrrolidin-1-yl)propoxy]quinazolin-4-amine MS0124, selective inhibitor Homo sapiens
6,7-dimethoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine
-
 Homo sapiens
6,7-dimethoxy-2-morpholino-N-(1-propylpiperidin-4-yl)-quinazolin-4-amine
-
 Homo sapiens
6,7-dimethoxy-N-(1-methylpiperidin-4-yl)-2-(piperidin-1-yl)-quinazolin-4-amine
-
 Homo sapiens
6,7-dimethoxy-N-(1-methylpiperidin-4-yl)-2-(pyrrolidin-1-yl)-quinazolin-4-amine
-
 Homo sapiens
6,7-dimethoxy-N-(1-methylpiperidin-4-yl)-2-(tetrahydro-2H-pyran-4-yl)quinazolin-4-amine
-
 Homo sapiens
6,7-dimethoxy-N-(1-methylpiperidin-4-yl)-2-morpholinoquinazolin-4-amine
-
 Homo sapiens
6,7-dimethoxy-N2-methyl-N4-(1-methylpiperidin-4-yl)-N2-pentyl-quinazoline-2,4-diamine
-
 Homo sapiens
6,7-dimethoxy-N4-(1-methylpiperidin-4-yl)-N2-pentylquinazoline-2,4-diamine
-
 Homo sapiens
6-ethoxy-7-methoxy-N-(1-methylpiperidin-4-yl)-2-morpholinoquinazolin-4-amine
-
 Homo sapiens
6-fluoro-7-methoxy-N-(1-methylpiperidin-4-yl)-2-morpholinoquinazolin-4-amine
-
 Homo sapiens
6-isopropoxy-7-methoxy-N-(1-methylpiperidin-4-yl)-2-morpholinoquinazolin-4-amine
-
 Homo sapiens
6-methoxy-7-methyl-N-(1-methylpiperidin-4-yl)-2-morpholinoquinazolin-4-amine
-
 Homo sapiens
7-ethoxy-6-methoxy-N-(1-methylpiperidin-4-yl)-2-morpholinoquinazolin-4-amine
-
 Homo sapiens
7-fluoro-6-methoxy-N-(1-methylpiperidin-4-yl)-2-morpholinoquinazolin-4-amine
-
 Homo sapiens
7-isopropoxy-6-methoxy-N-(1-methylpiperidin-4-yl)-2-morpholinoquinazolin-4-amine
-
 Homo sapiens
7-methoxy-6-methyl-N-(1-methylpiperidin-4-yl)-2-morpholinoquinazolin-4-amine
-
 Homo sapiens
7-[(5-aminopentyl)oxy]-N4-[1-(5-aminopentyl)piperidin-4-yl]-N2-[3-(dimethylamino)propyl]-6-methoxyquinazoline-2,4-diamine
-
 Homo sapiens
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
7-[3-(dimethylamino)propoxy]-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine
-
 Homo sapiens
BIX01294
-
 Homo sapiens
E72 i.e. 7-[(5-aminopentyl)oxy]-N4-[-1-(5-aminopentyl)piperidin-4-yl]-N2-[3-(dimethylamino)propyl]-6-methoxyquinazoline-2,4-diamine Homo sapiens
N-(1-benzylpiperidin-4-yl)-6,7-dimethoxy-2-(4-methyl-1,4-diazepan-1-yl)quinazolin-4-amine
-
 Homo sapiens
N-(1-cyclopropylpiperidin-4-yl)-6,7-dimethoxy-2-morpholinoquinazolin-4-amine
-
 Homo sapiens
N-(1-ethylpiperidin-4-yl)-6,7-dimethoxy-2-morpholinoquinazolin-4-amine
-
 Homo sapiens
N-(1-isopropylpiperidin-4-yl)-6,7-dimethoxy-2-morpholinoquinazolin-4-amine
-
 Homo sapiens
N2-butyl-6,7-dimethoxy-N2-methyl-N4-(1-methylpiperidin-4-yl)-quinazoline-2,4-diamine
-
 Homo sapiens
N2-heptyl-6,7-dimethoxy-N4-(1-methylpiperidin-4-yl)-quinazoline-2,4-diamine
-
 Homo sapiens
N2-hexyl-6,7-dimethoxy-N2-methyl-N4-(1-methylpiperidin-4-yl)-quinazoline-2,4-diamine
-
 Homo sapiens
N2-hexyl-6,7-dimethoxy-N4-(1-methylpiperidin-4-yl)quinazoline-2,4-diamine MS012, selective inhibitor Homo sapiens
UNC0224
-
 Homo sapiens
UNC0321
-
 Homo sapiens
UNC0638
-
 Homo sapiens
UNC0642
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
3 S-adenosyl-L-methionine + a [histone H3]-L-lysine9 Homo sapiens overall reaction 3 S-adenosyl-L-homocysteine + a [histone H3]-N6,N6,N6-trimethyl-L-lysine9
-
 ?
S-adenosyl-L-methionine + a [histone H3]-L-lysine9 Homo sapiens
-
 S-adenosyl-L-homocysteine + a [histone H3]-N6-methyl-L-lysine9
-
 ?
S-adenosyl-L-methionine + a [histone H3]-N6,N6-dimethyl-L-lysine9 Homo sapiens preferred substrate S-adenosyl-L-homocysteine + a [histone H3]-N6,N6,N6-trimethyl-L-lysine9
-
 ?
S-adenosyl-L-methionine + a [histone H3]-N6-methyl-L-lysine9 Homo sapiens
-
 S-adenosyl-L-homocysteine + a [histone H3]-N6,N6-dimethyl-L-lysine9
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens Q96KQ7
-
-

Purification (Commentary)

Purification (Comment) Organism
HiTrap chelating column chromatography and Superdex S200 gel filtration Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3 S-adenosyl-L-methionine + a [histone H3]-L-lysine9 overall reaction Homo sapiens 3 S-adenosyl-L-homocysteine + a [histone H3]-N6,N6,N6-trimethyl-L-lysine9
-
 ?
3 S-adenosyl-L-methionine + biotinylated [histone H3]-L-lysine9
-
 Homo sapiens 3 S-adenosyl-L-homocysteine + biotinylated [histone H3]-N6-methyl-L-lysine9
-
 ?
S-adenosyl-L-methionine + a [histone H3]-L-lysine9
-
 Homo sapiens S-adenosyl-L-homocysteine + a [histone H3]-N6-methyl-L-lysine9
-
 ?
S-adenosyl-L-methionine + a [histone H3]-N6,N6-dimethyl-L-lysine9 preferred substrate Homo sapiens S-adenosyl-L-homocysteine + a [histone H3]-N6,N6,N6-trimethyl-L-lysine9
-
 ?
S-adenosyl-L-methionine + a [histone H3]-N6-methyl-L-lysine9
-
 Homo sapiens S-adenosyl-L-homocysteine + a [histone H3]-N6,N6-dimethyl-L-lysine9
-
 ?

Synonyms

Synonyms Comment Organism
EHMT2
-
 Homo sapiens
G9a
-
 Homo sapiens
KMT1C
-
 Homo sapiens