2.3.1.286: protein acetyllysine N-acetyltransferase
This is an abbreviated version!
For detailed information about protein acetyllysine N-acetyltransferase, go to the full flat file.
Word Map on EC 2.3.1.286
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2.3.1.286
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deacetylation
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resveratrol
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nad+-dependent
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nicotinamide
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deacetylases
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endothelial
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longevity
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peroxisome
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cardiac
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tnf
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obesity
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proliferator-activated
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cardiovascular
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dismutase
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neurodegenerative
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chromatin
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neuroprotective
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lifespan
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sirna
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myocardial
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amp-activated
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fibrosis
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adipose
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polyphenolic
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high-fat
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cardiomyocytes
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forkhead
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calorie
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alzheimer
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hdacs
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obese
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adipocytes
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sod2
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steatosis
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caspase-3
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nafld
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cardioprotective
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foxo3a
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senescence-associated
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aging-related
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mir-34a
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hyperacetylation
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anti-aging
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nampt
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tfam
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mnsod
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p-ampk
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monophosphate-activated
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coactivator-1
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non-histone
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medicine
- 2.3.1.286
-
deacetylation
- resveratrol
-
nad+-dependent
- nicotinamide
- deacetylases
- endothelial
-
longevity
- peroxisome
- cardiac
- tnf
- obesity
-
proliferator-activated
- cardiovascular
- dismutase
- neurodegenerative
- chromatin
-
neuroprotective
-
lifespan
- sirna
- myocardial
-
amp-activated
- fibrosis
- adipose
-
polyphenolic
-
high-fat
- cardiomyocytes
-
forkhead
-
calorie
- alzheimer
- hdacs
-
obese
- adipocytes
- sod2
- steatosis
- caspase-3
- nafld
-
cardioprotective
-
foxo3a
-
senescence-associated
-
aging-related
-
mir-34a
-
hyperacetylation
-
anti-aging
- nampt
- tfam
- mnsod
-
p-ampk
-
monophosphate-activated
- coactivator-1
-
non-histone
- medicine
Reaction
Synonyms
