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Information on EC 2.3.1.48 - histone acetyltransferase and Organism(s) Homo sapiens and UniProt Accession Q09472

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EC Tree
     2 Transferases
         2.3 Acyltransferases
             2.3.1 Transferring groups other than aminoacyl groups
                2.3.1.48 histone acetyltransferase
IUBMB Comments
A group of enzymes acetylating histones. Several of the enzymes can also acetylate lysines in other proteins [3,4].
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Select one or more organisms in this record: ?
This record set is specific for:
Homo sapiens
UNIPROT: Q09472
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Word Map
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The taxonomic range for the selected organisms is: Homo sapiens
The enzyme appears in selected viruses and cellular organisms
Synonyms
clock, histone acetyltransferase, n-acetyltransferase, tip60, histone acetyltransferases, cbp/p300, creb-binding protein, ep300, crebbp, creb binding protein, more
SYNONYM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
CREB binding protein
-
histone acetyltransferases
-
lysine acetyltransferase
-
p300 HAT
UniProt
p300/CBP associated factor
-
acetyltransferase, histone
-
-
-
-
ARD1 acetyltransferase
-
arrest defective 1
-
arrest defective protein 1 acetyltransferase
-
ATase1
-
-
ATase2
-
-
circadian locomoter output cycles protein kaput
UniProt
CREB binding protein
-
CREBBP
factor acetyltransferase
-
enzyme form A is also able to acetylate nonhistone proteins, mostly transcription factors, overview
FAT
-
when acetylating nonhistone transcription factor proteins, factor specific, overview
Gcn5 related N-acetyltransferase
-
general control non-derepressible 5
-
-
GNAT-related histone acetyltransferase complex
-
PCAF, STAGA or TFTC
histone (H4 K16) acetyltransferase
-
histone acetokinase
-
-
-
-
histone acetyl transferase
-
histone acetylase
histone acetyltransferase
histone acetyltransferase 1
-
histone acetyltransferase Tip60
-
-
histone acetyltransferases
-
histone H4 acetyltransferase
-
-
histone H4 lysine 16 acetyltransferase
-
histone transacetylase
-
-
-
-
human acetylase binding to ORC1
-
-
KAT2A/GCN5
-
lysine acetyltransferase
lysine acetyltransferase 2
-
lysine acetyltransferase 2A
-
lysine acetyltransferase 2B
-
lysine acetyltransferase 5
-
lysine acetyltransferase 8
-
MORF histone acetyltransferase
-
-
MOZ histone acetyltransferase
-
-
Myb-binding protein 1A
UniProt
MYST protein lysine acetyltransferase
-
-
MYST-related histone acetyltransferase complex
-
Tip60
MYST1
N(alpha)-acetyltransferase 10
-
N-terminal acetyltransferase
-
NCoA-1
UniProt
NCoA-3
UniProt
nuclear receptor coactivator 1
UniProt
nuclear receptor coactivator 3
UniProt
nucleosome-histone acetyltransferase
-
-
-
-
P/CAF histone acetyltransferase
-
-
p300 histone acetyltransferase
-
-
p300/CBP
-
CREB-binding protein (KAT3A) is a homologue to p300 (KAT3B)
p300/CBP associated factor
p300/CBP histone acetyltransferase
-
-
P300/CBP-associated factor
p300/CBP-associated factor (pCAF)
-
representing residues 492-658
p300HAT
-
-
PCAF histone acetyltransferase
-
-
TAF1
-
-
Tat-interactive protein, 60 kDa
-
-
Tip60
tumor suppressor histone H3 lysine 23 acetyltransferase
-
additional information
REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
acetyl-CoA + [protein]-L-lysine = CoA + [protein]-N6-acetyl-L-lysine
show the reaction diagram
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
Acyl group transfer
-
-
-
-
SYSTEMATIC NAME
IUBMB Comments
acetyl-CoA:[protein]-L-lysine acetyltransferase
A group of enzymes acetylating histones. Several of the enzymes can also acetylate lysines in other proteins [3,4].
CAS REGISTRY NUMBER
COMMENTARY hide
9054-51-7
-
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
3-azidopropionyl-CoA + [histone peptide H3-20]-L-lysine
CoA + [histone peptide H3-20]-N6-3-azidopropionyl-L-lysine
show the reaction diagram
-
-
-
?
3-azidopropionyl-CoA + [histone peptide H4-20]-L-lysine
CoA + [histone peptide H4-20]-N6-3-azidopropionyl-L-lysine
show the reaction diagram
-
-
-
?
4-pentynoyl-CoA + [histone peptide H3-20]-L-lysine
CoA + [histone peptide H3-20]-N6-4-pentynoyl-L-lysine
show the reaction diagram
-
-
-
?
4-pentynoyl-CoA + [histone peptide H4-20]-L-lysine
CoA + [histone peptide H4-20]-N6-4-pentynoyl-L-lysine
show the reaction diagram
-
-
-
?
5-hexynoyl-CoA + [histone peptide H3-20]-L-lysine
CoA + [histone peptide H3-20]-N6-5-hexynoyl-L-lysine
show the reaction diagram
very low activity with 5-hexynoyl-CoA
-
-
?
5-hexynoyl-CoA + [histone peptide H4-20]-L-lysine
CoA + [histone peptide H4-20]-N6-5-hexynoyl-L-lysine
show the reaction diagram
very low activity with 5-hexynoyl-CoA
-
-
?
6-heptynoyl-CoA + [histone peptide H3-20]-L-lysine
CoA + [histone peptide H3-20]-N6-6-heptynoyl-L-lysine
show the reaction diagram
very low activity with 6-heptynoyl-CoA
-
-
?
6-heptynoyl-CoA + [histone peptide H4-20]-L-lysine
CoA + [histone peptide H4-20]-N6-6-heptynoyl-L-lysine
show the reaction diagram
very low activity with 6-heptynoyl-CoA
-
-
?
acetyl-CoA + biotinylated histone H3 (1-21) peptide
CoA + acetylated biotinylated histone H3 (1-21) peptide
show the reaction diagram
-
-
-
?
acetyl-CoA + histone
CoA + acetylhistone
show the reaction diagram
acetyl-CoA + histone H3
CoA + acetylhistone H3
show the reaction diagram
-
-
-
?
acetyl-CoA + protein p53
CoA + acetylprotein p53
show the reaction diagram
-
-
-
?
acetyl-CoA + [histone H3]-L-lysine
CoA + [histone H3]-N6-acetyl-L-lysine
show the reaction diagram
-
-
-
?
acetyl-CoA + [histone H3]-L-lysine20
CoA + [histone H3]-N6-acetyl-L-lysine20
show the reaction diagram
-
-
-
?
acetyl-CoA + [histone H3]-L-lysine27
CoA + [histone H3]-N6-acetyl-L-lysine27
show the reaction diagram
-
-
-
?
acetyl-CoA + [histone peptide H3-20]-L-lysine
CoA + [histone peptide H3-20]-N6-acetyl-L-lysine
show the reaction diagram
-
-
-
?
acetyl-CoA + [histone peptide H4-20]-L-lysine
CoA + [histone peptide H4-20]-N6-acetyl-L-lysine
show the reaction diagram
-
-
-
?
acetyl-CoA + [protein]-L-lysine
CoA + [protein]-N6-acetyl-L-lysine
show the reaction diagram
3-azidopropionyl-CoA + [histone peptide H3-20]-L-lysine
CoA + [histone peptide H3-20]-N6-3-azidopropionyl-L-lysine
show the reaction diagram
substrate of wild-type enzyme GCN5 and enzyme mutant T612G
-
-
?
3-azidopropionyl-CoA + [histone peptide H4-20]-L-lysine
CoA + [histone peptide H4-20]-N6-3-azidopropionyl-L-lysine
show the reaction diagram
substrate of wild-type enzyme GCN5 and enzyme mutant T612G
-
-
?
4-pentynoyl-CoA + [histone peptide H3-20]-L-lysine
CoA + [histone peptide H3-20]-N6-4-pentynoyl-L-lysine
show the reaction diagram
substrate of wild-type enzyme GCN5 and enzyme mutant T612G
-
-
?
4-pentynoyl-CoA + [histone peptide H4-20]-L-lysine
CoA + [histone peptide H4-20]-N6-4-pentynoyl-L-lysine
show the reaction diagram
substrate of wild-type enzyme GCN5 and enzyme mutant T612G
-
-
?
5-hexynoyl-CoA + [histone peptide H3-20]-L-lysine
CoA + [histone peptide H3-20]-N6-5-hexynoyl-L-lysine
show the reaction diagram
substrate of wild-type enzyme GCN5 and enzyme mutant T612G
-
-
?
5-hexynoyl-CoA + [histone peptide H4-20]-L-lysine
CoA + [histone peptide H4-20]-N6-5-hexynoyl-L-lysine
show the reaction diagram
substrate of wild-type enzyme GCN5 and enzyme mutant T612G
-
-
?
6-heptynoyl-CoA + [histone peptide H3-20]-L-lysine
CoA + [histone peptide H3-20]-N6-6-heptynoyl-L-lysine
show the reaction diagram
substrate of wild-type enzyme GCN5 and enzyme mutant T612G
-
-
?
6-heptynoyl-CoA + [histone peptide H4-20]-L-lysine
CoA + [histone peptide H4-20]-N6-6-heptynoyl-L-lysine
show the reaction diagram
substrate of wild-type enzyme GCN5 and enzyme mutant T612G
-
-
?
acetyl-CoA + beta-site amyloid precursor protein-cleaving enzyme 1
CoA + acetylated beta-site amyloid precursor protein-cleaving enzyme 1
show the reaction diagram
acetyl-CoA + histone
CoA + acetylhistone
show the reaction diagram
acetyl-CoA + histone H1
CoA + acetylhistone H1
show the reaction diagram
acetyl-CoA + histone H2A
CoA + acetylhistone H2A
show the reaction diagram
acetyl-CoA + histone H2B
CoA + acetylhistone H2B
show the reaction diagram
acetyl-CoA + histone H3
CoA + acetylhistone H3
show the reaction diagram
acetyl-CoA + histone H3 N-terminal tail
CoA + acetylated histone H3 N-terminal tail
show the reaction diagram
-
50 mM Tris-HCl, pH 8.0, 30°C
-
-
?
acetyl-CoA + histone H3 peptide
CoA + acetylhistone H3 peptide
show the reaction diagram
acetyl-CoA + histone H3 peptide
CoA + actylhistone H3
show the reaction diagram
-
residues 1-21 of human histone H3
-
-
?
acetyl-CoA + histone H3-peptide
CoA + acetylhistone H3 -peptide
show the reaction diagram
-
-
-
-
?
acetyl-CoA + histone H3-peptide
CoA + acetylhistone H3-peptide
show the reaction diagram
-
-
-
-
?
acetyl-CoA + histone H3-peptide p19
CoA + acetylhistone H3 -peptide p19
show the reaction diagram
-
-
-
-
?
acetyl-CoA + histone H3-peptide p19
CoA + acetylhistone H3-peptide p19
show the reaction diagram
-
-
-
-
?
acetyl-CoA + histone H3-peptide p20
CoA + acetylhistone H3 -peptide p20
show the reaction diagram
-
-
-
-
?
acetyl-CoA + histone H3-peptide p27
CoA + acetylhistone H3 -peptide p27
show the reaction diagram
-
-
-
-
?
acetyl-CoA + histone H4
CoA + acetylhistone H4
show the reaction diagram
acetyl-CoA + histone H4
peptide CoA + acetylhistone H4 peptide
show the reaction diagram
-
specific acetylation of Lys16
-
-
?
acetyl-CoA + histone H4 peptide
CoA + acetylhistone H4 peptide
show the reaction diagram
a synthetic peptide corresponding to the first 20 amino acids of the histone H4 N-terminus
-
-
?
acetyl-CoA + histone H4 peptide
CoA + acetylpeptide of histone H4
show the reaction diagram
residues 1-20 of histone H4
-
-
?
acetyl-CoA + histone H4 peptide
CoA + actylhistone H4
show the reaction diagram
-
residues 2-24 of human histone H4
-
-
?
acetyl-CoA + N-terminal L-lysyl-[beta-catenin]
CoA + H+ + N-terminal Nalpha-acetyl-lysyl-[beta-catenin]
show the reaction diagram
-
-
-
ir
acetyl-CoA + N-terminal L-lysyl-[Hsp70]
CoA + H+ + N-terminal Nalpha-acetyl-L-lysyl-[Hsp70]
show the reaction diagram
acetyl-CoA + p50 protein
CoA + acetyl-p50 protein
show the reaction diagram
acetyl-CoA + p53
CoA + acetyl-p53
show the reaction diagram
acetyl-CoA + p65 protein
CoA + acetyl-p65 protein
show the reaction diagram
acetyl-CoA + protein p53
CoA + acetylprotein p53
show the reaction diagram
acetyl-CoA + SGRGKGGKGLGKGGAKRHRK
CoA + SGRGKGGKGLGKGGAKRHR(acK)
show the reaction diagram
-
-
-
?
acetyl-CoA + transcription factor TFIIE
CoA + acetylated transcription factor TFIIE
show the reaction diagram
-
substrate is a basal transcription factor
-
-
?
acetyl-CoA + transcription factor TFIIF
CoA + acetylated transcription factor TFIIF
show the reaction diagram
-
substrate is a basal transcription factor
-
-
?
acetyl-CoA + [alpha-tubulin]-L-lysine40
CoA + [alpha-tubulin]-N6-acetyl-L-lysine40
show the reaction diagram
acetyl-CoA + [ATM]-L-lysine
CoA + [ATM]-N6-acetyl-L-lysine
show the reaction diagram
-
-
-
?
acetyl-CoA + [AuA]-L-lysine125
CoA + [AuA]-N6-acetyl-L-lysine125
show the reaction diagram
lysine residues at positions 75 and 125 of aurora kinase A (AuA) are acetylated by ARD1, mutational analysis with AUA mutant substrates, overview
-
-
?
acetyl-CoA + [AuA]-L-lysine75
CoA + [AuA]-N6-acetyl-L-lysine75
show the reaction diagram
lysine residues at positions 75 and 125 of aurora kinase A (AuA) are acetylated by ARD1, mutational analysis with AUA mutant substrates, overview
-
-
?
acetyl-CoA + [beta-catenin]-L-lysine
CoA + [beta-catenin]-N6-acetyl-L-lysine
show the reaction diagram
-
-
-
?
acetyl-CoA + [c-myc]-L-lysine
CoA + [c-myc]-N6-acetyl-L-lysine
show the reaction diagram
-
-
-
?
acetyl-CoA + [CDC6]-L-lysine
CoA + [CDC6]-N6-acetyl-L-lysine
show the reaction diagram
-
-
-
?
acetyl-CoA + [CDC6]-L-lysine14
CoA + [CDC6]-N6-acetyl-L-lysine14
show the reaction diagram
-
-
-
?
acetyl-CoA + [connexin 43]-L-lysine
CoA + [connexin 43]-N6-acetyl-L-lysine
show the reaction diagram
-
-
-
?
acetyl-CoA + [DNMT1]-L-lysine
CoA + [DNMT1]-N6-acetyl-L-lysine
show the reaction diagram
-
-
-
?
acetyl-CoA + [E2F1]-L-lysine
CoA + [E2F1]-N6-acetyl-L-lysine
show the reaction diagram
-
-
-
?
acetyl-CoA + [Foxo1]-L-lysine
CoA + [Foxo1]-N6-acetyl-L-lysine
show the reaction diagram
-
-
-
?
acetyl-CoA + [Geminin]-L-lysine14
CoA + [Geminin]-N6-acetyl-L-lysine14
show the reaction diagram
-
-
-
?
acetyl-CoA + [histone H2A]-L-lysine5
CoA + [histone H2A]-N6-acetyl-L-lysine5
show the reaction diagram
acetyl-CoA + [histone H2B]-L-lysine
CoA + [histone H2B]-N6-acetyl-L-lysine
show the reaction diagram
-
-
-
?
acetyl-CoA + [histone H2B]-L-lysine12
CoA + [histone H2B]-N6-acetyl-L-lysine12
show the reaction diagram
-
-
-
?
acetyl-CoA + [histone H2B]-L-lysine15
CoA + [histone H2B]-N6-acetyl-L-lysine15
show the reaction diagram
-
-
-
?
acetyl-CoA + [histone H3]-L-lysine
CoA + [histone H3]-N6-acetyl-L-lysine
show the reaction diagram
acetyl-CoA + [histone H3]-L-lysine13
CoA + [histone H3]-N6-acetyl-L-lysine13
show the reaction diagram
-
-
-
-
ir
acetyl-CoA + [histone H3]-L-lysine14
CoA + [histone H3]-N6-acetyl-L-lysine14
show the reaction diagram
acetyl-CoA + [histone H3]-L-lysine18
CoA + [histone H3]-N6-acetyl-L-lysine18
show the reaction diagram
acetyl-CoA + [histone H3]-L-lysine27
CoA + [histone H3]-N6-acetyl-L-lysine27
show the reaction diagram
-
-
-
-
ir
acetyl-CoA + [histone H3]-L-lysine56
CoA + [histone H3]-N6-acetyl-L-lysine56
show the reaction diagram
-
-
-
-
ir
acetyl-CoA + [histone H3]-L-lysine79
CoA + [histone H3]-N6-acetyl-L-lysine79
show the reaction diagram
-
-
-
-
ir
acetyl-CoA + [histone H3]-L-lysine9
CoA + [histone H3]-N6-acetyl-L-lysine9
show the reaction diagram
acetyl-CoA + [histone H4]-L-lysine
CoA + [histone H4]-N6-acetyl-L-lysine
show the reaction diagram
acetyl-CoA + [histone H4]-L-lysine12
CoA + [histone H4]-N6-acetyl-L-lysine12
show the reaction diagram
acetyl-CoA + [histone H4]-L-lysine16
CoA + [histone H4]-N6-acetyl-L-lysine16
show the reaction diagram
acetyl-CoA + [histone H4]-L-lysine5
CoA + [histone H4]-N6-acetyl-L-lysine5
show the reaction diagram
acetyl-CoA + [histone H4]-L-lysine8
CoA + [histone H4]-N6-acetyl-L-lysine8
show the reaction diagram
acetyl-CoA + [histone peptide H3-20]-L-lysine
CoA + [histone peptide H3-20]-N6-acetyl-L-lysine
show the reaction diagram
substrate of wild-type enzyme GCN5 and enzyme mutant T612G
-
-
?
