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Literature summary extracted from

  • Zhang, R.; Wang, J.; Zhao, L.; Liu, S.; Du, D.; Ding, H.; Chen, S.; Yue, L.; Liu, Y.C.; Zhang, C.; Liu, H.; Luo, C.
    Identification of novel inhibitors of histone acetyltransferase hMOF through high throughput screening (2018), Eur. J. Med. Chem., 157, 867-876 .
    View publication on PubMed

Cloned(Commentary)

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

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.3.1.48 (E)-4-(2-(5,6-dimethylbenzo[d]thiazol-2-yl)vinyl)-N,N-diethylbenzenesulfonamide 96% inhibition at 0.1 mM Homo sapiens
2.3.1.48 (E)-4-(2-(5-bromobenzo[d]thiazol-2-yl)vinyl)-N,N-diethylbenzenesulfonamide 82% inhibition at 0.1 mM Homo sapiens
2.3.1.48 (E)-4-(2-(5-chlorobenzo[d]thiazol-2-yl)vinyl)-N,N-diethylbenzenesulfonamide 89% inhibition at 0.1 mM Homo sapiens
2.3.1.48 (E)-4-(2-(6-bromobenzo[d]thiazol-2-yl)vinyl)-N,N-diethylbenzenesulfonamide 21% inhibition at 0.1 mM Homo sapiens
2.3.1.48 (E)-4-(2-(benzo[d]thiazol-2-yl)vinyl)-2-chloro-N,N-diethylbenzenesulfonamide 12% inhibition at 0.1 mM Homo sapiens
2.3.1.48 (E)-4-(2-(benzo[d]thiazol-2-yl)vinyl)-N,N-diethyl-2-fluorobenzenesulfonamide 18% inhibition at 0.1 mM; 28% inhibition at 0.1 mM Homo sapiens
2.3.1.48 (E)-4-(2-(benzo[d]thiazol-2-yl)vinyl)-N,N-diethyl-2-methylbenzenesulfonamide 30% inhibition at 0.1 mM Homo sapiens
2.3.1.48 (E)-4-(2-(benzo[d]thiazol-2-yl)vinyl)-N,N-diethylbenzenesulfonamide competitive inhibition, complete inhibition at 0.1 mM Homo sapiens
2.3.1.48 (E)-4-(2-(benzo[d]thiazol-2-yl)vinyl)-N,N-dimethylbenzenesulfonamide 14% inhibition at 0.1 mM Homo sapiens
2.3.1.48 (E)-4-(2-(benzo[d]thiazol-2-yl)vinyl)-N-(4-methoxyphenyl)benzenesulfonamide 28% inhibition at 0.1 mM Homo sapiens
2.3.1.48 (E)-4-(2-(benzo[d]thiazol-2-yl)vinyl)-N-(4-methylbenzyl)benzenesulfonamide 33% inhibition at 0.1 mM Homo sapiens
2.3.1.48 (E)-4-(2-(benzo[d]thiazol-2-yl)vinyl)-N-benzylbenzenesulfonamide 11% inhibition at 0.1 mM Homo sapiens
2.3.1.48 (E)-4-(2-(benzo[d]thiazol-2-yl)vinyl)-N-phenylbenzenesulfonamide 25% inhibition at 0.1 mM Homo sapiens
2.3.1.48 (E)-N,N-diethyl-4-(2-(5-fluorobenzo[d]thiazol-2-yl)vinyl)benzenesulfonamide 84% inhibition at 0.1 mM Homo sapiens
2.3.1.48 (E)-N,N-diethyl-4-(2-(5-methoxybenzo[d]thiazol-2-yl)vinyl)benzenesulfonamide 13% inhibition at 0.1 mM Homo sapiens
2.3.1.48 (E)-N,N-diethyl-4-(2-(5-methylbenzo[d]thiazol-2-yl)vinyl)benzenesulfonamide 14% inhibition at 0.1 mM Homo sapiens
2.3.1.48 2-[2-(4-heptylphenyl)ethyl]-6-hydroxybenzoic acid complete inhibition at 0.05 mM Homo sapiens
2.3.1.48 MG149 complete inhibition at 0.05 mM Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.3.1.48 acetyl-CoA + [histone H4]-L-lysine16 Homo sapiens
-
 CoA + [histone H4]-N6-acetyl-L-lysine16
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.3.1.48 Homo sapiens Q9H7Z6
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
2.3.1.48 HisTrap column chromatography and Superdex 75 gel filtration Homo sapiens

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.3.1.48 HCT-116 cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.3.1.48 acetyl-CoA + [histone H4]-L-lysine16
-
 Homo sapiens CoA + [histone H4]-N6-acetyl-L-lysine16
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.3.1.48 HAT
-
 Homo sapiens
2.3.1.48 KAT8
-
 Homo sapiens
2.3.1.48 Mof
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.3.1.48 0.006
-
 at pH 7.5 and 25°C Homo sapiens (E)-4-(2-(benzo[d]thiazol-2-yl)vinyl)-N,N-diethylbenzenesulfonamide
2.3.1.48 0.0077
-
 at pH 7.5 and 25°C Homo sapiens (E)-4-(2-(5,6-dimethylbenzo[d]thiazol-2-yl)vinyl)-N,N-diethylbenzenesulfonamide
2.3.1.48 0.015
-
 at pH 7.5 and 25°C Homo sapiens 2-[2-(4-heptylphenyl)ethyl]-6-hydroxybenzoic acid
2.3.1.48 0.03
-
 at pH 7.5 and 25°C Homo sapiens (E)-4-(2-(5-bromobenzo[d]thiazol-2-yl)vinyl)-N,N-diethylbenzenesulfonamide
2.3.1.48 0.03
-
 at pH 7.5 and 25°C Homo sapiens (E)-4-(2-(5-chlorobenzo[d]thiazol-2-yl)vinyl)-N,N-diethylbenzenesulfonamide
2.3.1.48 0.04
-
 at pH 7.5 and 25°C Homo sapiens (E)-N,N-diethyl-4-(2-(5-fluorobenzo[d]thiazol-2-yl)vinyl)benzenesulfonamide