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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 PubMed
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