acetyl-CoA + [histone peptide H4-20]-L-lysine
CoA + [histone peptide H4-20]-N6-acetyl-L-lysine
show the reaction diagram
substrate of wild-type enzyme GCN5 and enzyme mutant T612G
-
-
?
acetyl-CoA + [Hsp70]-L-lysine
CoA + [Hsp70]-N6-acetyl-L-lysine
show the reaction diagram
difference in the acetylation of Hsp70 with or without rhARD1 can be observed at low ratio of enzyme: substrate up to 1:25 but not at that of higher ratio over 1:25. The enzyme targets Lys77 of Hsp70, the hARD1/NAA10-mediated catalysis of Hsp70 is abolished with K77R mutation in Hsp70
-
-
?
acetyl-CoA + [MCM2]-L-lysine14
CoA + [MCM2]-N6-acetyl-L-lysine14
show the reaction diagram
-
-
-
?
acetyl-CoA + [NFkappaB]-L-lysine
CoA + [NFkappaB]-N6-acetyl-L-lysine
show the reaction diagram
-
-
-
?
acetyl-CoA + [ORC2]-L-lysine14
CoA + [ORC2]-N6-acetyl-L-lysine14
show the reaction diagram
-
-
-
?
acetyl-CoA + [p27]-L-lysine
CoA + [p27]-N6-acetyl-L-lysine
show the reaction diagram
-
-
-
?
acetyl-CoA + [p53]-L-lysine
CoA + [p53]-N6-acetyl-L-lysine
show the reaction diagram
-
-
-
?
acetyl-CoA + [p53]-L-lysine120
CoA + [p53]-N6-acetyl-L-lysine120
show the reaction diagram
-
-
-
?
acetyl-CoA + [PGC-1alpha]-L-lysine
CoA + [PGC-1alpha]-N6-acetyl-L-lysine
show the reaction diagram
-
-
-
?
acetyl-CoA + [PGC-1]-L-lysine
CoA + [PGC-1]-N6-acetyl-L-lysine
show the reaction diagram
-
-
-
?
acetyl-CoA + [protein]-L-lysine
CoA + [protein]-N6-acetyl-L-lysine
show the reaction diagram
acetyl-CoA + [PTEN]-L-lysine
CoA + [PTEN]-N6-acetyl-L-lysine
show the reaction diagram
acetylation of the oncosuppressor protein PTEN on two lysine residues (Lys125 and Lys128)
-
-
?
acetyl-CoA + [STAT3]-L-lysine
CoA + [STAT3]-N6-acetyl-L-lysine
show the reaction diagram
-
-
-
?
acetyl-CoA + [TIP5]-L-lysine
CoA + [TIP5]-N6-acetyl-L-lysine
show the reaction diagram
-
-
-
?
acetyl-CoA + [TRRAP]-L-lysine
CoA + [TRRAP]-N6-acetyl-L-lysine
show the reaction diagram
-
-
-
?
alpha-tubulin + acetyl-CoA
acetyl-alpha-tubulin + CoA
show the reaction diagram
-
-
-
-
?
androgen receptor + acetyl-CoA
acetylated androgen receptor + CoA
show the reaction diagram
ATM kinase + acetyl-CoA
acetylated ATM kinase + CoA
show the reaction diagram
H4 peptide + acetyl-CoA
?
show the reaction diagram
-
-
-
-
?
histone + acetyl-CoA
acetyl-histone + CoA
show the reaction diagram
histone H3 + acetyl-CoA
acetyl-histone H3 + CoA
show the reaction diagram
histone H4 + acetyl-CoA
acetyl-histone H4 + CoA
show the reaction diagram
promyelotic leukemia zinc finger gene + acetyl-CoA
acetylated promyelotic leukemia zinc finger gene + CoA
show the reaction diagram
additional information
?
-
NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
acetyl-CoA + histone
CoA + acetylhistone
show the reaction diagram
-
-
-
?
acetyl-CoA + [histone H3]-L-lysine
CoA + [histone H3]-N6-acetyl-L-lysine
show the reaction diagram
-
-
-
?
acetyl-CoA + [histone H3]-L-lysine20
CoA + [histone H3]-N6-acetyl-L-lysine20
show the reaction diagram
-
-
-
?
acetyl-CoA + [protein]-L-lysine
CoA + [protein]-N6-acetyl-L-lysine
show the reaction diagram
acetyl-CoA + beta-site amyloid precursor protein-cleaving enzyme 1
CoA + acetylated beta-site amyloid precursor protein-cleaving enzyme 1
show the reaction diagram
-
-
-
-
?
acetyl-CoA + histone
CoA + acetylhistone
show the reaction diagram
acetyl-CoA + histone H2A
CoA + acetylhistone H2A
show the reaction diagram
-
acetylation at Lys5 by Tip60
-
-
?
acetyl-CoA + histone H3
CoA + acetylhistone H3
show the reaction diagram
acetyl-CoA + histone H4
CoA + acetylhistone H4
show the reaction diagram
acetyl-CoA + N-terminal L-lysyl-[beta-catenin]
CoA + H+ + N-terminal Nalpha-acetyl-lysyl-[beta-catenin]
show the reaction diagram
-
-
-
ir
acetyl-CoA + N-terminal L-lysyl-[Hsp70]
CoA + H+ + N-terminal Nalpha-acetyl-L-lysyl-[Hsp70]
show the reaction diagram
-
-
-
ir
acetyl-CoA + p50 protein
CoA + acetyl-p50 protein
show the reaction diagram
-
acetylation of p50 by p300 independent of shear stress
-
-
?
acetyl-CoA + p53
CoA + acetyl-p53
show the reaction diagram
p53 protein-acetylation of the Lys120 residue
-
-
?
acetyl-CoA + p65 protein
CoA + acetyl-p65 protein
show the reaction diagram
-
acetylation of p65 by p300 during translocation into the nuclei in response to shear stress
-
-
?
acetyl-CoA + [alpha-tubulin]-L-lysine40
CoA + [alpha-tubulin]-N6-acetyl-L-lysine40
show the reaction diagram
-
-
-
?
acetyl-CoA + [ATM]-L-lysine
CoA + [ATM]-N6-acetyl-L-lysine
show the reaction diagram
-
-
-
?
acetyl-CoA + [AuA]-L-lysine125
CoA + [AuA]-N6-acetyl-L-lysine125
show the reaction diagram
lysine residues at positions 75 and 125 of aurora kinase A (AuA) are acetylated by ARD1, mutational analysis with AUA mutant substrates, overview
-
-
?
acetyl-CoA + [AuA]-L-lysine75
CoA + [AuA]-N6-acetyl-L-lysine75
show the reaction diagram
lysine residues at positions 75 and 125 of aurora kinase A (AuA) are acetylated by ARD1, mutational analysis with AUA mutant substrates, overview
-
-
?
acetyl-CoA + [beta-catenin]-L-lysine
CoA + [beta-catenin]-N6-acetyl-L-lysine
show the reaction diagram
-
-
-
?
acetyl-CoA + [c-myc]-L-lysine
CoA + [c-myc]-N6-acetyl-L-lysine
show the reaction diagram
-
-
-
?
acetyl-CoA + [CDC6]-L-lysine
CoA + [CDC6]-N6-acetyl-L-lysine
show the reaction diagram
-
-
-
?
acetyl-CoA + [connexin 43]-L-lysine
CoA + [connexin 43]-N6-acetyl-L-lysine
show the reaction diagram
-
-
-
?
acetyl-CoA + [DNMT1]-L-lysine
CoA + [DNMT1]-N6-acetyl-L-lysine
show the reaction diagram
-
-
-
?
acetyl-CoA + [E2F1]-L-lysine
CoA + [E2F1]-N6-acetyl-L-lysine
show the reaction diagram
-
-
-
?
acetyl-CoA + [Foxo1]-L-lysine
CoA + [Foxo1]-N6-acetyl-L-lysine
show the reaction diagram
-
-
-
?
acetyl-CoA + [histone H2A]-L-lysine5
CoA + [histone H2A]-N6-acetyl-L-lysine5
show the reaction diagram
-
-
-
?
acetyl-CoA + [histone H2B]-L-lysine
CoA + [histone H2B]-N6-acetyl-L-lysine
show the reaction diagram
-
-
-
?
acetyl-CoA + [histone H2B]-L-lysine12
CoA + [histone H2B]-N6-acetyl-L-lysine12
show the reaction diagram
-
-
-
?
acetyl-CoA + [histone H2B]-L-lysine15
CoA + [histone H2B]-N6-acetyl-L-lysine15
show the reaction diagram
-
-
-
?
acetyl-CoA + [histone H3]-L-lysine
CoA + [histone H3]-N6-acetyl-L-lysine
show the reaction diagram
acetyl-CoA + [histone H3]-L-lysine14
CoA + [histone H3]-N6-acetyl-L-lysine14
show the reaction diagram
acetyl-CoA + [histone H3]-L-lysine18
CoA + [histone H3]-N6-acetyl-L-lysine18
show the reaction diagram
-
-
-
?
acetyl-CoA + [histone H3]-L-lysine9
CoA + [histone H3]-N6-acetyl-L-lysine9
show the reaction diagram
-
-
-
?
acetyl-CoA + [histone H4]-L-lysine
CoA + [histone H4]-N6-acetyl-L-lysine
show the reaction diagram
acetyl-CoA + [histone H4]-L-lysine12
CoA + [histone H4]-N6-acetyl-L-lysine12
show the reaction diagram
acetyl-CoA + [histone H4]-L-lysine16
CoA + [histone H4]-N6-acetyl-L-lysine16
show the reaction diagram
acetyl-CoA + [histone H4]-L-lysine5
CoA + [histone H4]-N6-acetyl-L-lysine5
show the reaction diagram
acetyl-CoA + [histone H4]-L-lysine8
CoA + [histone H4]-N6-acetyl-L-lysine8
show the reaction diagram
-
-
-
?
acetyl-CoA + [NFkappaB]-L-lysine
CoA + [NFkappaB]-N6-acetyl-L-lysine
show the reaction diagram
-
-
-
?
acetyl-CoA + [p27]-L-lysine
CoA + [p27]-N6-acetyl-L-lysine
show the reaction diagram
-
-
-
?
acetyl-CoA + [p53]-L-lysine
CoA + [p53]-N6-acetyl-L-lysine
show the reaction diagram
-
-
-
?
acetyl-CoA + [p53]-L-lysine120
CoA + [p53]-N6-acetyl-L-lysine120
show the reaction diagram
-
-
-
?
acetyl-CoA + [PGC-1alpha]-L-lysine
CoA + [PGC-1alpha]-N6-acetyl-L-lysine
show the reaction diagram
-
-
-
?
acetyl-CoA + [PGC-1]-L-lysine
CoA + [PGC-1]-N6-acetyl-L-lysine
show the reaction diagram
-
-
-
?
acetyl-CoA + [protein]-L-lysine
CoA + [protein]-N6-acetyl-L-lysine
show the reaction diagram
acetyl-CoA + [PTEN]-L-lysine
CoA + [PTEN]-N6-acetyl-L-lysine
show the reaction diagram
acetylation of the oncosuppressor protein PTEN on two lysine residues (Lys125 and Lys128)
-
-
?
acetyl-CoA + [STAT3]-L-lysine
CoA + [STAT3]-N6-acetyl-L-lysine
show the reaction diagram
-
-
-
?
acetyl-CoA + [TIP5]-L-lysine
CoA + [TIP5]-N6-acetyl-L-lysine
show the reaction diagram
-
-
-
?
acetyl-CoA + [TRRAP]-L-lysine
CoA + [TRRAP]-N6-acetyl-L-lysine
show the reaction diagram
-
-
-
?
androgen receptor + acetyl-CoA
acetylated androgen receptor + CoA
show the reaction diagram
-
receptor signaling in prostate cancer cells is augmented by the androgen receptor coactivator p300, which transactivates and acetylates the androgen receptor in the presence of 100 nM dihydrotestosterone, involvement of p300 in neuropeptide activation of androgen receptor signaling, overview
-
-
?
ATM kinase + acetyl-CoA
acetylated ATM kinase + CoA
show the reaction diagram
-
ATM protein kinase regulates the cell’s response to DNA damage through the phosphorylation of proteins involved in cell-cycle checkpoints and DNA repair, suppression of Tip60 blocks the activation of ATM’s kinase activity, ATM autophosphorylation e.g. at Ser1981, and prevents the ATM-dependent phosphorylation of p53 and chk2, inactivation of Tip60 sensitizes cells to ionizing radiation, overview
-
-
?
histone + acetyl-CoA
acetyl-histone + CoA
show the reaction diagram
histone H3 + acetyl-CoA
acetyl-histone H3 + CoA
show the reaction diagram
histone H4 + acetyl-CoA
acetyl-histone H4 + CoA
show the reaction diagram
-
-
-
-
?
promyelotic leukemia zinc finger gene + acetyl-CoA
acetylated promyelotic leukemia zinc finger gene + CoA
show the reaction diagram
-
-
-
-
?
additional information
?