Af2Sir2, Clr3, CobB, HDAC, histone deacetylase, Hst1, HST2, Hst2p, KAT, More, NAD+-dependent protein deacetylase, NAD-dependent histone deacetylase, NAD-dependent protein deacetylase, nicotinamide adenine dinucleotide-dependent protein deacetylase, patZ, peptidyl-lysine N-acetyltransferase, phnO, protein lysine acetyltransferase, protein lysine deacetylase, Rv1151c, silent information regulator 2, Sir-2, Sir2, SIR2-Af1, Sir2-Af2, Sir2A, Sir2Af2, Sir2alpha, Sir2p, SIRT1, SIRT2, SIRT3, SIRT5, sirtuin, sirtuin 1, sirtuin 3, sirtuin-2 deacetylase, YfiQ, YiaC, YjaB
ECTree
2.3.1.286 protein acetyllysine N-acetyltransferaseAdvanced search results
results (
results (Inhibitors
Inhibitors on EC 2.3.1.286 - protein acetyllysine N-acetyltransferase
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INHIBITOR 
ORGANISM
UNIPROT
COMMENTARY 
LITERATURE
IMAGE
(4R)-1-(tert-butoxycarbonyl)-4-hydroxyprolyl-N-benzyl-N6-ethanethioyl-L-lysinamide
Q96EB6
0.05 mM, 83.4% inhibition
(4R)-1-(tert-butoxycarbonyl)-N-[(2S)-6-(ethanethioylamino)-1-oxo-1-[(2-oxo-2-phenylethyl)amino]hexan-2-yl]-4-hydroxyprolinamide
Q96EB6
0.05 mM, 97.1% inhibition
(4R)-4-hydroxyprolyl-N-benzyl-N6-ethanethioyl-L-lysinamide
Q96EB6
0.05 mM, 89.3% inhibition
(4R)-N-[(2S)-6-(ethanethioylamino)-1-oxo-1-[(2-oxo-2-phenylethyl)amino]hexan-2-yl]-4-hydroxyprolinamide
Q96EB6
0.05 mM, 96.8% inhibition
(5E)-1-ethyl-5-(1H-indol-3-ylmethylidene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
10% inhibition at 0.05 mM
(5E)-5-(1H-indol-3-ylmethylidene)-1-methyl-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
17% inhibition at 0.05 mM; 20% inhibition at 0.05 mM
(5E)-5-[4-(benzyloxy)benzylidene]-1-(prop-2-en-1-yl)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
13% inhibition at 0.05 mM
(5E)-5-[4-(benzyloxy)benzylidene]-1-ethyl-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
25% inhibition at 0.05 mM
(5E)-5-[4-(benzyloxy)benzylidene]-1-methyl-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
22% inhibition at 0.05 mM
(5E)-5-[[5-(2,3-dichlorophenyl)furan-2-yl]methylidene]-1-(prop-2-en-1-yl)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
41% inhibition at 0.05 mM
(7aS,12aS)-7-(4-chlorophenyl)-1,6,7,7a,12,12a-hexahydroindolo[3,2-c]pyrazolo[3,4-f]quinoline
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about 5% inhibition at 0.05 mM
(7aS,12aS)-7-(4-methoxyphenyl)-1,6,7,7a,12,12a-hexahydroindolo[3,2-c]pyrazolo[3,4-f]quinoline
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about 38% inhibition at 0.05 mM
(7aS,12aS)-7-phenyl-1,6,7,7a,12,12a-hexahydroindolo[3,2-c]pyrazolo[3,4-f]quinoline
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about 18% inhibition at 0.05 mM
(7aS,12aS)-7-[4-(thiophen-2-yl)phenyl]-1,6,7,7a,12,12a-hexahydroindolo[3,2-c]pyrazolo[3,4-f]quinoline
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about 16% inhibition at 0.05 mM
(7aS,12aS)-9-bromo-7-(4-chlorophenyl)-1,6,7,7a,12,12a-hexahydroindolo[3,2-c]pyrazolo[3,4-f]quinoline
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about 50% inhibition at 0.05 mM
(7aS,12aS)-9-bromo-7-(4-fluorophenyl)-1,6,7,7a,12,12a-hexahydroindolo[3,2-c]pyrazolo[3,4-f]quinoline
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about 65% inhibition at 0.05 mM
(7aS,12aS)-9-bromo-7-(4-methoxyphenyl)-1,6,7,7a,12,12a-hexahydroindolo[3,2-c]pyrazolo[3,4-f]quinoline
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about 65% inhibition at 0.05 mM
(7aS,12aS)-9-bromo-7-phenyl-1,6,7,7a,12,12a-hexahydroindolo[3,2-c]pyrazolo[3,4-f]quinoline
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about 70% inhibition at 0.05 mM
(7aS,12aS)-9-bromo-7-[4-(furan-2-yl)phenyl]-1,6,7,7a,12,12a-hexahydroindolo[3,2-c]pyrazolo[3,4-f]quinoline
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about 78% inhibition at 0.05 mM
1-(tert-butoxycarbonyl)prolyl-N-benzyl-N6-ethanethioyl-L-lysinamide
Q96EB6
0.05 mM, 93.7% inhibition
2-(N-(4-chlorophenyl)-N-methylsulfamoyl)-N-(4-cyano-2-fluorophenyl)isonicotinamide
highly selective inhibitor for SIRT2, low inhibition of SIRT1 and SIRT3
2-(N-(4-chlorophenyl)-N-methylsulfamoyl)-N-(4-cyanophenyl)isonicotinamide
selective inhibitor for SIRT2, low inhibition of SIRT1 and SIRT3
2-[1-[3-(amidinothio)propyl]-1H-indol-3-yl]-3-(1-methylindol-3-yl)maleimide methanesulfonate
i.e. Ro 31-8220; i.e. Ro 31-8220; i.e. Ro 31-8220
3-((2-methoxynaphthalen-1-yl)methyl)-7-((2-methylbenzyl)amino)-5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4(3H)-one
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3-((2-methoxynaphthalen-1-yl)methyl)-7-((pyridin-3-ylmethyl)amino)-5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4(3H)-one
