Literature summary for 2.3.1.48 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 .

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Cloned(Commentary)

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

Inhibitors

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

Natural Substrates/ Products (Substrates)

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

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	Q9H7Z6	-	-

Purification (Commentary)

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

Source Tissue

Source Tissue	Comment	Organism	Textmining
HCT-116 cell	-	Homo sapiens	-

Substrates and Products (Substrate)

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

Synonyms

Synonyms	Comment	Organism
HAT	-	Homo sapiens
KAT8	-	Homo sapiens
Mof	-	Homo sapiens

IC50 Value

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

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Release 2023.1 (January 2023)