-
COFACTOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
3-azidopropionyl-CoA
-
4-pentynoyl-CoA
-
5-hexynoyl-CoA
a poor surrogate for acetyl-CoA with p300
6-heptynoyl-CoA
a poor surrogate for acetyl-CoA with p300
acetyl-CoA
3-azidopropionyl-CoA
-
4-pentynoyl-CoA
-
5-hexynoyl-CoA
-
6-heptynoyl-CoA
-
acetyl-CoA
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(2E,6E)-2,6-bis[(3,4-dihydroxyphenyl)methylidene]cyclohexan-1-one
89% residual activity at 0.1 mM
(2E,6E)-2,6-bis[(3,5-dibromo-4-hydroxyphenyl)methylidene]cyclohexan-1-one
complete inhibition at 0.1 mM
(2E,6E)-2,6-bis[(3-fluoro-4-hydroxyphenyl)methylidene]cyclohexan-1-one
6.3% residual activity at 0.1 mM
(2E,6E)-2,6-bis[(4-hydroxy-3-methylphenyl)methylidene]cyclohexan-1-one
3.0% residual activity at 0.1 mM
(2E,6E)-2,6-bis[(4-hydroxyphenyl)methylidene]cyclohexan-1-one
28.6% residual activity at 0.1 mM
(3E,5E)-1-benzyl-3,5-bis[(3,4-dihydroxyphenyl)methylidene]piperidin-4-one
19.4% residual activity at 0.1 mM
(3E,5E)-3,5-bis[(3,4-dihydroxyphenyl)methylidene]-1-methylpiperidin-4-one
82.4% residual activity at 0.1 mM
(3Z,5Z)-3,5-bis[(3-bromo-4-hydroxyphenyl)methylidene]thian-4-one
7.13% residual activity at 0.1 mM
(4-(4-((5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl)methylene)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl) phenyl)phosphonic acid
-
(4-(4-((5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl)methylene)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)phenyl)phosphonic acid
-
(4E)-2-(4-acetylphenyl)-4-[[5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl]methylidene]-5-methyl-2,4-dihydro-3H-pyrazol-3-one
-
(5E)-1-(3-chloro-4-methylphenyl)-5-[(2E)-3-(furan-2-yl)prop-2-en-1-ylidene]-2-sulfanylidenedihydropyrimidine-4,6(1H,5H)-dione
-
1-benzyl-3,5-bis[(E)-3-bromo-4-hydroxybenzylidene]piperidin-4-one
81.6% residual activity at 0.1 mM
2,5-bis[(E)-3-bromo-4-hydroxybenzylidene]cyclopentan-1-one
41.2% residual activity at 0.1 mM
2,6-bis(3,4-dibromobenzylidene)cyclohexan-1-one
85.1% residual activity at 0.1 mM
2,6-bis(3-bromo-4-hydroxybenzylidene)cyclohexanone
RC56, specific inhibitor, complete inhibition at 0.1 mM
2,6-bis(3-chloro-4-hydroxybenzylidene)cyclohexan-1-one
7.7% residual activity at 0.1 mM
2,6-bis(3-chloro-5-fluoro-4-hydroxybenzylidene)cyclohexan-1-one
41.1% residual activity at 0.1 mM
2,6-bis(4-hydroxy-3-iodobenzylidene)cyclohexan-1-one
5.8% residual activity at 0.1 mM
2,6-bis[(6-hydroxy-1,1'-biphenyl-3-yl)methylene]cyclohexan-1-one
92.2% residual activity at 0.1 mM
2-(3,5-difluoro-4-hydroxyphenyl)-4-((5-(4,5-dimethyl-2-(trifluoromethyl)phenyl)furan-2-yl)methylene)-5-methyl-2,4-dihydro-3H-pyrazol-3-one
-
2-(3,5-difluoro-4-hydroxyphenyl)-4-((5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl)methylene)-5-methyl-2,4-dihydro-3H-pyrazol-3-one
-
2-(3,5-difluoro-4-hydroxyphenyl)-5-methyl-4-((5-(2-(trifluoromethoxy)phenyl)furan-2-yl)methylene)-2,4-dihydro-3H-pyrazol-3-one
-
2-(3,5-difluoro-4-hydroxyphenyl)-5-methyl-4-((5-(3-oxo-2,3-dihydro-1H-inden-4-yl)furan-2-yl)methylene)-2,4-dihydro-3H-pyrazol-3-one
-
2-(4-(2H-tetrazol-5-yl) phenyl)-4-((5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl)methylene)-5-methyl-2,4-dihydro-3H-pyrazol-3-one
-
2-(4-(2H-tetrazol-5-yl)phenyl)-4-((5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl)methylene)-5-methyl-2,4-dihydro-3H-pyrazol-3-one
-
2-(4-bromophenyl)-5-nitro[1,2]thiazolo[5,4-b]pyridin-3(2H)-one
-
2-(heptylsulfanyl)-1-(2-hydroxyphenyl)ethan-1-one
-
2-butyl-6-hydroxybenzoic acid
-
2-decyl-6-hydroxybenzoic acid
88% inhibition at 0.05 mM
2-hydroxy-5-pentadecylbenzoic acid
85% inhibition at 0.05 mM
2-hydroxy-5-pentylbenzoic acid
-
2-hydroxy-6-(11-hydroxyundecyl)benzoic acid
-
2-hydroxy-6-(5-hydroxypentyl)benzoic acid
-
2-hydroxy-6-pentadecylbenzoic acid
i.e. anacardic acid, 97% inhibition at 0.05 mM
4,4'-(2-hydroxycyclohexane-1,3-diylidene)bis(methanylylidene)-bis(2-bromophenol)
12.5% residual activity at 0.1 mM
4-((5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl)methylene)-5-methyl-2-(4- (methylsulfonyl) phenyl)-2,4-dihydro-3H-pyrazol-3-one
-
4-((5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl)methylene)-5-methyl-2-(4-(methylsulfonyl)phenyl)-2,4-dihydro-3H-pyrazol-3-one
-
4-(3-cyclopropyl-4-((5-(4,5-dimethyl-2-(trifluoromethyl)phenyl)thiophen- 2-yl)methylene)-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
-
4-(3-cyclopropyl-4-((5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl)methylene)-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
-
4-(3-methyl-4-((5-(2-nitrophenyl)furan-2-yl)methylene)-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
-
4-(3-methyl-5-oxo-4-((5-(2-(trifluoromethoxy)phenyl)furan-2-yl)methylene)-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
-
4-(3-methyl-5-oxo-4-((5-(3-oxo-2,3-dihydro-1H-inden-4-yl)furan-2-yl)methylene)-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
-
4-(4-((2-(4,5-dimethyl-2-nitrophenyl)thiazol-5-yl)methylene)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
-
4-(4-((5-(2-(difluoromethyl)phenyl)furan-2-yl)methylene)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
-
4-(4-((5-(2-(dimethylphosphoryl)phenyl)furan-2-yl)methylene)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
-
4-(4-((5-(4,5-dimethyl-2-(trifluoromethyl)phenyl)furan-2-yl)methylene)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
-
4-(4-((5-(4,5-dimethyl-2-nitrophenyl)-1H-pyrrol-2-yl)methylene)-3-methyl-5-oxo-4, 5-dihydro-1H-pyrazol-1-yl)benzoic acid
-
4-(4-((5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl)methylene)-2,5-dioxoimidazolidin-1-yl)benzoic acid
-
4-(4-((5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl)methylene)-3-ethyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
-
4-(4-((5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl)methylene)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
C646, selective inhibitor
4-(4-((5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl)methylene)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzonitrile
-
4-(4-((5-(4,5-dimethyl-2-nitrophenyl)thiophen-2-yl)methylene)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
-
4-(4-(1-(5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl)ethylidene)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
-
4-(4-(2-((4,5-dimethyl-2-nitrophenyl)amino)-2-oxoethyl)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
-
4-(4-(3-((4,5-dimethyl-2-nitrophenyl)amino)-3-oxopropyl)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
-
4-(4-chlorophenyl)-2-(2-cyclopentylidenehydrazinyl)-1,3-thiazole
-
4-(5-((5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl)methylene)-2,4- dioxothiazolidin-3-yl)benzoic acid
-
4-(5-(4,5-dimethyl-2-nitrobenzoyl)-1H-indazol-1-yl)benzoic acid
-
4-(5-(4,5-dimethyl-2-nitrobenzoyl)-1H-indol-1-yl)benzoic acid
-
4-(5-(4,5-dimethyl-2-nitrobenzyl)-1H-indazol-1-yl)benzoic acid
-
4-([(2E)-2-cyano-3-[5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl]prop-2-enoyl]amino)benzoic acid
-
4-acetyl-2-methyl-N-(morpholin-4-yl)-3,4-dihydro-2H-1,4-benzothiazine-7-sulfonamide
-
4-hydroxy-2-pentylquinoline-3-carboxylic acid
-
4-[(4Z)-4-[[5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl]methylidene]-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl]-N-(prop-2-yn-1-yl)benzamide
i.e. C646-yne, docking study and protein interaction analysis, formation of a stable C646-cysteine adducts. The major targets of C646-yne reactivity are abundant cellular proteins containing reactive cysteine residues
4-[(4Z)-4-[[5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl]methylidene]-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl]benzoic acid
i.e. C646, inhibits the lysine acetyltransferases (KATs) p300 and CBP and represents a very potent and selective small molecule KAT inhibitor, docking study and protein interaction analysis. The pyrazolone-furan of C646 is an electrophilic chemotype capable of irreversible protein reactivity
5,5'-[(5-carboxy-2-oxocyclohexane-1,3-diylidene)bis(methanylylidene)]bis(2-hydroxybenzoic acid)
70.1% residual activity at 0.1 mM
5-decyl-2-hydroxybenzoic acid
95% inhibition at 0.05 mM
anacardic acid
-
epigallocatechin-3-gallate
-
N-[(4-fluorophenyl)methyl]-2-[(1R)-5-[(methylcarbamoyl)amino]-2',4'-dioxo-2,3-dihydrospiro[indene-1,5'-[1,3]oxazolidin]-3'-yl]-N-[(2S)-1,1,1-trifluoropropan-2-yl]acetamide
-
NSC694616
-
Plumbagin
-
(1E,4Z,6E)-1,7-bis(3-bromo-4-hydroxyphenyl)-5-hydroxyhepta-1,4,6-trien-3-one
-
cinnamoyl-II
(1E,4Z,6E)-5-hydroxy-1,7-bis(4-hydroxyphenyl)hepta-1,4,6-trien-3-one
-
BDMC
(1E,4Z,6E)-5-hydroxy-1-(4-hydroxy-3-methoxyphenyl)-7-(4-hydroxyphenyl)hepta-1,4,6-trien-3-one
-
DMC
(2-ethoxypropoxy)benzene
-
-
(2E)-2-(ethoxycarbonyl)heptadec-2-enoic acid
-
(2E)-2-(ethoxycarbonyl)hexadec-2-enoic acid
-
(2E)-2-acetylhexadec-2-enoic acid
-
-
(2E)-2-acetylpentadec-2-enoic acid
-
-
(2E,6E)-2,6-bis[(3,5-dibromo-4-hydroxyphenyl)methylidene]cyclohexan-1-one
-
-
(2E,6E)-2,6-bis[(3-bromophenyl)methylidene]cyclohexan-1-one
-
-
(2E,6E)-2,6-bis[(4-hydroxy-3,5-dimethylphenyl)methylidene]cyclohexan-1-one
-
-
(2E,6E)-2,6-bis[(4-hydroxy-3-iodophenyl)methylidene]cyclohexan-1-one
-
-
(2E,6E)-2,6-bis[(4-hydroxyphenyl)methylidene]cyclohexan-1-one
-
-
(2E,6E)-2,6-bis[(pyridin-3-yl)methylidene]cyclohexan-1-one
-
-
(2R,3S)-4-methylidene-5-oxo-2-propyltetrahydrofuran-3-carboxylic acid
-
i.e. butyrolactone MB-3, a GCN5 inhibitor
(3-oxo-1,2-benzothiazol-2(3H)-yl)(phenyl)acetic acid
-
-
(3E,5E)-3,5-bis[(3-bromo-4-hydroxyphenyl)methylidene]-4-oxopiperidin-1-ium
-
-
(E)-4-(2-(5,6-dimethylbenzo[d]thiazol-2-yl)vinyl)-N,N-diethylbenzenesulfonamide
(E)-4-(2-(5-bromobenzo[d]thiazol-2-yl)vinyl)-N,N-diethylbenzenesulfonamide
(E)-4-(2-(5-chlorobenzo[d]thiazol-2-yl)vinyl)-N,N-diethylbenzenesulfonamide
(E)-4-(2-(6-bromobenzo[d]thiazol-2-yl)vinyl)-N,N-diethylbenzenesulfonamide
(E)-4-(2-(benzo[d]thiazol-2-yl)vinyl)-2-chloro-N,N-diethylbenzenesulfonamide
(E)-4-(2-(benzo[d]thiazol-2-yl)vinyl)-N,N-diethyl-2-fluorobenzenesulfonamide
(E)-4-(2-(benzo[d]thiazol-2-yl)vinyl)-N,N-diethyl-2-methylbenzenesulfonamide
(E)-4-(2-(benzo[d]thiazol-2-yl)vinyl)-N,N-diethylbenzenesulfonamide
(E)-4-(2-(benzo[d]thiazol-2-yl)vinyl)-N,N-dimethylbenzenesulfonamide
(E)-4-(2-(benzo[d]thiazol-2-yl)vinyl)-N-(4-methoxyphenyl)benzenesulfonamide
(E)-4-(2-(benzo[d]thiazol-2-yl)vinyl)-N-(4-methylbenzyl)benzenesulfonamide
(E)-4-(2-(benzo[d]thiazol-2-yl)vinyl)-N-benzylbenzenesulfonamide
(E)-4-(2-(benzo[d]thiazol-2-yl)vinyl)-N-phenylbenzenesulfonamide
(E)-N,N-diethyl-4-(2-(5-fluorobenzo[d]thiazol-2-yl)vinyl)benzenesulfonamide
(E)-N,N-diethyl-4-(2-(5-methoxybenzo[d]thiazol-2-yl)vinyl)benzenesulfonamide
(E)-N,N-diethyl-4-(2-(5-methylbenzo[d]thiazol-2-yl)vinyl)benzenesulfonamide
1,1'-(1,4-phenylene)bis[3-(butylsulfanyl)pyrrolidine-2,5-dione]
-
-
1,3-dibenzyl-5-[(4-hydroxy-2,6-dimethylphenyl)methylidene]-1,3-diazinane-2,4,6-trione
-
-
1,3-dibenzyl-5-[(4-hydroxyphenyl)methylidene]-1,3-diazinane-2,4,6-trione
-
-
1,7-bis(3-bromo-4-hydroxyphenyl)-1,6-heptadiene-3,5-dione
-
-
1-(2-pentylphenyl)ethan-1-ol
-
-
1-(2-pentylphenyl)ethan-1-one
-
-
1-(4-(3-nitrophenyl)thiazol-2-yl)-2-(propan-2-ylidene)hydrazine
-
1-(4-(4-chlorophenyl)thiazol-2-yl)-2-(propan-2-ylidene)hydrazine
-
i.e. BF1, shows substrate selectivity for histone H3 acetylation and inhibitory activity in vitro on recombinant HATs Gcn5 and p300. Both global acetylation of histone H3 and specific acetylation at lysine 18 (H3AcK18) are lowered by BF1 treatment
10-(benzyloxy)-2,3,11-trimethoxy-6,7-dihydro-5H-isoquinolino[3,2-a][2]benzazepin-8-ium chloride
-
-
13,14 disulfoxyisogarcinol
-
LTK-19
14-isopropoxyisogarcinol
-
LTK-13
14-methoxyisogarcinol
-
LTK-14
2,2-dimethyl-5-tetradecyl-1,3-dioxane-4,6-dione
-
-
2,2-dimethyl-5-tetradecylidene-1,3-dioxane-4,6-dione
-
-
2,3,11,12-tetramethoxy-6,7-dihydro-5H-isoquinolino[3,2-a][2]benzazepin-8-ium methanesulfonate
-
-
2,3,11-trimethoxy-10-[(4-nitrophenyl)methoxy]-6,7-dihydro-5H-isoquinolino[3,2-a][2]benzazepin-8-ium bromide
-
-
2,3-difluoro-N'-(2-fluorobenzene-1-sulfonyl)-5-(pyridin-2-yl)benzohydrazide
-
WM-1119
2,3-difluoro-N'-(3-methyl-5-(1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
-
2,4-difluoro-N'-(3-methyl-5-(1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
-
2,5-diphenylisothiazol-3(2H)-one
-
-
2,6-bis(3-bromo-4-hydroxybenzylidene)cyclohexanone
2,6-difluoro-N'-(3-methyl-5-(1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
-
2-(1,3-benzothiazol-2-yl)-1,2-benzothiazol-3(2H)-one
-
-
2-(2-cyclopentylidenehydrazinyl)-4-(3-methoxyphenyl)-1,3-thiazole
-
2-(2-cyclopentylidenehydrazinyl)-4-(3-nitrophenyl)-1,3-thiazole
-
2-(2-cyclopentylidenehydrazinyl)-4-(4-fluorophenyl)-1,3-thiazole
2-(2-cyclopentylidenehydrazinyl)-4-(4-methoxyphenyl)-1,3-thiazole
-
2-(2-cyclopentylidenehydrazinyl)-4-phenyl-1,3-thiazole
-
2-(2-pyridyl)-isothiazol-3(2H)-one
-
-
2-(2-[[(1S)-3-(5-[[5-(3-carbamimidamidopropyl)-3,6-dioxopiperazin-2-yl]methyl]-2-hydroxyphenoxy)-1-carboxypropyl]amino]-2-oxoethyl)-2-hydroxybutanedioic acid
-
NK13650B
2-(3-chloro-4-fluorophenyl)isothiazol-3(2H)-one
-
2-(3-fluoro-5-(2-((2-fluorophenyl)sulfonyl)hydrazinecarbonyl)-phenyl)pyridine 1-Oxide
-
2-(3-methoxyphenyl)isothiazolo[5,4-b]pyridin-3(2H)-one
-
antiproliferative effects in cancer cells, GI50 value 0.007 mM with SK-N-SH cell
2-(3-oxo-1,2-benzothiazol-2(3H)-yl)-N-(1,3-thiazol-2-yl)acetamide
-
-
2-(3-pyridyl)-isothiazol-3(2H)-one
-
-
2-(4,6-dimethyl-3-oxo[1,2]thiazolo[5,4-b]pyridin-2(3H)-yl)ethyl ethylcarbamate
-
-
2-(4-(trifluoromethyl)benzyl)isothiazolo[5,4-b]pyridin-3(2H)-one
-
antiproliferative effects in cancer cells, GI50 value 0.0005 mM with SK-N-SH cell, 0.030 mM with MCF-7 cell
2-(4-dimethylaminoaniline)-isothiazol-3(2H)-one
-
-
2-(4-fluorophenyl)isothiazolo[5,4-b]pyridin-3(2H)-one
-
antiproliferative effects in cancer cells, GI50 value 0.010 mM with SK-N-SH cell, 0.037 mM with MCF-7 cell
2-(4-fluorophenyl)[1,2]thiazolo[5,4-b]pyridin-3(2H)-one
-
PU139
2-(4-methylphenyl)isothiazolo[5,4-b]pyridin-3(2H)-one
-
antiproliferative effects in cancer cells, GI50 value 0.006 mM with SK-N-SH cell