i.e. ICL-SIRT078, a substrate-competitive SIRT2 inhibitor with more than 50fold selectivity against SIRT1, 3 and 5. Treatment of MCF-7 breast cancer cells with ICL-SIRT078 results in hyperacetylation of alpha-tubulin, an established SIRT2 biomarker, at doses comparable with the biochemical IC50 data, while suppressing MCF-7 proliferation at higher concentrations
3-((2-methoxynaphthalen-1-yl)methyl)-7-((thiophen-2-ylmethyl)-amino)-5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4(3H)-one
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3-((2-methoxynaphthalen-1-yl)methyl)-7-(neopentylamino)-5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4(3H)-one
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3-(azepan-1-ylsulfonyl)-N-(3-nitrophenyl)benzamide
highly selective inhibitor for SIRT2, low inhibition of SIRT1 and SIRT3
3-(N-(4-acetylphenyl)-N-methylsulfamoyl)-N-(4-chlorophenyl)benzamide
highly selective inhibitor for SIRT2, no inhibition of SIRT1, low inhibition of and SIRT3
3-(N-(4-acetylphenyl)-N-methylsulfamoyl)-N-(4-cyanophenyl)benzamide
highly selective inhibitor for SIRT2, low inhibition of SIRT1 and SIRT3
3-(N-(4-acetylphenyl)-N-methylsulfamoyl)-N-(5-chloropyridin-2-yl)benzamide
highly selective inhibitor for SIRT2, low inhibition of SIRT1, no inhibition of and SIRT3
3-(N-(4-bromophenyl)-N-methylsulfamoyl)-N-(4-chloro-2-fluorophenyl)-N-methylbenzamide
highly selective inhibitor for SIRT2, low inhibition of SIRT1 and SIRT3
3-(N-(4-chlorophenyl)-N-methylsulfamoyl)-N-(4-(methylsulfinyl)phenyl)benzamide
highly selective inhibitor for SIRT2, no inhibition of SIRT1, low inhibition of and SIRT3
3-(N-(4-chlorophenyl)-N-methylsulfamoyl)-N-(4-(methylsulfonyl)phenyl)benzamide
highly selective inhibitor for SIRT2, low inhibition of SIRT1 and SIRT3
3-(N-(4-chlorophenyl)-N-methylsulfamoyl)-N-(4-cyano-2-fluorophenyl)benzamide
highly selective inhibitor for SIRT2, low inhibition of SIRT1 and SIRT3
3-(N-(4-chlorophenyl)-N-methylsulfamoyl)-N-(4-cyanophenyl)benzamide
highly selective inhibitor for SIRT2, low inhibition of SIRT1, no inhibition of and SIRT3
3-(N-(4-chlorophenyl)-N-methylsulfamoyl)-N-(5-cyanopyridin-2-yl)benzamide
highly selective inhibitor for SIRT2, low inhibition of SIRT1, no inhibition of and SIRT3
3-(N-(4-chlorophenyl)-N-methylsulfamoyl)-N-(5-fluoropyridin-2-yl)benzamide
highly selective inhibitor for SIRT2, no inhibition of SIRT1 and SIRT3
3-(N-(4-chlorophenyl)-N-methylsulfamoyl)-N-(6-chloropyridazin-3-yl)benzamide
highly selective inhibitor for SIRT2, low inhibition of SIRT1
3-(N-(5-chloropyridin-2-yl)-N-methylsulfamoyl)-N-(4-cyanophenyl)benzamide
highly selective inhibitor for SIRT2, low inhibition of SIRT1 and SIRT3
4-bromo-N-(3-(N-methyl-N-(4-(methylsulfonyl)phenyl)sulfamoyl)phenyl)benzamide
selective inhibitor for SIRT2, low inhibition of SIRT1 and SIRT3
5-(1H-indol-3-ylmethylidene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
14% inhibition at 0.05 mM
5-(biphenyl-4-ylmethylidene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
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5-[(1-benzyl-1H-indol-3-yl)methylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
20% inhibition at 0.05 mM
5-[(6-methoxynaphthalen-1-yl)methylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
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5-[4-(benzyloxy)benzylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
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5-[4-(propan-2-yl)benzylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
13% inhibition at 0.05 mM
5-[4-[(2-chlorobenzyl)oxy]-3-methoxybenzylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
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5-[4-[(4-bromobenzyl)oxy]benzylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
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5-[[5-(2,3-dichlorophenyl)furan-2-yl]methylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
30% inhibition at 0.05 mM
7-((3-fluorobenzyl)amino)-3-((2-methoxynaphthalen-1-yl)methyl)-5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4(3H)-one
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7-((3-methoxybenzyl)amino)-3-((2-methoxynaphthalen-1-yl)-methyl)-5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4(3H)-one
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7-(benzylamino)-3-((2-methoxynaphthalen-1-yl)methyl)-5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4(3H)-one
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macrocyclic peptide inhibitor S2iL5
the inhibitor binds to the active site of SIRT2 through extensive interactions. The inhibitor induces an open-to-closed domain movement and a helix-to-coil transition in a SIRT2-specific region
