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Literature summary extracted from

  • Wapenaar, H.; van der Wouden, P.E.; Groves, M.R.; Rotili, D.; Mai, A.; Dekker, F.J.
    Enzyme kinetics and inhibition of histone acetyltransferase KAT8 (2015), Eur. J. Med. Chem., 105, 289-296.
    View publication on PubMedView publication on EuropePMC

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.3.1.48 (4E)-2-(4-acetylphenyl)-4-[[5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl]methylidene]-5-methyl-2,4-dihydro-3H-pyrazol-3-one
-
 Homo sapiens
2.3.1.48 2-(heptylsulfanyl)-1-(2-hydroxyphenyl)ethan-1-one
-
 Homo sapiens
2.3.1.48 2-butyl-6-hydroxybenzoic acid
-
 Homo sapiens
2.3.1.48 2-decyl-6-hydroxybenzoic acid 88% inhibition at 0.05 mM Homo sapiens
2.3.1.48 2-hydroxy-5-pentadecylbenzoic acid 85% inhibition at 0.05 mM Homo sapiens
2.3.1.48 2-hydroxy-5-pentylbenzoic acid
-
 Homo sapiens
2.3.1.48 2-hydroxy-6-(11-hydroxyundecyl)benzoic acid
-
 Homo sapiens
2.3.1.48 2-hydroxy-6-(5-hydroxypentyl)benzoic acid
-
 Homo sapiens
2.3.1.48 2-hydroxy-6-pentadecylbenzoic acid i.e. anacardic acid, 97% inhibition at 0.05 mM Homo sapiens
2.3.1.48 5-decyl-2-hydroxybenzoic acid 95% inhibition at 0.05 mM Homo sapiens
2.3.1.48 anacardic acid
-
 Homo sapiens
2.3.1.48 additional information no inhibition by 14, 11c, 13, 8a, and 8b; no inhibition by 2-hydroxy-5-pentylbenzoic acid, 2-hydroxy-6-(5-hydroxypentyl)benzoic acid, and (4E)-2-(4-acetylphenyl)-4-[[5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl]methylidene]-5-methyl-2,4-dihydro-3H-pyrazol-3-one Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
2.3.1.48 additional information
-
 additional information kinetics and catalytic mechanism of the bi-substrate enzyme KAT8, non-linear Michaelis-Menten regression, overview Homo sapiens
2.3.1.48 0.0011
-
 acetyl-CoA at 0.015 mM histone H4 peptide, pH and temperature not specified in the publication Homo sapiens
2.3.1.48 0.0012
-
 acetyl-CoA at 0.030 mM histone H4 peptide, pH and temperature not specified in the publication Homo sapiens
2.3.1.48 0.0021
-
 acetyl-CoA at 0.060 mM histone H4 peptide, pH and temperature not specified in the publication Homo sapiens
2.3.1.48 0.0028
-
 acetyl-CoA at 0.090 mM histone H4 peptide, pH and temperature not specified in the publication Homo sapiens

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
2.3.1.48 nucleus
-
 Homo sapiens 5634
-

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 Homo sapiens
-
 CoA + acetylhistone
-
 ?
2.3.1.48 acetyl-CoA + histone H4 Homo sapiens acetylation of Lys16 CoA + acetylhistone H4
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.3.1.48 Homo sapiens Q09472
-
-
2.3.1.48 Homo sapiens Q9H7Z6
-
-

Reaction

EC Number Reaction Comment Organism Reaction ID
2.3.1.48 acetyl-CoA + [protein]-L-lysine = CoA + [protein]-N6-acetyl-L-lysine ping-pong catalytic mechanism of bi-substrate histone acetyltransferase KAT8 Homo sapiens
a

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.3.1.48 acetyl-CoA + histone
-
 Homo sapiens CoA + acetylhistone
-
 ?
2.3.1.48 acetyl-CoA + histone
-
 Homo sapiens CoA + acetylhistone in the assay the CoA thiolate is detected by the thiol sensitive fluorescent dye 7-diethylamino-3-(4'-maleimidylphenyl)-4-methylcoumarin ?
2.3.1.48 acetyl-CoA + histone H4 acetylation of Lys16 Homo sapiens CoA + acetylhistone H4
-
 ?
2.3.1.48 acetyl-CoA + histone H4 acetylation of Lys16 Homo sapiens CoA + acetylhistone H4 in the assay the CoA thiolate is detected by the thiol sensitive fluorescent dye 7-diethylamino-3-(4'-maleimidylphenyl)-4-methylcoumarin ?
2.3.1.48 acetyl-CoA + histone H4 peptide a synthetic peptide corresponding to the first 20 amino acids of the histone H4 N-terminus Homo sapiens CoA + acetylhistone H4 peptide
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.3.1.48 HAT
-
 Homo sapiens
2.3.1.48 KAT8
-
 Homo sapiens
2.3.1.48 p300
-
 Homo sapiens

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
2.3.1.48 0.0033
-
 acetyl-CoA at 0.015 mM histone H4 peptide, pH and temperature not specified in the publication Homo sapiens
2.3.1.48 0.005
-
 acetyl-CoA at 0.030 mM histone H4 peptide, pH and temperature not specified in the publication Homo sapiens
2.3.1.48 0.012
-
 acetyl-CoA at 0.060 mM histone H4 peptide, pH and temperature not specified in the publication Homo sapiens
2.3.1.48 0.018
-
 acetyl-CoA at 0.090 mM histone H4 peptide, pH and temperature not specified in the publication Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
2.3.1.48 acetyl-CoA
-
 Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.3.1.48 0.037
-
 2-decyl-6-hydroxybenzoic acid pH and temperature not specified in the publication Homo sapiens
2.3.1.48 0.057
-
 5-decyl-2-hydroxybenzoic acid pH and temperature not specified in the publication Homo sapiens
2.3.1.48 0.064
-
 2-hydroxy-6-pentadecylbenzoic acid pH and temperature not specified in the publication Homo sapiens
2.3.1.48 0.079
-
 2-hydroxy-5-pentadecylbenzoic acid pH and temperature not specified in the publication Homo sapiens
2.3.1.48 0.157
-
 2-hydroxy-6-(11-hydroxyundecyl)benzoic acid pH and temperature not specified in the publication Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.3.1.48 0.32
-
 pH and temperature not specified in the publication Homo sapiens (4E)-2-(4-acetylphenyl)-4-[[5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl]methylidene]-5-methyl-2,4-dihydro-3H-pyrazol-3-one

General Information

EC Number General Information Comment Organism
2.3.1.48 evolution histone acetyltransferase KAT8 is a member of the MYST family Homo sapiens
2.3.1.48 evolution histone acetyltransferase p300 is a member of the p300/CBP family Homo sapiens
2.3.1.48 physiological function lysine acetyltransferase 8 is a histone acetyltransferase responsible for acetylating lysine 16 on histone H4 and plays a role in cell cycle progression as well as acetylation of the tumor suppressor protein p53 Homo sapiens