2-(4-morpholinoaniline)-isothiazol-3(2H)-one
-
-
2-(4-pyridyl)-isothiazol-3(2H)-one
-
-
2-(4-[2-[3-(4-chlorophenyl)-5-(3,4-dimethoxyphenyl)-4,5-dihydro-1H-pyrazol-1-yl]-1,3-thiazol-4-yl]phenyl)-1H-isoindole-1,3(2H)-dione
-
-
2-(4-[2-[5-(3,4-dimethoxyphenyl)-3-(thiophen-2-yl)-4,5-dihydro-1H-pyrazol-1-yl]-1,3-thiazol-4-yl]phenyl)-1H-isoindole-1,3(2H)-dione
-
-
2-(4-[2-[5-(furan-2-yl)-3-(4-methoxyphenyl)-4,5-dihydro-1H-pyrazol-1-yl]-1,3-thiazol-4-yl]phenyl)-1H-isoindole-1,3(2H)-dione
-
-
2-(6,7-dihydroxynaphthyl) beta-D-xylopyranoside
-
less than 50% residual activity at 0.1 mM
2-(6,7-dimethoxynaphthyl) beta-D-xylopyranoside
-
about 80% residual activity at 0.1 mM
2-(6-fluoro-3-oxo-1,2-benzothiazol-2(3H)-yl)-N-(4-phenyl-1,3-thiazol-2-yl)acetamide
-
-
2-(6-hydroxy-7-methoxy-naphthyl) beta-D-xylopyranoside
-
less than 50% residual activity at 0.1 mM
2-(7-hydroxy-6-methoxy-naphthyl) beta-D-xylopyranoside
-
about 55% residual activity at 0.1 mM
2-(dimethylamino)-6-pentadecylpyrimidin-4(3H)-one
-
-
2-(dimethylamino)-6-tetradecylpyrimidin-4(3H)-one
-
-
2-(dimethylamino)-6-tridecylpyrimidin-4(3H)-one
-
-
2-(heptylsulfanyl)-1-(2-hydroxyphenyl)ethan-1-one
-
2-(hexylsulfanyl)-1-(2-hydroxyphenyl)ethan-1-one
-
-
2-(methylsulfanyl)-6-tridecylpyrimidin-4(3H)-one
-
-
2-(phenyl)-isothiazolo[5,4-b]pyridin-3(2H)-one
-
-
2-butyl-6-hydroxybenzoic acid
2-chloro-4-[5-[(E)-[3-[2-(4-methylanilino)-2-oxoethyl]-2,4-dioxo-1,3-thiazolidin-5-ylidene]methyl]furan-2-yl]benzoic acid
-
C375
2-decyl-4-hydroxyquinoline-3-carboxylic acid
-
-
2-decyl-6-hydroxybenzoic acid
-
2-dodecylmalonate
-
compound induces hyperacetylation of specific lysine residues of histone H3, in particular residues K9 and K18, and raises the level of pan-acetylated H4. Compound inhibits the acetylation of all the other H3 and H4 lysines, with the exception of residue K8Ac of histone H4
2-ethylisothiazol-3(2H)-one
-
2-fluoro-3-hydroxy-N'-(3-methyl-5-(1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
-
2-fluoro-3-methyl-N'-(3-methyl-5-(1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
-
2-fluoro-4-methyl-N'-(3-methyl-5-(1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
-
2-fluoro-5-hydroxy-N'-(3-methyl-5-(1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
-
2-fluoro-5-methoxy-N'-(3-methyl-5-(1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
-
2-fluoro-5-methyl-N'-(3-methyl-5-(1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
-
2-fluoro-6-methoxy-N'-(3-methyl-5-(1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
-
2-fluoro-N'-(2-fluoro-5-methyl-3-(1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
-
2-fluoro-N'-(2-fluoro-5-methyl-3-(pyridin-2-yl)benzoyl)benzenesulfonohydrazide
-
2-fluoro-N'-(2-phenylisonicotinoyl)benzenesulfonohydrazide
-
2-fluoro-N'-(3-(3-methyl-1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
-
2-fluoro-N'-(3-(4-fluoro-1H-pyrazol-1-yl)-5-methylbenzoyl)benzenesulfonohydrazide
-
2-fluoro-N'-(3-(4-fluoro-1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
-
2-fluoro-N'-(3-(4-methyl-1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
-
2-fluoro-N'-(3-(furan-2-yl)benzoyl)benzenesulfonohydrazide
-
2-fluoro-N'-(3-(pyridin-2-yl)benzoyl)benzenesulfonohydrazide
-
2-fluoro-N'-(3-(thiophen-2-yl)benzoyl)benzenesulfonohydrazide
-
2-fluoro-N'-(3-(thiophen-3-yl)benzoyl)benzenesulfonohydrazide
-
2-fluoro-N'-(3-fluoro-5-(1H-pyrazol-1-yl)benzoyl)-3-methoxybenzenesulfonohydrazide
-
2-fluoro-N'-(3-fluoro-5-(1H-pyrazol-1-yl)benzoyl)-4-methoxybenzenesulfonohydrazide
-
2-fluoro-N'-(3-fluoro-5-(1H-pyrazol-1-yl)benzoyl)-5-hydroxybenzenesulfonohydrazide
-
2-fluoro-N'-(3-fluoro-5-(1H-pyrazol-1-yl)benzoyl)-5-methoxybenzenesulfonohydrazide
-
2-fluoro-N'-(3-fluoro-5-(2H-1,2,3-triazol-2-yl)benzoyl)benzenesulfonohydrazide
-
2-fluoro-N'-(3-fluoro-5-(3-methyl-1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
-
2-fluoro-N'-(3-fluoro-5-(4-methyl-1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
-
2-fluoro-N'-(3-fluoro-5-(5-methyl-1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
-
2-fluoro-N'-(3-fluoro-5-(pyridin-2-yl)benzoyl)-3-hydroxybenzenesulfonohydrazide
-
2-fluoro-N'-(3-fluoro-5-(pyridin-2-yl)benzoyl)benzenesulfonohydrazide
competes with Ac-CoA by binding to the Ac-CoA binding site
2-fluoro-N'-(3-iodobenzoyl)benzenesulfonohydrazide
-
2-fluoro-N'-(3-isobutoxybenzoyl)benzenesulfonohydrazide
-
2-fluoro-N'-(3-isopropoxybenzoyl)benzenesulfonohydrazide
-
2-fluoro-N'-(3-isopropylbenzoyl)benzenesulfonohydrazide
-
2-fluoro-N'-(3-methoxy-5-(1H-pyrazol-1-yl)benzoyl)-benzenesulfonohydrazide
-
2-fluoro-N'-(3-methoxy-5-(1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
-
2-fluoro-N'-(3-methoxy-5-(3-methyl-1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
-
2-fluoro-N'-(3-methoxy-5-(pyrimidin-2-yl)benzoyl)-benzenesulfonohydrazide
-
2-fluoro-N'-(3-methyl-5-(1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
-
2-fluoro-N'-(3-methyl-5-(2H-1,2,3-triazol-2-yl)benzoyl)benzenesulfonohydrazide
-
2-fluoro-N'-(3-methyl-5-(3-methyl-1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
-
2-fluoro-N'-(3-methyl-5-(4-methyl-1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
-
2-fluoro-N'-(3-methyl-5-(5-methyl-1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
-
2-fluoro-N'-(3-methylbenzoyl)benzenesulfonohydrazide
-
2-fluoro-N'-(3-propoxybenzoyl)benzenesulfonohydrazide
-
2-fluoro-N'-(3-propylbenzoyl)benzenesulfonohydrazide
-
2-fluoro-N'-(4-fluoro-5-methyl-[1,1'-biphenyl]-3-carbonyl)benzenesulfonohydrazide
-
2-fluoro-N'-(5-fluoro-[1,1'-biphenyl]-3-carbonyl)-3-hydroxybenzenesulfonohydrazide
-
2-fluoro-N'-(5-fluoro-[1,1'-biphenyl]-3-carbonyl)-4-hydroxybenzenesulfonohydrazide
-
2-fluoro-N'-(5-fluoro-[1,1'-biphenyl]-3-carbonyl)-4-methoxybenzenesulfonohydrazide
-
2-fluoro-N'-(5-phenylnicotinoyl)benzenesulfonohydrazide
-
2-fluoro-N'-(6-phenylpicolinoyl)benzenesulfonohydrazide
-
2-fluoro-N'-(naphthalene-2-sulfonyl)benzohydrazide
2-hydroxy-5-nonylbenzoic acid
-
-
2-hydroxy-5-pentadecylbenzoic acid
-
2-hydroxy-5-tetradecylbenzoic acid
-
-
2-hydroxy-6-(11-hydroxyundecyl)benzoic acid
2-hydroxy-6-nonylbenzoic acid
-
-
2-hydroxy-6-pentadecylbenzoic acid
-
2-hydroxy-6-tetradecylbenzoic acid
-
-
2-hydroxy-6-[(Z)-2-[4-(pentyloxy)phenyl]ethenyl]benzoic acid
-
-
2-pentylisothiazol-3(2H)-one
-
2-phenyl-5-(trityloxymethyl)isothiazol-3(2H)-one
-
-
2-phenylisothiazol-3(2H)-one
-
-
2-sulfanylidene-6-tridecyl-2,3-dihydropyrimidin-4(1H)-one
-
-
2-tert-butyl-5-(dodecylthio)isothiazol-3(2H)-one-1-oxide
-
-
2-tert-butyl-5-chloroisothiazol-3(2H)-one 1-oxide
-
-
2-tridecylmalonate
-
inhibition of the acetylation of histone H3 residuesK9/K18, being practically inactive in all the other assays
2-undecylmalonate
-
compound exhibits a significant inhibition of the acetylation of almost any lysine residue explored, with the sole exception of residue K8 of H4. Compound reduces the level of K5Ac of H4 and, more markedly, K16Ac of H4
2-[(1E)-1-[2-[4-(4-chlorophenyl)-1,3-thiazol-2-yl]hydrazinylidene]ethyl]pyridine
-
2-[(1Z)-1-[(3E)-3-[2-[4-(4-chlorophenyl)-1,3-thiazol-2-yl]hydrazinylidene]cyclopentylidene]ethyl]pyridine
-
-
2-[(3,4-dichlorophenyl)methyl]-1H-1l4-[1,2]thiazolo[5,4-b]pyridine-1,3(2H)-dione
-
-
2-[(3,4-dichlorophenyl)methyl]-1H-1l6-[1,2]thiazolo[5,4-b]pyridine-1,1,3(2H)-trione
-
-
2-[(4-bromophenyl)methyl]-5-methyl[1,2]thiazolo[5,4-b]pyridin-3(2H)-one
-
NSC694614
2-[(4-methoxyphenyl)methyl]-5-nitro[1,2]thiazolo[5,4-b]pyridin-3(2H)-one
-
NSC694622
2-[2-(4-heptylphenyl)ethyl]-6-hydroxybenzoic acid
2-[4-(4-methylphenyl)-1,3-thiazol-2-yl]-1,2-benzothiazol-3(2H)-one
-
-
2-[[4-(trifluoromethyl)phenyl]methyl][1,2]thiazolo[5,4-b]pyridin-3(2H)-one
-
PU141
3,3'-[(2-oxocyclohexane-1,3-diylidene)di(E)methanylylidene]dibenzonitrile
-
-
3-(Z)-(benzylsulfanyl)propenoic acid
-
-
3-(Z)-(benzylsulfinyl)-2-N-(4-dimethylaminoanilino)-propenamide
-
-
3-(Z)-(benzylsulfinyl)-2-N-(4-morpholinoanilino)-propenamide
-
-
3-(Z)-(benzylsulfinyl)-N-(2-pyridyl)propenamide
-
-
3-(Z)-(benzylsulfinyl)-N-(3-pyridyl)propenamide
-
-
3-(Z)-(benzylsulfinyl)-N-(4-pyridyl)propenamide
-
-
3-bromo-N'-(3-ethoxybenzoyl)-2-fluorobenzenesulfonohydrazide
-
3-fluoro-N'-(2-fluorobenzene-1-sulfonyl)-5-(1H-pyrazol-1-yl)benzohydrazide
-
3-fluoro-N'-(2-fluorobenzene-1-sulfonyl)-5-(furan-2-yl)benzohydrazide
-
3-fluoro-N'-(2-fluorobenzene-1-sulfonyl)-5-(pyrimidin-2-yl)benzohydrazide
-
3-pentadecylidenepentane-2,4-dione
-
inhibition of the acetylation of histone H3 residuesK9/K14, being practically inactive in all the other assays
3-quinolinecarboxylic acid ethyl ester
-
effects in vivo, overview
3-Z-benzylsulfanyl-4-trityloxy-but-2-enoic acid phenylamide
-
-
3-Z-benzylsulfinyl-4-trityloxy-but-2-enoic acid phenylamide
-
-
3-[(1E)-1-[2-[4-(4-chlorophenyl)-1,3-thiazol-2-yl]hydrazinylidene]ethyl]-2H-1-benzopyran-2-one
-
3-[(1Z)-1-[(3E)-3-[2-[4-(4-chlorophenyl)-1,3-thiazol-2-yl]hydrazinylidene]cyclopentylidene]ethyl]-2H-1-benzopyran-2-one
-
-
3-[(E)-[2-[4-(4-chlorophenyl)-1,3-thiazol-2-yl]hydrazinylidene]methyl]-2,3-dihydro-1H-indole
-
3-[(Z)-[(3E)-3-[2-[4-(4-chlorophenyl)-1,3-thiazol-2-yl]hydrazinylidene]cyclopentylidene]methyl]-1H-indole
-
-
3-[2-(pentadecanoylamino)benzamido]benzoic acid
-
-
3-[2-(tridecanoylamino)benzamido]benzoic acid
-
-
3-[2-[(2E)-2-(3-methylcyclopentylidene)hydrazinyl]-1,3-thiazol-4-yl]-2H-1-benzopyran-2-one
-
-
3-[2-[(2Z)-2-(3-methylcyclopentylidene)hydrazinyl]-1,3-thiazol-4-yl]-2H-1-benzopyran-2-one
-
3-[2-[2-(propan-2-ylidene)hydrazinyl]-1,3-thiazol-4-yl]-2H-1-benzopyran-2-one
-
4,5-dichloro-2-ethylisothiazol-3(2H)-one
-
-
4,5-dichloro-2-ethylisothiazol-3(2H)-one-1-oxide
-
-
4-(3-oxo-1,2-benzothiazol-2(3H)-yl)butanoic acid
-
-
4-(4-bromophenyl)-2-[2-(propan-2-ylidene)hydrazinyl]-1,3-thiazole
4-(4-chlorophenyl)-2-(2-cyclopentylidenehydrazinyl)-1,3-thiazole
-
CPTH2
4-(4-chlorophenyl)-2-[(2E)-2-(3-cyclooctylcyclopentylidene)hydrazinyl]-1,3-thiazole
-
-
4-(4-chlorophenyl)-2-[(2E)-2-(3-methylcyclopentylidene)hydrazinyl]-1,3-thiazole
-
CPTH6
4-(4-chlorophenyl)-2-[(2E)-2-[(3Z)-3-(1-cyclohexylethylidene)cyclopentylidene]hydrazinyl]-1,3-thiazole
-
-
4-(4-chlorophenyl)-2-[(2E)-2-[(3Z)-3-(4,4-dimethylcyclohex-2-en-1-ylidene)cyclopentylidene]hydrazinyl]-1,3-thiazole
-
-
4-(4-chlorophenyl)-2-[(2E)-2-[(3Z)-3-[1-(1,3-thiazol-2-yl)ethylidene]cyclopentylidene]hydrazinyl]-1,3-thiazole
-
-
4-(4-chlorophenyl)-2-[(2E)-2-[1-(1,3-thiazol-2-yl)ethylidene]hydrazinyl]-1,3-thiazole
-
4-(4-chlorophenyl)-2-[(2E)-2-[3-(propan-2-ylidene)cyclopentylidene]hydrazinyl]-1,3-thiazole
-
-
4-(4-chlorophenyl)-2-[2-(propan-2-ylidene)hydrazinyl]-1,3-thiazole
-
4-(4-nitrophenyl)-2-[2-(propan-2-ylidene)hydrazinyl]-1,3-thiazole
-
-
4-(aminoacetyl)-N-benzyl-2-methyl-3,4-dihydro-2H-1,4-benzothiazine-7-sulfonamide
-
-
4-([4-[3-(methoxycarbonyl)-2,7,7-trimethyl-5-oxo-1,4,5,6,7,8-hexahydroquinolin-4-yl]phenoxy]methyl)benzoic acid
-
-
4-acetyl-2-methyl-3,4-dihydro-2H-1,4-benzothiazine-7-sulfonamide
-
-
4-acetyl-2-methyl-N-(morpholin-4-yl)-3,4-dihydro-2H-1,4-benzothiazine-7-sulfonamide
-
-
4-acetyl-2-methyl-N-phenyl-3,4-dihydro-2H-1,4-benzothiazine-7-sulfonamide
-
-
4-acetyl-2-methyl-N-propyl-3,4-dihydro-2H-1,4-benzothiazine-7-sulfonamide
-
-
4-acetyl-N,N-dibenzyl-2-methyl-3,4-dihydro-2H-1,4-benzothiazine-7-sulfonamide
-
-
4-acetyl-N-benzyl-2-methyl-3,4-dihydro-2H-1,4-benzothiazine-7-sulfonamide
-
-
4-acetyl-N-cyclohexyl-2-methyl-3,4-dihydro-2H-1,4-benzothiazine-7-sulfonamide
-
-
4-acetyl-N-[(3-bromophenyl)methyl]-2-methyl-3,4-dihydro-2H-1,4-benzothiazine-7-sulfonamide
-
-
4-acetyl-N-[(4-methoxyphenyl)methyl]-2-methyl-3,4-dihydro-2H-1,4-benzothiazine-7-sulfonamide
-
-
4-azidomethyl-2-phenyl-isothiazol-3(2H)-one
-
-
4-bromomethyl-2-phenylisothiazol-3(2H)-one
-
-
4-hydroxy-2-methylquinoline-3-carboxylic acid
-
-
4-hydroxy-2-pentadecylquinoline-3-carboxylic acid
-
-
4-hydroxy-2-pentylquinoline-3-carboxylate
-
effects in vivo, overview, in vitro clear reduction of the acetylation extents of both histone H3 and alpha-tubulin at 0.1 mM
4-hydroxy-2-pentylquinoline-3-carboxylic acid
4-hydroxy-3-[(E)-[[2-(3-iodophenyl)-1,3-benzoxazol-5-yl]imino]methyl]benzoic acid
-
C146
4-methoxymethyl-2-phenyl-isothiazol-3(2H)-one
-
-
4-methyl-2-phenylisothiazol-3(2H)-one
-
-
4-methyl-5-methoxy-2-phenyl-isothiazol-3(2H)-one
-
-
4-trityloxy-but-2-ynoic acid phenylamide
-
-
4-[2-(pentadecanoylamino)benzamido]benzoic acid
-
-
4-[2-(tridecanoylamino)benzamido]benzoic acid
-
-
4-[[(4-methoxybenzene-1-sulfonyl)oxy]imino]-2,6-dimethylcyclohexa-2,5-dien-1-one
-
L002
4-[[2,6-dibromo-4-(3,3,6,6-tetramethyl-1,8-dioxo-1,2,3,4,5,6,7,8,9,10-decahydroacridin-9-yl)phenoxy]methyl]benzoic acid
-
DC-G16-11
4-[[2,6-dichloro-4-(1,8-dioxo-1,2,3,4,5,6,7,8,9,10-decahydroacridin-9-yl)phenoxy]methyl]benzoic acid
-
-
4-[[2-bromo-4-(3,3,6,6-tetramethyl-1,8-dioxo-1,2,3,4,5,6,7,8,9,10-decahydroacridin-9-yl)phenoxy]methyl]benzoic acid
-
-
4-[[4-(1,8-dioxo-1,2,3,4,5,6,7,8,9,10-decahydroacridin-9-yl)-2-methoxyphenoxy]methyl]benzoic acid
-
-
4-[[4-(3-cyano-2-methyl-5-oxo-1,4,5,6,7,8-hexahydroquinolin-4-yl)phenoxy]methyl]benzoic acid
-
-
4-[[4-(8-oxo-7,8,9,10,11,12-hexahydrobenzo[c]acridin-7-yl)phenoxy]methyl]benzoic acid
-
-
5,5'-disulfanediylbis(1,2-thiazole)
-
NU9056
5-acetoxymethyl-2-phenylisothiazol-3(2H)-one
-
-
5-azidomethyl-2-phenylisothiazol-3(2H)-one
-
-
5-bromo-2-(dimethylamino)-6-tetradecylpyrimidin-4(3H)-one
-
-
5-bromo-2-(dimethylamino)-6-tridecylpyrimidin-4(3H)-one
-
-
5-bromo-N'-(3-ethoxybenzoyl)-2-fluorobenzenesulfonohydrazide
-
5-butyl-2-hydroxybenzoic acid
-
-
5-chloro-2-(3-chloro-4-fluorophenyl)isothiazol-3(2H)-one
-
5-chloro-2-(4-nitrophenyl)-1,2-thiazol-3(2H)-one
-
CCT077791
5-chloro-2-ethyl-4-methyl-1H-1l4,2-thiazole-1,3(2H)-dione
-
-
5-chloro-2-ethyl-4-methylisothiazol-3(2H)-one
-
-
5-chloro-2-ethyl-4-methylisothiazol-3(2H)-one-1-oxide
-
-
5-chloro-2-ethylisothiazol-3(2H)-one
5-chloro-2-ethylisothiazol-3(2H)-one-1-oxide
-
-
5-chloro-2-pentylisothiazol-3(2H)-one
-
5-chloro-4-methyl-2-phenylisothiazol-3(2H)-one
-
-
5-decyl-2-hydroxybenzoic acid
-
5-hydroxy-2,3-dimethylnaphthalene-1,4-dione
-
PTK1
5-hydroxy-2-methylnaphthalene-1,4-dione
-
RTK1