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methyl N2-(tert-butoxycarbonyl)-N6-ethanethioyl-L-lysyl-D-alaninate
Q96EB6
0.05 mM, 81.3% inhibition
N-(3-(N-(4-chlorophenyl)-N-methylsulfamoyl)phenyl)-4-cyanobenzamide
highly selective inhibitor for SIRT2, low inhibition of SIRT1, no inhibition of and SIRT3
N-(4-acetylphenyl)-3-(N-(4-acetylphenyl)-N-methylsulfamoyl)benzamide
highly selective inhibitor for SIRT2, no inhibition of SIRT1 and SIRT3
N-(4-bromo-2-fluorophenyl)-3-(N-(4-bromophenyl)-N-methylsulfamoyl)-N-methylbenzamide
highly selective inhibitor for SIRT2, no inhibition of SIRT1 and SIRT3
N-(4-chlorophenyl)-3-(N-methyl-N-(4-(methylsulfonyl)phenyl)sulfamoyl)benzamide
highly selective inhibitor for SIRT2, no inhibition of SIRT1 and SIRT3
N-(4-cyanophenyl)-3-(N-(4-(1-hydroxyethyl)phenyl)-N-methylsulfamoyl)benzamide
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N-(4-cyanophenyl)-3-(N-(4-fluorophenyl)-N-methylsulfamoyl)benzamide
highly selective inhibitor for SIRT2, low inhibition of SIRT1 and SIRT3
N-(4-cyanophenyl)-3-(N-(4-methoxyphenyl)-N-methylsulfamoyl)benzamide
highly selective inhibitor for SIRT2, low inhibition of SIRT1 and SIRT3
N-(4-cyanophenyl)-3-(N-methyl-N-(4-(methylsulfonyl)phenyl)sulfamoyl)benzamide
highly selective inhibitor for SIRT2, low inhibition of SIRT1, no inhibition of and SIRT3
N-[(2S)-6-(ethanethioylamino)-1-oxo-1-[(2-oxo-2-phenylethyl)amino]hexan-2-yl]-5-oxoprolinamide
Q96EB6
0.05 mM, 98.2% inhibition
N-[(2S)-6-(ethanethioylamino)-1-[[2-(morpholin-4-yl)ethyl]amino]-1-oxohexan-2-yl]-6-oxoheptanamide
Q96EB6
0.05 mM, 61.1% inhibition
N2-(tert-butoxycarbonyl)-N6-ethanethioyl-N-[2-(4-methoxyphenyl)-2-oxoethyl]-L-lysinamide
Q96EB6
0.05 mM, 95.6% inhibition
N2-(tert-butoxycarbonyl)-N6-ethanethioyl-N-[2-(morpholin-4-yl)ethyl]-L-lysinamide
Q96EB6
0.05 mM, 37.5% inhibition
N2-[(benzyloxy)carbonyl]-N6-ethanethioyl-N-[2-(morpholin-4-yl)ethyl]-L-lysinamide
Q96EB6
0.05 mM, 54.9% inhibition
N6-ethanethioyl-N2-(6-oxoheptanoyl)-N-(2-oxo-2-phenylethyl)-L-lysinamide
Q96EB6
0.05 mM, 97.7% inhibition
6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide
i.e. EX-527; i.e. EX-527; i.e. EX-527
Isonicotinamide
Q96EB6, Q9NTG7
weak competitive inhibitor of hSIRT3 with respect to NAD+ in vitro; weak inhibitor
meta-azi-propofol
only binds specifically and competitively to the enzyme when co-equilibrated with other substrates
meta-azi-propofol
-
only binds specifically and competitively to the enzyme when co-equilibrated with other substrates
nicotinamide
Q96EB6, Q9NTG7
mixed noncompetitive inhibitor. Inhibition of SIRT3 involves apparent competition between the inhibitor and the enzyme cofactor NAD+; predominantly noncompetitive inhibitor
nicotinamide
-
noncompetitive inhibitor versus NAD+. 95% inhibition at 1.5 mM
propofol
only binds specifically and competitively to the enzyme when co-equilibrated with other substrates
propofol
-
only binds specifically and competitively to the enzyme when co-equilibrated with other substrates
additional information
no inhibition at 0.05 mM: (5E)-1-ethyl-5-(1H-indol-3-ylmethylidene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione; no inhibition at 0.05 mM: (5E)-5-[4-(benzyloxy)benzylidene]-1-(prop-2-en-1-yl)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione; no inhibition by EX-527, HR 103 or Ro 31-8220; no inhibition by EX-527, HR 103 or Ro 31-8220; no inhibition by EX-527, HR 103 or Ro 31-8220
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additional information
Q96EB6
no inhibition at 0.05 mM: (5E)-1-ethyl-5-(1H-indol-3-ylmethylidene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione; no inhibition at 0.05 mM: (5E)-5-[4-(benzyloxy)benzylidene]-1-(prop-2-en-1-yl)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione; no inhibition by EX-527, HR 103 or Ro 31-8220; no inhibition by EX-527, HR 103 or Ro 31-8220; no inhibition by EX-527, HR 103 or Ro 31-8220
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additional information
no inhibition at 0.05 mM: (5E)-1-ethyl-5-(1H-indol-3-ylmethylidene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione; no inhibition at 0.05 mM: (5E)-5-[4-(benzyloxy)benzylidene]-1-(prop-2-en-1-yl)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione; no inhibition by EX-527, HR 103 or Ro 31-8220; no inhibition by EX-527, HR 103 or Ro 31-8220; no inhibition by EX-527, HR 103 or Ro 31-8220
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