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Literature summary 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

Cloned(Commentary)

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

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
2.1.1.355 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

EC Number Inhibitors Comment Organism Structure
2.1.1.355 2-(4,4-difluoropiperidin-1-yl)-6,7-dimethoxy-N-(1-methylpiperidin-4-yl)quinazolin-4-amine
-
 Homo sapiens
2.1.1.355 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
2.1.1.355 2-(azepan-1-yl)-6,7-dimethoxy-N-(1-methylpiperidin-4-yl)-quinazolin-4-amine
-
 Homo sapiens
2.1.1.355 2-cyclohexyl-6,7-dimethoxy-N-(1-methylpiperidin-4-yl)-quinazolin-4-amine
-
 Homo sapiens
2.1.1.355 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
2.1.1.355 6,7-dimethoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine
-
 Homo sapiens
2.1.1.355 6,7-dimethoxy-2-morpholino-N-(1-propylpiperidin-4-yl)-quinazolin-4-amine
-
 Homo sapiens
2.1.1.355 6,7-dimethoxy-N-(1-methylpiperidin-4-yl)-2-(piperidin-1-yl)-quinazolin-4-amine
-
 Homo sapiens
2.1.1.355 6,7-dimethoxy-N-(1-methylpiperidin-4-yl)-2-(pyrrolidin-1-yl)-quinazolin-4-amine
-
 Homo sapiens
2.1.1.355 6,7-dimethoxy-N-(1-methylpiperidin-4-yl)-2-(tetrahydro-2H-pyran-4-yl)quinazolin-4-amine
-
 Homo sapiens
2.1.1.355 6,7-dimethoxy-N-(1-methylpiperidin-4-yl)-2-morpholinoquinazolin-4-amine
-
 Homo sapiens
2.1.1.355 6,7-dimethoxy-N2-methyl-N4-(1-methylpiperidin-4-yl)-N2-pentyl-quinazoline-2,4-diamine
-
 Homo sapiens
2.1.1.355 6,7-dimethoxy-N4-(1-methylpiperidin-4-yl)-N2-pentylquinazoline-2,4-diamine
-
 Homo sapiens
2.1.1.355 6-ethoxy-7-methoxy-N-(1-methylpiperidin-4-yl)-2-morpholinoquinazolin-4-amine
-
 Homo sapiens
2.1.1.355 6-fluoro-7-methoxy-N-(1-methylpiperidin-4-yl)-2-morpholinoquinazolin-4-amine
-
 Homo sapiens
2.1.1.355 6-isopropoxy-7-methoxy-N-(1-methylpiperidin-4-yl)-2-morpholinoquinazolin-4-amine
-
 Homo sapiens
2.1.1.355 6-methoxy-7-methyl-N-(1-methylpiperidin-4-yl)-2-morpholinoquinazolin-4-amine
-
 Homo sapiens
2.1.1.355 7-ethoxy-6-methoxy-N-(1-methylpiperidin-4-yl)-2-morpholinoquinazolin-4-amine
-
 Homo sapiens
2.1.1.355 7-fluoro-6-methoxy-N-(1-methylpiperidin-4-yl)-2-morpholinoquinazolin-4-amine
-
 Homo sapiens
2.1.1.355 7-isopropoxy-6-methoxy-N-(1-methylpiperidin-4-yl)-2-morpholinoquinazolin-4-amine
-
 Homo sapiens
2.1.1.355 7-methoxy-6-methyl-N-(1-methylpiperidin-4-yl)-2-morpholinoquinazolin-4-amine
-
 Homo sapiens
2.1.1.355 7-[(5-aminopentyl)oxy]-N4-[1-(5-aminopentyl)piperidin-4-yl]-N2-[3-(dimethylamino)propyl]-6-methoxyquinazoline-2,4-diamine
-
 Homo sapiens
2.1.1.355 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
2.1.1.355 7-[3-(dimethylamino)propoxy]-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine
-
 Homo sapiens
2.1.1.355 BIX01294
-
 Homo sapiens
2.1.1.355 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
2.1.1.355 N-(1-benzylpiperidin-4-yl)-6,7-dimethoxy-2-(4-methyl-1,4-diazepan-1-yl)quinazolin-4-amine
-
 Homo sapiens
2.1.1.355 N-(1-cyclopropylpiperidin-4-yl)-6,7-dimethoxy-2-morpholinoquinazolin-4-amine
-
 Homo sapiens
2.1.1.355 N-(1-ethylpiperidin-4-yl)-6,7-dimethoxy-2-morpholinoquinazolin-4-amine
-
 Homo sapiens
2.1.1.355 N-(1-isopropylpiperidin-4-yl)-6,7-dimethoxy-2-morpholinoquinazolin-4-amine
-
 Homo sapiens
2.1.1.355 N2-butyl-6,7-dimethoxy-N2-methyl-N4-(1-methylpiperidin-4-yl)-quinazoline-2,4-diamine
-
 Homo sapiens
2.1.1.355 N2-heptyl-6,7-dimethoxy-N4-(1-methylpiperidin-4-yl)-quinazoline-2,4-diamine
-
 Homo sapiens
2.1.1.355 N2-hexyl-6,7-dimethoxy-N2-methyl-N4-(1-methylpiperidin-4-yl)-quinazoline-2,4-diamine
-
 Homo sapiens
2.1.1.355 N2-hexyl-6,7-dimethoxy-N4-(1-methylpiperidin-4-yl)quinazoline-2,4-diamine MS012, selective inhibitor Homo sapiens
2.1.1.355 UNC0224
-
 Homo sapiens
2.1.1.355 UNC0321
-
 Homo sapiens
2.1.1.355 UNC0638
-
 Homo sapiens
2.1.1.355 UNC0642
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.1.1.355 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
-
 ?
2.1.1.355 S-adenosyl-L-methionine + a [histone H3]-L-lysine9 Homo sapiens
-
 S-adenosyl-L-homocysteine + a [histone H3]-N6-methyl-L-lysine9
-
 ?
2.1.1.355 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
-
 ?
2.1.1.355 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

EC Number Organism UniProt Comment Textmining
2.1.1.355 Homo sapiens Q96KQ7
-
-

Purification (Commentary)

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

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.1.1.355 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
-
 ?
2.1.1.355 3 S-adenosyl-L-methionine + biotinylated [histone H3]-L-lysine9
-
 Homo sapiens 3 S-adenosyl-L-homocysteine + biotinylated [histone H3]-N6-methyl-L-lysine9
-
 ?
2.1.1.355 S-adenosyl-L-methionine + a [histone H3]-L-lysine9
-
 Homo sapiens S-adenosyl-L-homocysteine + a [histone H3]-N6-methyl-L-lysine9
-
 ?
2.1.1.355 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
-
 ?
2.1.1.355 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

EC Number Synonyms Comment Organism
2.1.1.355 EHMT2
-
 Homo sapiens
2.1.1.355 G9a
-
 Homo sapiens
2.1.1.355 KMT1C
-
 Homo sapiens