5-hydroxymethyl-2-phenylisothiazol-3(2H)-one
-
-
5-methyl-2-phenylisothiazol-3(2H)-one
-
-
5-phenylureidomethyl-2-phenylisothiazol-3(2H)-one
-
-
6-(4-chlorophenyl)-2-(2-(3-methylcyclopentylidene)hydrazinyl)pyrimidin-4(3H)-one
-
6-(4-chlorophenyl)-2-(2-cyclopentylidenehydrazinyl)pyrimidin-4(3H)-one
-
6-(4-chlorophenyl)-2-[(2E)-2-(3-methylcyclopentylidene)hydrazinyl]pyrimidin-4(3H)-one
-
-
6-dodecyl-2-(methylsulfanyl)pyrimidin-4(3H)-one
-
-
6-dodecyl-2-sulfanylidene-2,3-dihydropyrimidin-4(1H)-one
-
-
8-benzyl-10,11-dimethoxy-5,6,7,9,14,14a-hexahydro-2H-[1,3]dioxolo[4,5-h]isoquinolino[3,2-a][2]benzazepin-8-ium bromide
-
-
8-benzyl-11,12-dimethoxy-5,6,7,9,14,14a-hexahydro-2H-[1,3]dioxolo[4,5-h]isoquinolino[3,2-a][2]benzazepin-8-ium bromide
-
-
8-benzyl-2,3,10,11-tetramethoxy-5,6,7,9-tetrahydroisoquinolino[3,2-a][2]benzazepin-8-ium chloride
-
-
8-benzyl-2,3,11,12-tetramethoxy-5,6,7,9-tetrahydroisoquinolino[3,2-a][2]benzazepin-8-ium bromide
-
-
9-[3-bromo-4-[(3-fluorophenyl)methoxy]phenyl]-3,4,6,7,9,10-hexahydroacridine-1,8(2H,5H)-dione
-
-
9-[4-(benzyloxy)-3-bromophenyl]-3,3,6,6-tetramethyl-3,4,6,7,9,10-hexahydroacridine-1,8(2H,5H)-dione
-
-
Ac-L-Lys(CoA)-NH2
bisubstrate inhibitor
acetylated histone H3 peptide
-
acetylated at Lys14, product inhibition of PCAF protein, noncompetitive against both substrates
-
allspice hot water extract
-
leads to a potent anti-HAT activity since the allspice hot water extract possesses a strong inhibitory effect on p300 and CBP (40% at 0.1 ng/ml). Chromatin immunoprecipitation indicates that the acetylation of histone H3 in the PSA and B2M promoter regions was also repressed
-
anacardic acid
anarcadic acid
-
B-homo berberine
-
10,11-dimethoxy-6,7-dihydro-2H,5H-[1,3]dioxolo[4,5-h]isoquinolino[3,2-a][2]benzazepin-8-ium methanesulfonate
B-homo palmatine
-
2,3,10,11-tetramethoxy-6,7-dihydro-5H-isoquinolino[3,2-a][2]benzazepin-8-ium methanesulfonate
benzyl [2-(5-chloro-3-oxoisothiazol-2(3H)-yl)ethyl]carbamate
-
bisubstrate analogue histone H3-peptide-coenzyme A
-
bisubstrate analogue methyl-histone H3-peptide-coenzyme A
-
peptide consisting of 20 and 7 amino acid residues
-
catechin
-
-
CCT004463
-
in vivo cell proliferation inhibition
CCT004464
-
in vivo cell proliferation inhibition
CCT004465
-
in vivo cell proliferation inhibition
CCT004466
-
in vivo cell proliferation inhibition
CCT004467
-
in vivo cell proliferation inhibition
CCT077791
-
IC50: 0.0022-0.0073 mM, in vivo cell proliferation inhibition, reduces acetylation of histones H3 and H4 and alpha-tubulin in cancer cell lines
CCT077792
-
IC50: 0.0027-0.015 mM, in vivo cell proliferation inhibition
CCT077796
-
IC50: 0.0187-0.0202 mM, in vivo cell proliferation inhibition
CCT079769
-
IC50: 0.0547 mM, in vivo cell proliferation inhibition
chondroitin sulfate
-
-
CPTH6
curcumin
delphinidin
-
-
DELTA12-prostaglandin J2
-
-
desulfo-coenzyme A
-
dead-end inhibitor, noncompetitive versus histone H3-peptide and competitive versus actyl-CoA
diethyl (1-aminotetradecyl)propanedioate
-
-
diethyl (1-chlorotetradecyl)propanedioate
-
-
diethyl (1-hydroxytetradecyl)propanedioate
-
-
diethyl (pentadecan-2-yl)propanedioate
-
-
diethyl 2-tetradecylidenemalonate
-
compound exhibits a significant inhibition of the acetylation of almost any lysine residue explored, with the sole exception of residue K8 of H4. Compound reduces the level of K5Ac of H4 and, more markedly, K16Ac of H4
diethyl benzylidenepropanedioate
-
-
diethyl decylidenepropanedioate
-
-
diethyl dodecylidenepropanedioate
-
-
diethyl dodecylpropanedioate
-
-
diethyl pentadecylidenepropanedioate
i.e. SPV106, a long-chain alkylidenemalonate (LoCAM), 74% inhibition at 0.05 mM
diethyl tetradecylidenepropanedioate
-
-
diethyl tetradecylpropanedioate
-
-
diethyl tridecylidenepropanedioate
-
-
diethyl tridecylpropanedioate
-
-
diethyl undecylidenepropanedioate
-
-
diethyl [(dodecylamino)methylidene]propanedioate
-
-
diethyl [(naphthalen-1-yl)methylidene]propanedioate
-
-
diethyl [(naphthalen-2-yl)methylidene]propanedioate
-
-
DNA
-
acetylation of histone H1by the enzymes PCAF and GNC5 is inhibited in vivo by complexing of H1 with DNA
epigallocatechin-3-gallate
ethyl (3E,5E)-3,5-bis[(3-bromo-4-hydroxyphenyl)methylidene]-4-oxocyclohexane-1-carboxylate
-
-
ethyl 2-decyl-4-hydroxyquinoline-3-carboxylate
-
-
ethyl 2-methyl-6-([5-[(prop-2-yn-1-yl)amino]pentyl]oxy)quinoline-3-carboxylate
ethyl 2-methylquinoline-3-carboxylate
ethyl 3-(5-chloro-3-oxoisothiazol-2(3H)-yl)propanoate
-
ethyl 4-hydroxy-2-methylquinoline-3-carboxylate
-
-
ethyl 4-hydroxy-2-pentadecylquinoline-3-carboxylate
-
-
ethyl 4-hydroxy-2-pentylquinoline-3-carboxylate
-
-
ethyl 4-oxo-2-sulfanylidene-6-tetradecyl-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
-
ethyl quinoline-3-carboxylate
-
MC1752
garcinol
geminin
-
a Cdt1 repressor, inhibits HBO1 acetylase activity in a a Cdt1-dependent manner in the context of a Cdt1-HBO1 complex, and it associates with origins and inhibits H4 acetylation and licensing in vivo, but geminin does not block the interaction of Cdt1 with HBO1 in vitro or Cdt1-dependent recruitment of HBO1 to replication origins in vivo
-
H3-CoA-20
H3-CoA-20-Tat
-
IC50: 0.012 mM, recombinant enzyme
-
heparan sulfate proteoglycans
-
heparan sulfate proteoglycans isolated from corneal and pulmonary fibroblasts inhibit HAT activity with similar effectiveness as heparin
-
heparin
-
ability of heparin to inhibit HAT is dependent upon its size and structure: small heparin-derived oligosaccharides (above 8 sugars) and N-desulfated or O-desulfated heparin show reduced inhibitory activity. Heparin is shown to bind to pCAF. Enzyme assays indicate that heparin shows the characteristics of a competitive-like inhibitor causing a 50fold increase in the Km of pCAF for histone H4
heptylbenzene
-
-
histone H3-peptide mutant K14A
-
dead-end inhibitor analogue, mutant histone H3 -peptide consisting of amino acid residues 3-20 K14A
-
hyaluronic acid
-
-
isogarcinol
isothiazole
-
-
isothiazolone
Keratan sulfate
-
-
L-Lys-CoA
-
-
LTK14
Lys-CoA
Lys-CoA-Tat
-
IC50: 250 nM, recombinant enzyme, complete inhibition of acetylation of the promyelotic leukemia zinc finger gene
methyl 2-(5-chloro-3-oxoisothiazol-2(3H)-yl)ethanoate
-
methyl 3-(3-oxoisothiazol-2(3H)-yl)propanoate
-
methyl 3-(4,5-dichloro-1-oxido-3-oxoisothiazol-2(3H)-yl)propanoate
-
-
methyl 3-(4,5-dichloro-3-oxoisothiazol-2(3H)-yl)propanoate
-
-
methyl 3-(5-chloro-1,3-dioxo-1,3-dihydro-2H-1l4,2-thiazol-2-yl)propanoate
-
-
methyl 3-(5-chloro-1-oxido-3-oxoisothiazol-2(3H)-yl)propanoate
methyl 3-(5-chloro-3-oxo-1,2-thiazol-2(3H)-yl)propanoate
-
-
methyl 3-(5-chloro-3-oxoisothiazol-2(3H)-yl)propanoate
-
-
methyl 3-(5-chloro-3-oxoisothiazol-2(3H)-yl)propanoic acid
-
methyl 3-(5-chloro-4-methyl-1,3-dioxo-1,3-dihydro-2H-1l4,2-thiazol-2-yl)propanoate
-
-
methyl 3-(5-chloro-4-methyl-1-oxido-3-oxoisothiazol-2(3H)-yl)propanoate
-
-
methyl 3-(5-chloro-4-methyl-3-oxoisothiazol-2(3H)-yl)propanoate
-
-
methyl 3-[(5-chloro-1,2-thiazol-3-yl)amino]propanoate
-
-
methyl 3-[(5-chloroisothiazol-3-yl)amino]propanoate
-
methyl 3-[4-chloro-5-(dodecylthio)-1-oxido-3-oxoisothiazol-2(3H)-yl]propanoate
-
-
methyl 3-[4-[[(benzyloxy)carbonyl]amino]-5-chloro-3-oxo-1,2-thiazol-2(3H)-yl]propanoate
-
-
methyl 3-[4-{[(benzyloxy)carbonyl]amino}-5-chloro-3-oxoisothiazol-2(3H)-yl]propanoate
-
methyl 3-[5-(dodecylthio)-1-oxido-3-oxoisothiazol-2(3H)-yl] propanoate
-
-
methyl 4-(3-oxoisothiazol-2(3H)-yl)butanoate
-
methyl 4-(5-chloro-3-oxoisothiazol-2(3H)-yl)butanoate
-
methyl 5-(5-chloro-3-oxoisothiazol-2(3H)-yl)pentanoate
-
methyl 6-(5-chloro-3-oxoisothiazol-2(3H)-yl)hexanoate
-
MG149
montelukast
-
decreases HAT activity by attenuating the activating effect of TNF-alpha
N'-(2,6-difluorobenzene-1-sulfonyl)-3-fluoro-5-propoxybenzohydrazide
-
N'-(2,6-difluorobenzene-1-sulfonyl)-3-fluoro-5-[(propan-2-yl)oxy]benzohydrazide
-
N'-(2,6-difluorobenzene-1-sulfonyl)-3-methoxy-5-[(propan-2-yl)oxy]benzohydrazide
-
N'-(2,6-difluorobenzene-1-sulfonyl)-3-methyl-5-[(propan-2-yl)oxy]benzohydrazide
-
N'-(2-fluoro-3-methyl-5-((2-methylallyl)oxy)benzoyl)-benzenesulfonohydrazide
-
N'-(2-fluoro-3-methyl-5-((2-methylallyl)oxy)benzoyl)benzenesulfonohydrazide
-
N'-(2-fluoro-3-methyl-5-(1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
-
N'-(2-fluoro-3-methyl-5-(2H-1,2,3-triazol-2-yl)benzoyl)-naphthalene-2-sulfonohydrazide
-
N'-(2-fluoro-3-methyl-5-(3-methyl-1H-pyrazol-1-yl)benzoyl)-benzenesulfonohydrazide
-
N'-(2-fluoro-3-methyl-5-(3-methyl-1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
-
N'-(2-fluoro-3-methyl-5-(4-methyl-1H-pyrazol-1-yl)benzoyl)-benzenesulfonohydrazide
-
N'-(2-fluoro-3-methyl-5-(4-methyl-1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
-
N'-(2-fluoro-3-methyl-5-(5-methyl-1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
-
N'-(2-fluoro-5-(1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
-
N'-(2-fluoro-5-(2H-1,2,3-triazol-2-yl)benzoyl)benzenesulfonohydrazide
-
N'-(2-fluoro-5-(3-methyl-1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
-
N'-(2-fluoro-5-(4-fluoro-1H-pyrazol-1-yl)-3-methylbenzoyl)benzenesulfonohydrazide
-
N'-(2-fluoro-5-(4-methyl-1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
-
N'-(2-fluoro-5-(furan-2-yl)-3-methylbenzoyl)benzenesulfonohydrazide
-
N'-(2-fluoro-5-(furan-2-yl)benzoyl)benzenesulfonohydrazide
-
N'-(2-fluoro-5-(pyridin-2-yl)benzoyl)benzenesulfonohydrazide
-
N'-(2-fluoro-5-isopropoxy-3-methylbenzoyl)benzenesulfonohydrazide
-
N'-(2-fluoro-5-isopropoxybenzoyl)benzenesulfonohydrazide
-
N'-(2-fluoro-5-propoxybenzoyl)benzenesulfonohydrazide
-
N'-(2-fluorobenzene-1-sulfonyl)-3-(furan-2-yl)-5-methoxybenzohydrazide
-
N'-(2-fluorobenzene-1-sulfonyl)-3-(furan-2-yl)-5-methylbenzohydrazide
-
N'-(2-fluorobenzene-1-sulfonyl)-3-(naphthalen-2-yl)benzohydrazide
-
N'-(2-fluorobenzene-1-sulfonyl)-3-(pyrimidin-2-yl)benzohydrazide
-
N'-(2-fluorobenzene-1-sulfonyl)-3-(pyrimidin-4-yl)benzohydrazide
-
N'-(2-fluorobenzene-1-sulfonyl)-3-(trifluoromethoxy)benzohydrazide
-
N'-(2-fluorobenzene-1-sulfonyl)-3-methoxy-5-(pyridin-2-yl)benzohydrazide
-
N'-(2-fluorobenzene-1-sulfonyl)-3-methyl-5-(pyridin-2-yl)benzohydrazide
-
N'-(2-fluorobenzene-1-sulfonyl)-3-methyl-5-(pyrimidin-2-yl)benzohydrazide
-
N'-(2-fluorobenzene-1-sulfonyl)benzohydrazide
-
N'-(3-(1,2,4-oxadiazol-3-yl)benzoyl)-2-fluorobenzenesulfonohydrazide
-
N'-(3-(1,3,4-oxadiazol-2-yl)benzoyl)-2-fluorobenzenesulfonohydrazide
-
N'-(3-(1H-pyrazol-1-yl)benzoyl)-2-fluorobenzenesulfonohydrazide
-
N'-(3-(1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
-
N'-(3-(3,5-dimethyl-1H-pyrazol-1-yl)benzoyl)-2-fluorobenzenesulfonohydrazide
-
N'-(3-(4-fluoro-1H-pyrazol-1-yl)-5-methylbenzoyl)benzenesulfonohydrazide
-
N'-(3-(allyloxy)-5-fluorobenzoyl)-2-fluorobenzenesulfonohydrazide
-
N'-(3-(allyloxy)-5-methylbenzoyl)-2-fluorobenzenesulfonohydrazide
-
N'-(3-(allyloxy)benzoyl)-2-fluorobenzenesulfonohydrazide
-
N'-(3-(cyclopentyloxy)benzoyl)-2-fluorobenzenesulfonohydrazide
-
N'-(3-(cyclopentyloxy)benzoyl)benzenesulfonohydrazide
-
N'-(3-(cyclopropylmethoxy)-5-fluorobenzoyl)-2-fluorobenzenesulfonohydrazide
-
N'-(3-(cyclopropylmethoxy)-5-methylbenzoyl)-2-fluorobenzenesulfonohydrazide
-
N'-(3-(cyclopropylmethoxy)benzoyl)-2-fluorobenzenesulfonohydrazide
-
N'-(3-(ethoxymethyl)-5-methylbenzoyl)-2-fluorobenzenesulfonohydrazide
-
N'-(3-(furan-2-yl)-5-methoxybenzoyl)benzenesulfonohydrazide
-
N'-(3-(furan-2-yl)-5-methylbenzoyl)benzenesulfonohydrazide
-
N'-(3-(pyridin-2-yl)benzoyl)benzenesulfonohydrazide
-
N'-(3-(pyrimidin-2-yl)benzoyl)benzenesulfonohydrazide
-
N'-(3-(pyrimidin-5-yl)benzoyl)benzenesulfonohydrazide
-
N'-(3-(thiazol-2-yl)benzoyl)benzenesulfonohydrazide
-
N'-(3-(thiazol-4-yl)benzoyl)benzenesulfonohydrazide
-
N'-(3-(trifluoromethoxy)benzoyl)benzenesulfonohydrazide
-
N'-(3-(trifluoromethyl)benzoyl)benzenesulfonohydrazide
-
N'-(3-bromobenzoyl)-2-fluorobenzenesulfonohydrazide
-
N'-(3-butoxybenzoyl)-2-fluorobenzenesulfonohydrazide
-
N'-(3-butoxybenzoyl)benzenesulfonohydrazide
-
N'-(3-chloro-5-(furan-2-yl)benzoyl)-2-fluorobenzenesulfonohydrazide
-
N'-(3-chloro-5-(furan-2-yl)benzoyl)benzenesulfonohydrazide
-
N'-(3-chloro-5-(thiophen-2-yl)benzoyl)-2-fluorobenzenesulfonohydrazide
-
N'-(3-cyclopropoxy-5-methylbenzoyl)-2-fluorobenzenesulfonohydrazide
-
N'-(3-ethoxy-5-fluorobenzoyl)-2-fluorobenzenesulfonohydrazide
-
N'-(3-ethoxy-5-methoxybenzoyl)-2-fluorobenzenesulfonohydrazide
-
N'-(3-ethoxy-5-methylbenzoyl)-2,3-difluorobenzenesulfonohydrazide
-
N'-(3-ethoxy-5-methylbenzoyl)-2,4-difluorobenzenesulfonohydrazide
-
N'-(3-ethoxy-5-methylbenzoyl)-2,5-difluorobenzenesulfonohydrazide
-
N'-(3-ethoxy-5-methylbenzoyl)-2,6-difluorobenzenesulfonohydrazide
-
N'-(3-ethoxy-5-methylbenzoyl)-2-fluoro-3-methylbenzenesulfonohydrazide
-
N'-(3-ethoxy-5-methylbenzoyl)-2-fluoro-4-methylbenzenesulfonohydrazide
-
N'-(3-ethoxy-5-methylbenzoyl)-2-fluoro-5-methylbenzenesulfonohydrazide
-
N'-(3-ethoxy-5-methylbenzoyl)-2-fluorobenzenesulfonohydrazide
-
N'-(3-ethoxybenzoyl)-2-fluoro-5-methoxybenzenesulfonohydrazide
-
N'-(3-ethoxybenzoyl)-2-fluoro-6-methoxybenzenesulfonohydrazide
-
N'-(3-ethoxybenzoyl)-2-fluorobenzenesulfonohydrazide
-
N'-(3-ethoxybenzoyl)benzenesulfonohydrazide
-
N'-(3-ethoxybenzoyl)naphthalene-2-sulfonohydrazide
-
N'-(3-ethylbenzoyl)-2-fluorobenzenesulfonohydrazide
-
N'-(3-ethylbenzoyl)benzenesulfonohydrazide
-
N'-(3-fluoro-5-(1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
-
N'-(3-fluoro-5-(3-methyl-1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
-
N'-(3-fluoro-5-(4-methyl-1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
-
N'-(3-fluoro-5-(furan-2-yl)benzoyl)benzenesulfonohydrazide
-
N'-(3-fluoro-5-(pyridin-2-yl)benzoyl)benzenesulfonohydrazide
-
N'-(3-fluoro-5-propoxybenzoyl)benzenesulfonohydrazide
-
N'-(3-isobutoxybenzoyl)benzenesulfonohydrazide
-
N'-(3-isopropoxybenzoyl)benzenesulfonohydrazide
-
N'-(3-isopropylbenzoyl)benzenesulfonohydrazide
-
N'-(3-methoxy-5-(1H-pyrazol-1-yl)benzoyl)-benzenesulfonohydrazide
-
N'-(3-methoxy-5-(1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
-
N'-(3-methoxy-5-(pyridin-2-yl)benzoyl)benzenesulfonohydrazide
-
N'-(3-methoxybenzoyl)naphthalene-2-sulfonohydrazide
-
N'-(3-methylbenzoyl)benzenesulfonohydrazide
-
N'-(3-phenoxybenzoyl)benzenesulfonohydrazide
-
N'-(3-propoxybenzoyl)benzenesulfonohydrazide
-
N'-(3-propoxybenzoyl)naphthalene-2-sulfonohydrazide
-
N'-(3-propylbenzoyl)benzenesulfonohydrazide
-
N'-(5-(allyloxy)-2-fluoro-3-methylbenzoyl)-benzenesulfonohydrazide
-
N'-(5-(allyloxy)-2-fluoro-3-methylbenzoyl)benzenesulfonohydrazide
-
N'-(5-(allyloxy)-2-fluorobenzoyl)benzenesulfonohydrazide
-
N'-(5-(cyclopropylmethoxy)-2-fluoro-3-methylbenzoyl)-benzenesulfonohydrazide
-
N'-(5-(cyclopropylmethoxy)-2-fluoro-3-methylbenzoyl)benzenesulfonohydrazide
-
N'-(5-(ethoxymethyl)-2-fluoro-3-methylbenzoyl)-benzenesulfonohydrazide
-
N'-(5-(ethoxymethyl)-2-fluoro-3-methylbenzoyl)benzenesulfonohydrazide
-
N'-(5-ethoxy-2-fluoro-3-methylbenzoyl)-2-fluorobenzenesulfonohydrazide
-
N'-(5-ethoxy-2-fluoro-3-methylbenzoyl)naphthalene-2-sulfonohydrazide
-
N'-(5-ethoxy-2-fluorobenzoyl)benzenesulfonohydrazide
-
N'-(benzenesulfonyl)-2-fluoro-3-methyl-5-(pyridin-2-yl)benzohydrazide
-
N'-(benzenesulfonyl)-2-fluoro-3-methyl-5-(pyrimidin-2-yl)benzohydrazide
-
N'-(benzenesulfonyl)-2-fluoro-3-methyl-5-[(propan-2-yl)oxy]benzohydrazide
-
N'-(benzenesulfonyl)-2-fluoro-5-(pyridazin-4-yl)benzohydrazide
-
WM-2474
N'-(benzenesulfonyl)-2-fluoro-5-(pyrimidin-2-yl)benzohydrazide
-
N'-(benzenesulfonyl)-2-fluoro-5-(pyrimidin-4-yl)benzohydrazide
-
N'-(benzenesulfonyl)-2-fluoro-5-[(prop-2-yn-1-yl)oxy]benzohydrazide
-
N'-(benzenesulfonyl)-3-fluoro-5-(pyrimidin-2-yl)benzohydrazide
-
N'-(benzenesulfonyl)-3-fluorobenzohydrazide
-
N'-(benzenesulfonyl)-3-methoxy-5-(pyrimidin-2-yl)benzohydrazide
-
N'-(benzenesulfonyl)-3-methoxybenzohydrazide
-
N'-(benzenesulfonyl)-3-methyl-5-(pyrimidin-2-yl)benzohydrazide
-
N'-(benzenesulfonyl)-4-fluoro-5-methyl[1,1'-biphenyl]-3-carbohydrazide
N'-(benzenesulfonyl)-5-chloro-4-fluoro[1,1'-biphenyl]-3-carbohydrazide
-
N'-(ethoxy-2-fluoro-3-methylbenzoyl)-benzenesulfonohydrazide
-
N'-(ethoxy-2-fluoro-3-methylbenzoyl)benzenesulfonohydrazide
-
N'-(naphthalene-2-sulfonyl)benzohydrazide
-
N'-([1,1'-biphenyl]-3-carbonyl)-2-fluorobenzenesulfonohydrazide
-
N-(2-fluoro-3-methyl-5-(2H-1,2,3-triazol-2-yl)benzoyl)benzenesulfonohydrazide
-
N-(2-fluoro-3-methyl-5-propoxybenzoyl)-benzenesulfonohydrazide
-
N-(2-fluoro-3-methyl-5-propoxybenzoyl)benzenesulfonohydrazide
-
N-(3-aminopropyl)acetamido-CoA
-
-
N-(3-benzamidobutyl)acetamido-CoA
-
-
N-(3-benzamidopentyl)acetamido-CoA
-
-
N-(3-benzamidopropyl)acetamido-CoA
-
-
N-(3-[[(2,2-dimethylpropanoyl)oxy]amino]propyl)acetamido-CoA
-
-
N-(4-acetyl-2-methyl-3,4-dihydro-2H-1,4-benzothiazine-7-sulfonyl)benzamide
-
-
N-(4-chloro-3-trifluoromethyl-phenyl)-2-ethoxy-6-pentadecyl-benzamide
-
-
N-(4-chlorophenyl)-2-(4,6-dimethyl-3-oxo[1,2]thiazolo[5,4-b]pyridin-2(3H)-yl)acetamide
-
-
N-(4-cyano-3-(trifluoromethyl)phenyl)-2-decyl-6-ethoxybenzamide
-
inhibits human p300 recombinant enzyme similar to anacardic acid
N-(4-cyano-3-(trifluoromethyl)phenyl)-2-ethoxy-6-octylbenzamide
-
inhibits human p300 recombinant enzyme similar to anacardic acid, moreover this inhibitor induces significant apoptosis at 0.05 nM in U937 leukemia cells
N-(4-[[(2,2-dimethylpropanoyl)oxy]amino]butyl)acetamido-CoA
-
-
N-(4-[[(2-amino-4-oxo-3,4-dihydroquinazolin-6-yl)methyl](prop-2-yn-1-yl)amino]benzoyl)-L-glutamic acid
-
-
N-(5-[[(2,2-dimethylpropanoyl)oxy]amino]pentyl)acetamido-CoA
-
-
N-benzyl-2,4-dimethyl-3,4-dihydro-2H-1,4-benzothiazine-7-sulfonamide
-
-
N-benzyl-2-methyl-4-(phenylacetyl)-3,4-dihydro-2H-1,4-benzothiazine-7-sulfonamide
-
-
N-benzyl-4-(chloroacetyl)-2-methyl-3,4-dihydro-2H-1,4-benzothiazine-7-sulfonamide
-
-
N-benzyl-4-(cyclohexanecarbonyl)-2-methyl-3,4-dihydro-2H-1,4-benzothiazine-7-sulfonamide
-
-
N-benzyl-4-(cyclopropanecarbonyl)-2-methyl-3,4-dihydro-2H-1,4-benzothiazine-7-sulfonamide
-
-
N-benzylacetamido-CoA
-
-
N-[(1S)-1-cyclopropyl-2,2,2-trifluoroethyl]-N-[(4-fluorophenyl)methyl]-2-[(1R)-5-[(methylcarbamoyl)amino]-2',4'-dioxo-2,3-dihydrospiro[indene-1,5'-[1,3]oxazolidin]-3'-yl]acetamide
-
-
N-[(2-chloro-6-fluorophenyl)methyl]-2-(2,5-dioxo-4-phenyl-4-propylimidazolidin-1-yl)-N-methylacetamide
-
-
N-[(3S)-5-[[(1S)-3-(5-[[(5S)-5-(3-carbamimidamidopropyl)-3,6-dioxopiperazin-2-yl]methyl]-2-hydroxyphenoxy)-1-carboxypropyl]amino]-3-carboxy-3-hydroxy-5-oxopentanoyl]-L-aspartic acid
-
NK13650A
N-[(4-fluorophenyl)methyl]-2-[(1R)-5-[(methylcarbamoyl)amino]-2',4'-dioxo-2,3-dihydrospiro[indene-1,5'-[1,3]oxazolidin]-3'-yl]-N-[(2S)-1,1,1-trifluoropropan-2-yl]acetamide
-
A-485
N-[2-(2,5-dimethoxybenzoyl)-3-methyl-1-benzofuran-6-yl]-3,5-dimethoxybenzamide
-
F2209-0381
N-[4-chloro-3-(trifluoromethyl)phenyl]-2-ethoxy-6-tetradecylbenzamide
-
-
N-[4-cyano-3-(trifluoromethyl)phenyl]-2-ethoxy-6-heptylbenzamide
-
-
N-[5-[(5-[[5-([4-[(5-[[5-([5-[(5-[[3-(dimethylamino)propyl]carbamoyl]-1-methyl-1H-pyrrol-3-yl)carbamoyl]-1-methyl-1H-pyrrol-3-yl]carbamoyl)-1-methyl-1H-pyrrol-3-yl]carbamoyl]-1-methyl-1H-pyrrol-3-yl)amino]-4-oxobutyl]carbamoyl)-1-methyl-1H-pyrrol-3-yl]carbamoyl]-1-methyl-1H-pyrrol-3-yl)carbamoyl]-1-methyl-1H-pyrrol-3-yl]-4-[(N-[[2-(2-[4-[(4Z)-4-[[5-(2,3-dimethyl-6-nitrophenyl)furan-2-yl]methylidene]-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl]benzamido]ethoxy)ethoxy]acetyl]-beta-alanyl)amino]-1-methyl-1H-pyrrole-2-carboxamide
-
naphthoquinone
-
-
NU9056
palmatine
-
-
peptide conjugate Boc-C5-CoA
peptide Boc-C5-CoA, the molecule exploits an additional electron-rich pocket (P2) about 10 A away from the lysine binding pocket (P1). Boc-C5-CoA that shows high affinity for, comprises a CoA moiety which binds to the P1 pocket, a 1,5-pentanediamine linker and a tert-butoxycarbonyl cap, which is accommodated by the P2 pocket. CoA is connected to the N1 of the linker through a carboxymethylene bridge, while the tert-butoxycarbonyl cap protects the N5
-
peptide conjugate H3-CoA-20
peptide H3-CoA-20 resembles the K14-containing sequence of histone H3, the main substrate of PCAF, R1 is A-P-R-K-Q-L-OH and R2 is G-G-T-S-L-R-A-T-Q-K-T-R-A-NHCH3
-
peptide conjugate H4-K16-CoA
peptide H4-K16-CoA, R1 is K-A-G-G-K-G-L-G-K-G-G-K-G-R-G-S-OCH3 and R2 is R-H-R-K-NH2
-
Plumbagin
procyanidin B1
-
-
procyanidin B2
-
-
procyanidin B3
-
-
Prostaglandin A2
-
-
Prostaglandin B2
-
-
prostaglandin J2
-
-
prostaglandin K2
-
-
protein HBZ
HTLV-1 (basic zipper factor, from a human T cell leukemia virus), interacts with HBO1 during pathogenesis and inhibits its acetylation activity to reduce p53-mediated transcription activation of p21/CDKN1A and Gadd45a, and subsequently delays G2-cell cycle arrest. BRPF2 binds to HBO1 on the hinge connecting the NTD and MYST domain, thus it is reasonable to develop BRPF2-mimic peptides or molecules for disrupting HBO1-BRPF2 interaction and subsequently prevent the binding of HBO1 to chromatin
-
S-(4-benzylpiperazin-1-yl)(1-oxo)ethyl-CoA
-
-
S-(piperazin-1-yl)(1-oxo)ethyl-CoA
-
-
S-(tert-butyl 4-acetylpiperazin-1-yl)(1-oxo)ethyl-CoA
-
-
siRNA
-
silencing of enzyme gene
-
sodium 4-[3,5-bis[(E)-2-(4-hydroxy-3-methoxyphenyl)ethenyl]-1H-pyrazol-1-yl]benzoate
-
CTK7A
Spd(N1)-CoA
obtained by linking the polyamine spermidine to CoA using a carboxymethylene bridge
spermidine-CoA
-
-
spinosine
-
-
taxodione
-
-
tetradecylidenepropanedioic acid
-
EML264
thiazole
-
-
tridecylidenepropanedioic acid
-
-
venenatine
-
-
[(3,7-dimethyloctyl)oxy]benzene
-
-
[5-(4-[[(2-phenylethyl)(4-[4-[(pyrrolidin-1-yl)methyl]phenoxy]butyl)amino]methyl]phenyl)-2H-tetrazol-2-yl]acetic acid
-
TH1834
[histone H4]-L-lysine12-CoA
bisubstrate inhibitor, i.e. Ac-SGRGKGGKGLGK(CoA)GGAKRHRK, competitive inhibition with respect to both acetyl-CoA and histone H4, highly specific inhibitor for histone acetyltransferase 1
-
[histone H4]-L-lysine16-CoA
-
[histone H4]-L-lysine5-CoA
bisubstrate inhibitor, i.e. Ac-SGRGK(CoA)GGKGLGKGGAKRHRK
-
[histone H4]-L-lysine8-CoA
bisubstrate inhibitor, i.e. Ac-SGRGKGGK(CoA)GLGKGGAKRHRK
-
additional information
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(3E,5E)-1-ethyl-3,5-bis[(4-hydroxy-3-nitrophenyl)methylidene]piperidin-4-one
128% activity at 0.1 mM
(3E,5E)-3,5-bis[(3,4-dihydroxyphenyl)methylidene]piperidin-4-one
114% activity at 0.1 mM
[(3E,5E)-3,5-bis[(3,4-dihydroxyphenyl)methylidene]-4-oxocyclohexyl]acetic acid
128% activity at 0.1 mM
2-chloro-4-trifluoromethyl benzamide
-
activates the enzyme, the relative position of the -CF3 and -Cl is crucial for p300 HAT activity enhancement, overview
2-dodecylmalonate
-
compound induces hyperacetylation of specific lysine residues of histone H3, in particular residues K9 and K18, and raises the level of pan-acetylated H4. Compound inhibits the acetylation of all the other H3 and H4 lysines, with the exception of residue K8Ac of histone H4
4-chloro-2-trifluoromethyl benzamide
-
activates the enzyme, the relative position of the -CF3 and -Cl is crucial for p300 HAT activity enhancement, overview
bleomycin
-
activation of the ATM-associated enzyme by bleomycin, the free, non-ATM-associated, Tip60 activity is not activated by bleomycin
BRPF2
-
CDT1
-
licensing factor Cdt1 stabilizes HBO1 at origins. HBO1 directly interacts with Cdt1, and it enhances Cdt1-dependent rereplication
-
diethyl 2-pentadecylidenemalonate
-
compound induces hyperacetylation of specific lysine residues of histone H3, in particular residues K9 and K18, and raises the level of pan-acetylated H4
E2F1
the transcription factor associates with and recruits GCN5 to sites of DNA damage. E2F1 is required for the GCN5-mediated regulation of lung cancer cell growth and for theG1/S transition. Cyclin D1 and cyclin E1 are downstream targets of E2F1. GCN5 is enriched at the E2F1-binding site of the cyclin D1, cyclin E1, or E2F1 promoters
-
laminar shear stress
-
laminar shear stress stimulates acetylation of histones 3 and 4 at the region of the eNOS promoter SSRE and extends 3' toward the eNOS coding region. Laminar shear stress induces p300 binding to p65 and leads to increase of p300 histone acetyltransferase activity by 2.5fold and to increase of acetylation of p65, but not of p50 acetylation, overview
-
LoCAM
i.e. SPV106, 137% activation at 0.05 mM
membrane transporter
-
for acetyl-CoA and acetyltransferase from cytosol into lumen of the ER/ER Golgi intermediate compartment
-
TNF-alpha
-
additional information
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0086
3-azidopropionyl-CoA
pH and temperature not specified in the publication
0.0024
4-pentynoyl-CoA
pH and temperature not specified in the publication
0.0173
acetyl-CoA
pH and temperature not specified in the publication
0.24 - 0.7
histone H3
-
1.28 - 4.63
protein p53
-
0.0002 - 0.0082
3-azidopropionyl-CoA
0.0009
4-pentynoyl-CoA
mutant GCN5 T612G, pH and temperature not specified in the publication
0.0006
5-hexynoyl-CoA
mutant GCN5 T612G, pH and temperature not specified in the publication
0.0003
6-heptynoyl-CoA
mutant GCN5 T612G, pH and temperature not specified in the publication
0.00027 - 0.046
acetyl-CoA
0.039 - 0.56
histone H3
-
0.05
histone H3-peptide
-
PCAF catalytic domain
-
1.12
histone H3-peptide p19
-
PCAF catalytic domain
-
0.75
histone H3-peptide p27
-
PCAF catalytic domain
-
0.0000053 - 0.5
histone H4
0.0208 - 0.197
histone H4 peptide
-
0.0081
SGRGKGGKGLGKGGAKRHRK
at pH 8.0 and 30°C
additional information
additional information
-
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.233
3-azidopropionyl-CoA
pH and temperature not specified in the publication
0.0067
4-pentynoyl-CoA
pH and temperature not specified in the publication
0.567
acetyl-CoA
pH and temperature not specified in the publication
0.005 - 0.148
3-azidopropionyl-CoA
0.208
4-pentynoyl-CoA
mutant GCN5 T612G, pH and temperature not specified in the publication
0.24
5-hexynoyl-CoA
mutant GCN5 T612G, pH and temperature not specified in the publication
0.063
6-heptynoyl-CoA
mutant GCN5 T612G, pH and temperature not specified in the publication
0.0033 - 4.14
acetyl-CoA
0.18 - 0.22
histone H3
-
0.0117 - 0.0667
histone H3-peptide
-
0.131
histone H3-peptide p19
-
PCAF catalytic domain
-
0.00317 - 0.0583
histone H3-peptide p20
-
0.17
histone H3-peptide p27
-
PCAF catalytic domain
-
0.0018 - 0.0062
histone H4
0.15 - 4.28
histone H4 peptide
-
kcat/KM VALUE [1/mMs-1]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
27.09
3-azidopropionyl-CoA
pH and temperature not specified in the publication
2.79
4-pentynoyl-CoA
pH and temperature not specified in the publication
32.78
acetyl-CoA
pH and temperature not specified in the publication
2.73 - 9.73
histone H3
-
0.036 - 0.068
protein p53
-
0.61 - 740
3-azidopropionyl-CoA
231.11
4-pentynoyl-CoA
mutant GCN5 T612G, pH and temperature not specified in the publication
400
5-hexynoyl-CoA
mutant GCN5 T612G, pH and temperature not specified in the publication
210
6-heptynoyl-CoA
mutant GCN5 T612G, pH and temperature not specified in the publication
160.5 - 619
acetyl-CoA
1.41 - 205
histone H4 peptide
-
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0198
2,5-diphenylisothiazol-3(2H)-one
-
PCAF
0.019 - 0.028
2-(2-pyridyl)-isothiazol-3(2H)-one
0.0065 - 0.0144
2-(3-pyridyl)-isothiazol-3(2H)-one
0.0054
2-(4-dimethylaminoaniline)-isothiazol-3(2H)-one
-
PCAF
0.0075 - 0.0099
2-(4-morpholinoaniline)-isothiazol-3(2H)-one
0.0015 - 0.003
2-(4-pyridyl)-isothiazol-3(2H)-one
0.037
2-decyl-6-hydroxybenzoic acid
pH and temperature not specified in the publication
0.079
2-hydroxy-5-pentadecylbenzoic acid
pH and temperature not specified in the publication
0.157
2-hydroxy-6-(11-hydroxyundecyl)benzoic acid
pH and temperature not specified in the publication
0.064
2-hydroxy-6-pentadecylbenzoic acid
pH and temperature not specified in the publication
0.023 - 0.028
2-phenylisothiazol-3(2H)-one
0.0427
4-azidomethyl-2-phenyl-isothiazol-3(2H)-one
-
PCAF
0.102
4-methoxymethyl-2-phenyl-isothiazol-3(2H)-one
-
PCAF
0.032
4-methyl-2-phenylisothiazol-3(2H)-one
-
PCAF
0.2
4-methyl-5-methoxy-2-phenyl-isothiazol-3(2H)-one
-
above, PCAF
0.162
5-acetoxymethyl-2-phenylisothiazol-3(2H)-one
-
PCAF
0.058
5-azidomethyl-2-phenylisothiazol-3(2H)-one
-
PCAF
0.2
5-chloro-4-methyl-2-phenylisothiazol-3(2H)-one
-
above, PCAF
0.057
5-decyl-2-hydroxybenzoic acid
pH and temperature not specified in the publication
0.109
5-hydroxymethyl-2-phenylisothiazol-3(2H)-one
-
PCAF
0.2
5-methyl-2-phenylisothiazol-3(2H)-one
-
above, PCAF
0.2
5-phenylureidomethyl-2-phenylisothiazol-3(2H)-one
-
above, PCAF
0.0262
Ac-L-Lys(CoA)-NH2
at pH 8.0 and 30°C
0.00066
acetylated histone H3 peptide
-
PCAF catalytic domain
-
0.46
C646
pH and temperature not specified in the publication
0.0146
CoA
at pH 8.0 and 30°C
0.00044
coenzyme A
-
PCAF catalytic domain
0.0049
garcinol
-
0.0039
isogarcinol
-
0.0051
LTK14
-
0.00002
Lys-CoA
-
inhibition of peptide acetylation
0.0000011
[histone H4]-L-lysine12-CoA
at pH 8.0 and 30°C
-
0.0025
[histone H4]-L-lysine16-CoA
at pH 8.0 and 30°C
-
0.000022
[histone H4]-L-lysine5-CoA
at pH 8.0 and 30°C
-
0.00092
[histone H4]-L-lysine8-CoA
at pH 8.0 and 30°C
-
additional information
additional information
-
-
-
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0023
(2E,6E)-2,6-bis[(3,5-dibromo-4-hydroxyphenyl)methylidene]cyclohexan-1-one
Homo sapiens
at pH 8.0 and 30°C
0.0389
(2E,6E)-2,6-bis[(3-fluoro-4-hydroxyphenyl)methylidene]cyclohexan-1-one
Homo sapiens
at pH 8.0 and 30°C
0.0268
(2E,6E)-2,6-bis[(4-hydroxy-3-methylphenyl)methylidene]cyclohexan-1-one
Homo sapiens
at pH 8.0 and 30°C
0.035
(3Z,5Z)-3,5-bis[(3-bromo-4-hydroxyphenyl)methylidene]thian-4-one
Homo sapiens
at pH 8.0 and 30°C
0.00047
(4-(4-((5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl)methylene)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)phenyl)phosphonic acid
Homo sapiens
at pH 8.0 and 25°C
0.32
(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
pH and temperature not specified in the publication
0.0309
2,6-bis(3-bromo-4-hydroxybenzylidene)cyclohexanone
Homo sapiens
at pH 8.0 and 30°C
0.0455
2,6-bis(3-chloro-4-hydroxybenzylidene)cyclohexan-1-one
Homo sapiens
at pH 8.0 and 30°C
0.0081
2,6-bis(4-hydroxy-3-iodobenzylidene)cyclohexan-1-one
Homo sapiens
at pH 8.0 and 30°C
0.00731
2-(3,5-difluoro-4-hydroxyphenyl)-4-((5-(4,5-dimethyl-2-(trifluoromethyl)phenyl)furan-2-yl)methylene)-5-methyl-2,4-dihydro-3H-pyrazol-3-one
Homo sapiens
at pH 8.0 and 25°C
0.0048
2-(3,5-difluoro-4-hydroxyphenyl)-4-((5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl)methylene)-5-methyl-2,4-dihydro-3H-pyrazol-3-one
Homo sapiens
at pH 8.0 and 25°C
0.01
2-(3,5-difluoro-4-hydroxyphenyl)-5-methyl-4-((5-(2-(trifluoromethoxy)phenyl)furan-2-yl)methylene)-2,4-dihydro-3H-pyrazol-3-one
Homo sapiens
IC50 above 0.01 mM, at pH 8.0 and 25°C
0.00373 - 0.00605
2-(3,5-difluoro-4-hydroxyphenyl)-5-methyl-4-((5-(3-oxo-2,3-dihydro-1H-inden-4-yl)furan-2-yl)methylene)-2,4-dihydro-3H-pyrazol-3-one
0.00067
2-(4-(2H-tetrazol-5-yl)phenyl)-4-((5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl)methylene)-5-methyl-2,4-dihydro-3H-pyrazol-3-one
Homo sapiens
at pH 8.0 and 25°C
0.00406
4-((5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl)methylene)-5-methyl-2-(4-(methylsulfonyl)phenyl)-2,4-dihydro-3H-pyrazol-3-one
Homo sapiens
at pH 8.0 and 25°C
0.00016
4-(3-cyclopropyl-4-((5-(4,5-dimethyl-2-(trifluoromethyl)phenyl)thiophen- 2-yl)methylene)-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
Homo sapiens
at pH 8.0 and 25°C
0.0002
4-(3-cyclopropyl-4-((5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl)methylene)-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
Homo sapiens
at pH 8.0 and 25°C
0.00056
4-(3-methyl-4-((5-(2-nitrophenyl)furan-2-yl)methylene)-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
Homo sapiens
at pH 8.0 and 25°C
0.00113
4-(3-methyl-5-oxo-4-((5-(2-(trifluoromethoxy)phenyl)furan-2-yl)methylene)-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
Homo sapiens
at pH 8.0 and 25°C
0.00058
4-(3-methyl-5-oxo-4-((5-(3-oxo-2,3-dihydro-1H-inden-4-yl)furan-2-yl)methylene)-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
Homo sapiens
at pH 8.0 and 25°C
0.00086
4-(4-((2-(4,5-dimethyl-2-nitrophenyl)thiazol-5-yl)methylene)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
Homo sapiens
at pH 8.0 and 25°C
0.00117
4-(4-((5-(2-(difluoromethyl)phenyl)furan-2-yl)methylene)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
Homo sapiens
at pH 8.0 and 25°C
0.01
4-(4-((5-(2-(dimethylphosphoryl)phenyl)furan-2-yl)methylene)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
Homo sapiens
IC50 above 0.01 mM, at pH 8.0 and 25°C
0.00029
4-(4-((5-(4,5-dimethyl-2-(trifluoromethyl)phenyl)furan-2-yl)methylene)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
Homo sapiens
at pH 8.0 and 25°C
0.00195
4-(4-((5-(4,5-dimethyl-2-nitrophenyl)-1H-pyrrol-2-yl)methylene)-3-methyl-5-oxo-4, 5-dihydro-1H-pyrazol-1-yl)benzoic acid
Homo sapiens
at pH 8.0 and 25°C
0.01
4-(4-((5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl)methylene)-2,5-dioxoimidazolidin-1-yl)benzoic acid
Homo sapiens
IC50 above 0.01 mM, at pH 8.0 and 25°C
0.00019
4-(4-((5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl)methylene)-3-ethyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
Homo sapiens
at pH 8.0 and 25°C
0.00023
4-(4-((5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl)methylene)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
Homo sapiens
at pH 8.0 and 37°C
0.00153
4-(4-((5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl)methylene)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzonitrile
Homo sapiens
at pH 8.0 and 25°C
0.00023
4-(4-((5-(4,5-dimethyl-2-nitrophenyl)thiophen-2-yl)methylene)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
Homo sapiens
at pH 8.0 and 25°C
0.00207
4-(4-(1-(5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl)ethylidene)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
Homo sapiens
at pH 8.0 and 25°C
0.00961
4-(4-(2-((4,5-dimethyl-2-nitrophenyl)amino)-2-oxoethyl)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
Homo sapiens
at pH 8.0 and 25°C
0.01
4-(4-(3-((4,5-dimethyl-2-nitrophenyl)amino)-3-oxopropyl)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid
Homo sapiens
IC50 above 0.01 mM, at pH 8.0 and 25°C
0.01
4-(5-((5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl)methylene)-2,4- dioxothiazolidin-3-yl)benzoic acid
Homo sapiens
IC50 above 0.01 mM, at pH 8.0 and 25°C
0.01
4-(5-(4,5-dimethyl-2-nitrobenzoyl)-1H-indazol-1-yl)benzoic acid
Homo sapiens
IC50 above 0.01 mM, at pH 8.0 and 25°C
0.01
4-(5-(4,5-dimethyl-2-nitrobenzoyl)-1H-indol-1-yl)benzoic acid
Homo sapiens
IC50 above 0.01 mM, at pH 8.0 and 25°C
0.01
4-(5-(4,5-dimethyl-2-nitrobenzyl)-1H-indazol-1-yl)benzoic acid
Homo sapiens
IC50 above 0.01 mM, at pH 8.0 and 25°C
0.00713
4-([(2E)-2-cyano-3-[5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl]prop-2-enoyl]amino)benzoic acid
Homo sapiens
at pH 8.0 and 25°C
0.0141
4-[(4Z)-4-[[5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl]methylidene]-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl]-N-(prop-2-yn-1-yl)benzamide
Homo sapiens
pH and temperature not specified in the publication
0.0068
4-[(4Z)-4-[[5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl]methylidene]-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl]benzoic acid
Homo sapiens
pH and temperature not specified in the publication
0.0077
(E)-4-(2-(5,6-dimethylbenzo[d]thiazol-2-yl)vinyl)-N,N-diethylbenzenesulfonamide
Homo sapiens
at pH 7.5 and 25°C
0.03
(E)-4-(2-(5-bromobenzo[d]thiazol-2-yl)vinyl)-N,N-diethylbenzenesulfonamide
Homo sapiens
at pH 7.5 and 25°C
0.03
(E)-4-(2-(5-chlorobenzo[d]thiazol-2-yl)vinyl)-N,N-diethylbenzenesulfonamide
Homo sapiens
at pH 7.5 and 25°C
0.006
(E)-4-(2-(benzo[d]thiazol-2-yl)vinyl)-N,N-diethylbenzenesulfonamide
Homo sapiens
at pH 7.5 and 25°C
0.04
(E)-N,N-diethyl-4-(2-(5-fluorobenzo[d]thiazol-2-yl)vinyl)benzenesulfonamide
Homo sapiens
at pH 7.5 and 25°C
0.005
1,7-bis(3-bromo-4-hydroxyphenyl)-1,6-heptadiene-3,5-dione
Homo sapiens
-
-
0.00023
2,3-difluoro-N'-(3-methyl-5-(1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00018
2,4-difluoro-N'-(3-methyl-5-(1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.033
2,6-bis(3-bromo-4-hydroxybenzylidene)cyclohexanone
Homo sapiens
-
-
0.00018
2,6-difluoro-N'-(3-methyl-5-(1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.0024
2-(3-fluoro-5-(2-((2-fluorophenyl)sulfonyl)hydrazinecarbonyl)-phenyl)pyridine 1-Oxide
Homo sapiens
pH and temperature not specified in the publication
0.00503
2-(3-methoxyphenyl)isothiazolo[5,4-b]pyridin-3(2H)-one
Homo sapiens
-
substrate histone H3 peptide, pH 7.5, 30°C
0.0255 - 0.13
2-(4-(trifluoromethyl)benzyl)isothiazolo[5,4-b]pyridin-3(2H)-one
0.00072 - 0.00164
2-(4-fluorophenyl)isothiazolo[5,4-b]pyridin-3(2H)-one
0.00463
2-(4-methylphenyl)isothiazolo[5,4-b]pyridin-3(2H)-one
Homo sapiens
-
substrate histone H3 peptide, pH 7.5, 30°C
0.00053
2-fluoro-3-hydroxy-N'-(3-methyl-5-(1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00039
2-fluoro-3-methyl-N'-(3-methyl-5-(1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00012
2-fluoro-4-methyl-N'-(3-methyl-5-(1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00023
2-fluoro-5-hydroxy-N'-(3-methyl-5-(1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000073
2-fluoro-5-methoxy-N'-(3-methyl-5-(1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000096
2-fluoro-5-methyl-N'-(3-methyl-5-(1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00011
2-fluoro-6-methoxy-N'-(3-methyl-5-(1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000062
2-fluoro-N'-(2-fluoro-5-methyl-3-(1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000044
2-fluoro-N'-(2-fluoro-5-methyl-3-(pyridin-2-yl)benzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00169
2-fluoro-N'-(2-phenylisonicotinoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000018
2-fluoro-N'-(3-(3-methyl-1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000029
2-fluoro-N'-(3-(4-fluoro-1H-pyrazol-1-yl)-5-methylbenzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00034
2-fluoro-N'-(3-(4-fluoro-1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.0003
2-fluoro-N'-(3-(4-methyl-1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00002
2-fluoro-N'-(3-(furan-2-yl)benzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000006
2-fluoro-N'-(3-(pyridin-2-yl)benzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000025
2-fluoro-N'-(3-(thiophen-2-yl)benzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000014
2-fluoro-N'-(3-(thiophen-3-yl)benzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00027
2-fluoro-N'-(3-fluoro-5-(1H-pyrazol-1-yl)benzoyl)-3-methoxybenzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00035
2-fluoro-N'-(3-fluoro-5-(1H-pyrazol-1-yl)benzoyl)-4-methoxybenzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000026
2-fluoro-N'-(3-fluoro-5-(1H-pyrazol-1-yl)benzoyl)-5-hydroxybenzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.0001
2-fluoro-N'-(3-fluoro-5-(1H-pyrazol-1-yl)benzoyl)-5-methoxybenzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000009
2-fluoro-N'-(3-fluoro-5-(2H-1,2,3-triazol-2-yl)benzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000023
2-fluoro-N'-(3-fluoro-5-(3-methyl-1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000032
2-fluoro-N'-(3-fluoro-5-(4-methyl-1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000031
2-fluoro-N'-(3-fluoro-5-(5-methyl-1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00027
2-fluoro-N'-(3-fluoro-5-(pyridin-2-yl)benzoyl)-3-hydroxybenzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.0000063
2-fluoro-N'-(3-fluoro-5-(pyridin-2-yl)benzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00006
2-fluoro-N'-(3-iodobenzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000017 - 0.08
2-fluoro-N'-(3-isobutoxybenzoyl)benzenesulfonohydrazide
0.059
2-fluoro-N'-(3-isopropoxybenzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00097
2-fluoro-N'-(3-isopropylbenzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000013
2-fluoro-N'-(3-methoxy-5-(1H-pyrazol-1-yl)benzoyl)-benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000203
2-fluoro-N'-(3-methoxy-5-(3-methyl-1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000024
2-fluoro-N'-(3-methoxy-5-(pyrimidin-2-yl)benzoyl)-benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000027
2-fluoro-N'-(3-methyl-5-(1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000018
2-fluoro-N'-(3-methyl-5-(2H-1,2,3-triazol-2-yl)benzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000007
2-fluoro-N'-(3-methyl-5-(3-methyl-1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000014
2-fluoro-N'-(3-methyl-5-(4-methyl-1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000013
2-fluoro-N'-(3-methyl-5-(5-methyl-1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00038
2-fluoro-N'-(3-methylbenzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.094
2-fluoro-N'-(3-propoxybenzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000094
2-fluoro-N'-(3-propylbenzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00235
2-fluoro-N'-(5-phenylnicotinoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.0029
2-fluoro-N'-(6-phenylpicolinoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.001
2-fluoro-N'-(naphthalene-2-sulfonyl)benzohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.01
2-tert-butyl-5-(dodecylthio)isothiazol-3(2H)-one-1-oxide
Homo sapiens
-
above
0.01
2-tert-butyl-5-chloroisothiazol-3(2H)-one 1-oxide
Homo sapiens
-
above
0.015
2-[2-(4-heptylphenyl)ethyl]-6-hydroxybenzoic acid
Homo sapiens
at pH 7.5 and 25°C
0.0036
3-bromo-N'-(3-ethoxybenzoyl)-2-fluorobenzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000023
3-fluoro-N'-(2-fluorobenzene-1-sulfonyl)-5-(1H-pyrazol-1-yl)benzohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.0000094
3-fluoro-N'-(2-fluorobenzene-1-sulfonyl)-5-(furan-2-yl)benzohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000014
3-fluoro-N'-(2-fluorobenzene-1-sulfonyl)-5-(pyrimidin-2-yl)benzohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.0024
4,5-dichloro-2-ethylisothiazol-3(2H)-one
Homo sapiens
-
-
0.01
4,5-dichloro-2-ethylisothiazol-3(2H)-one-1-oxide
Homo sapiens
-
above
0.0097
4-amino-1-naphthol
Homo sapiens
pH and temperature not specified in the publication
0.00053
5-bromo-N'-(3-ethoxybenzoyl)-2-fluorobenzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.01
5-chloro-2-ethyl-4-methylisothiazol-3(2H)-one
Homo sapiens
-
above
0.01
5-chloro-2-ethyl-4-methylisothiazol-3(2H)-one-1-oxide
Homo sapiens
-
above
0.003
5-chloro-2-ethylisothiazol-3(2H)-one
Homo sapiens
-
-
0.01
5-chloro-2-ethylisothiazol-3(2H)-one-1-oxide
Homo sapiens
-
above
0.0000026 - 0.0000098
A-485
0.0749
Ac-L-Lys(CoA)-NH2
Homo sapiens
at pH 8.0 and 30°C
0.043 - 0.348
anacardic acid
Homo sapiens
pH and temperature not specified in the publication
0.0016
C646
Homo sapiens
pH and temperature not specified in the publication
0.0022 - 0.0073
CCT077791
Homo sapiens
-
IC50: 0.0022-0.0073 mM, in vivo cell proliferation inhibition, reduces acetylation of histones H3 and H4 and alpha-tubulin in cancer cell lines
0.0027 - 0.015
CCT077792
Homo sapiens
-
IC50: 0.0027-0.015 mM, in vivo cell proliferation inhibition
0.0187 - 0.0202
CCT077796
Homo sapiens
-
IC50: 0.0187-0.0202 mM, in vivo cell proliferation inhibition
0.0547
CCT079769
Homo sapiens
-
IC50: 0.0547 mM, in vivo cell proliferation inhibition
0.0415
CoA
Homo sapiens
at pH 8.0 and 30°C
0.025 - 0.4
curcumin
0.0072
embelin
Homo sapiens
pH and temperature not specified in the publication
0.0011 - 0.0029
EML425
0.03 - 0.07
epigallocatechin-3-gallate
0.0575
ethyl 2-methyl-6-([5-[(prop-2-yn-1-yl)amino]pentyl]oxy)quinoline-3-carboxylate
Homo sapiens
pH and temperature not specified in the publication
0.005 - 0.007
garcinol
0.034 - 0.064
H3-CoA-20
Homo sapiens
-
IC50: 0.034-0.064 mM
0.012
H3-CoA-20-Tat
Homo sapiens
-
IC50: 0.012 mM, recombinant enzyme
-
0.002 - 0.128
L002
0.0001 - 0.2
Lys-CoA
0.00025
Lys-CoA-Tat
Homo sapiens
-
IC50: 250 nM, recombinant enzyme, complete inhibition of acetylation of the promyelotic leukemia zinc finger gene
0.1
MB-3
Homo sapiens
pH and temperature not specified in the publication
0.01
methyl 3-(4,5-dichloro-1-oxido-3-oxoisothiazol-2(3H)-yl)propanoate
Homo sapiens
-
above
0.0026
methyl 3-(4,5-dichloro-3-oxoisothiazol-2(3H)-yl)propanoate
Homo sapiens
-
-
0.0056
methyl 3-(5-chloro-1-oxido-3-oxoisothiazol-2(3H)-yl)propanoate
Homo sapiens
-
-
0.0018
methyl 3-(5-chloro-3-oxoisothiazol-2(3H)-yl)propanoate
Homo sapiens
-
-
0.01
methyl 3-(5-chloro-4-methyl-1-oxido-3-oxoisothiazol-2(3H)-yl)propanoate
Homo sapiens
-
above
0.01
methyl 3-(5-chloro-4-methyl-3-oxoisothiazol-2(3H)-yl)propanoate
Homo sapiens
-
above
0.01
methyl 3-[4-chloro-5-(dodecylthio)-1-oxido-3-oxoisothiazol-2(3H)-yl]propanoate
Homo sapiens
-
above
0.01
methyl 3-[5-(dodecylthio)-1-oxido-3-oxoisothiazol-2(3H)-yl] propanoate
Homo sapiens
-
above
0.000072
N'-(2,6-difluorobenzene-1-sulfonyl)-3-fluoro-5-propoxybenzohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000061
N'-(2,6-difluorobenzene-1-sulfonyl)-3-fluoro-5-[(propan-2-yl)oxy]benzohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00011
N'-(2,6-difluorobenzene-1-sulfonyl)-3-methoxy-5-[(propan-2-yl)oxy]benzohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000015
N'-(2,6-difluorobenzene-1-sulfonyl)-3-methyl-5-[(propan-2-yl)oxy]benzohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000017
N'-(2-fluoro-3-methyl-5-((2-methylallyl)oxy)benzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000078
N'-(2-fluoro-3-methyl-5-(1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000096
N'-(2-fluoro-3-methyl-5-(2H-1,2,3-triazol-2-yl)benzoyl)-naphthalene-2-sulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000065
N'-(2-fluoro-3-methyl-5-(3-methyl-1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000084
N'-(2-fluoro-3-methyl-5-(4-methyl-1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000087
N'-(2-fluoro-3-methyl-5-(5-methyl-1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00014
N'-(2-fluoro-5-(1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00034
N'-(2-fluoro-5-(2H-1,2,3-triazol-2-yl)benzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00016
N'-(2-fluoro-5-(3-methyl-1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000052
N'-(2-fluoro-5-(4-fluoro-1H-pyrazol-1-yl)-3-methylbenzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00022
N'-(2-fluoro-5-(4-methyl-1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00008
N'-(2-fluoro-5-(furan-2-yl)-3-methylbenzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00012
N'-(2-fluoro-5-(furan-2-yl)benzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00009
N'-(2-fluoro-5-(pyridin-2-yl)benzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000063
N'-(2-fluoro-5-isopropoxy-3-methylbenzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000062
N'-(2-fluoro-5-isopropoxybenzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000081
N'-(2-fluoro-5-propoxybenzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00011
N'-(2-fluorobenzene-1-sulfonyl)-3-(furan-2-yl)-5-methoxybenzohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000011
N'-(2-fluorobenzene-1-sulfonyl)-3-(furan-2-yl)-5-methylbenzohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00023
N'-(2-fluorobenzene-1-sulfonyl)-3-(naphthalen-2-yl)benzohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000054
N'-(2-fluorobenzene-1-sulfonyl)-3-(pyrimidin-2-yl)benzohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.0019
N'-(2-fluorobenzene-1-sulfonyl)-3-(pyrimidin-4-yl)benzohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.56
N'-(2-fluorobenzene-1-sulfonyl)-3-(trifluoromethoxy)benzohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000005
N'-(2-fluorobenzene-1-sulfonyl)-3-methoxy-5-(pyridin-2-yl)benzohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000008
N'-(2-fluorobenzene-1-sulfonyl)-3-methyl-5-(pyridin-2-yl)benzohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000009
N'-(2-fluorobenzene-1-sulfonyl)-3-methyl-5-(pyrimidin-2-yl)benzohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.8
N'-(2-fluorobenzene-1-sulfonyl)benzohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00049
N'-(3-(1,2,4-oxadiazol-3-yl)benzoyl)-2-fluorobenzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00463
N'-(3-(1,3,4-oxadiazol-2-yl)benzoyl)-2-fluorobenzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000043
N'-(3-(1H-pyrazol-1-yl)benzoyl)-2-fluorobenzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00061
N'-(3-(1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00018
N'-(3-(3,5-dimethyl-1H-pyrazol-1-yl)benzoyl)-2-fluorobenzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.0006
N'-(3-(4-fluoro-1H-pyrazol-1-yl)-5-methylbenzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00002
N'-(3-(allyloxy)-5-fluorobenzoyl)-2-fluorobenzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000016
N'-(3-(allyloxy)-5-methylbenzoyl)-2-fluorobenzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.03
N'-(3-(allyloxy)benzoyl)-2-fluorobenzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.23
N'-(3-(cyclopentyloxy)benzoyl)-2-fluorobenzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00044
N'-(3-(cyclopentyloxy)benzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000091 - 0.00011
N'-(3-(cyclopropylmethoxy)-5-fluorobenzoyl)-2-fluorobenzenesulfonohydrazide
0.00009
N'-(3-(cyclopropylmethoxy)-5-methylbenzoyl)-2-fluorobenzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.12
N'-(3-(cyclopropylmethoxy)benzoyl)-2-fluorobenzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000024
N'-(3-(ethoxymethyl)-5-methylbenzoyl)-2-fluorobenzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00048
N'-(3-(furan-2-yl)-5-methoxybenzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00013
N'-(3-(furan-2-yl)-5-methylbenzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00014
N'-(3-(pyridin-2-yl)benzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00063
N'-(3-(pyrimidin-2-yl)benzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.125
N'-(3-(pyrimidin-5-yl)benzoyl)benzenesulfonohydrazide
Homo sapiens
above, pH and temperature not specified in the publication
0.00016
N'-(3-(thiazol-2-yl)benzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00027
N'-(3-(thiazol-4-yl)benzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.01
N'-(3-(trifluoromethoxy)benzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.011
N'-(3-(trifluoromethyl)benzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00018
N'-(3-bromobenzoyl)-2-fluorobenzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.23
N'-(3-butoxybenzoyl)-2-fluorobenzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.003
N'-(3-butoxybenzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.0000055
N'-(3-chloro-5-(furan-2-yl)benzoyl)-2-fluorobenzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00011
N'-(3-chloro-5-(furan-2-yl)benzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000024
N'-(3-chloro-5-(thiophen-2-yl)benzoyl)-2-fluorobenzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000027
N'-(3-cyclopropoxy-5-methylbenzoyl)-2-fluorobenzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00011
N'-(3-ethoxy-5-fluorobenzoyl)-2-fluorobenzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00016
N'-(3-ethoxy-5-methoxybenzoyl)-2-fluorobenzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00017
N'-(3-ethoxy-5-methylbenzoyl)-2,3-difluorobenzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00013
N'-(3-ethoxy-5-methylbenzoyl)-2,4-difluorobenzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00017
N'-(3-ethoxy-5-methylbenzoyl)-2,5-difluorobenzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00013
N'-(3-ethoxy-5-methylbenzoyl)-2,6-difluorobenzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00016
N'-(3-ethoxy-5-methylbenzoyl)-2-fluoro-3-methylbenzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00018
N'-(3-ethoxy-5-methylbenzoyl)-2-fluoro-4-methylbenzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00012
N'-(3-ethoxy-5-methylbenzoyl)-2-fluoro-5-methylbenzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000016
N'-(3-ethoxy-5-methylbenzoyl)-2-fluorobenzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00027
N'-(3-ethoxybenzoyl)-2-fluoro-5-methoxybenzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.005
N'-(3-ethoxybenzoyl)-2-fluoro-6-methoxybenzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.069
N'-(3-ethoxybenzoyl)-2-fluorobenzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00037
N'-(3-ethoxybenzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00057
N'-(3-ethoxybenzoyl)naphthalene-2-sulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00022
N'-(3-ethylbenzoyl)-2-fluorobenzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.0036
N'-(3-ethylbenzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00044
N'-(3-fluoro-5-(1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00043
N'-(3-fluoro-5-(3-methyl-1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.0008
N'-(3-fluoro-5-(4-methyl-1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00014
N'-(3-fluoro-5-(furan-2-yl)benzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.0001
N'-(3-fluoro-5-(pyridin-2-yl)benzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.0004
N'-(3-fluoro-5-propoxybenzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00024
N'-(3-isobutoxybenzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00033
N'-(3-isopropoxybenzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.0062
N'-(3-isopropylbenzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.0012
N'-(3-methoxy-5-(1H-pyrazol-1-yl)benzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00039
N'-(3-methoxy-5-(pyridin-2-yl)benzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00069
N'-(3-methoxybenzoyl)naphthalene-2-sulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.0023
N'-(3-methylbenzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.0047
N'-(3-phenoxybenzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00038
N'-(3-propoxybenzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00012
N'-(3-propoxybenzoyl)naphthalene-2-sulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.0033
N'-(3-propylbenzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000061
N'-(5-(allyloxy)-2-fluoro-3-methylbenzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00007
N'-(5-(allyloxy)-2-fluorobenzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000054
N'-(5-(cyclopropylmethoxy)-2-fluoro-3-methylbenzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000029
N'-(5-(ethoxymethyl)-2-fluoro-3-methylbenzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000074
N'-(5-ethoxy-2-fluoro-3-methylbenzoyl)-2-fluorobenzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000082
N'-(5-ethoxy-2-fluoro-3-methylbenzoyl)naphthalene-2-sulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00019
N'-(5-ethoxy-2-fluorobenzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000073
N'-(benzenesulfonyl)-2-fluoro-3-methyl-5-(pyridin-2-yl)benzohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000067
N'-(benzenesulfonyl)-2-fluoro-3-methyl-5-(pyrimidin-2-yl)benzohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00014
N'-(benzenesulfonyl)-2-fluoro-5-(pyrimidin-2-yl)benzohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.125
N'-(benzenesulfonyl)-2-fluoro-5-(pyrimidin-4-yl)benzohydrazide
Homo sapiens
above, pH and temperature not specified in the publication
0.00012
N'-(benzenesulfonyl)-2-fluoro-5-[(prop-2-yn-1-yl)oxy]benzohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00045
N'-(benzenesulfonyl)-3-fluoro-5-(pyrimidin-2-yl)benzohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.0072
N'-(benzenesulfonyl)-3-fluorobenzohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00067
N'-(benzenesulfonyl)-3-methoxy-5-(pyrimidin-2-yl)benzohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.0023
N'-(benzenesulfonyl)-3-methoxybenzohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00023
N'-(benzenesulfonyl)-3-methyl-5-(pyrimidin-2-yl)benzohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000062
N'-(ethoxy-2-fluoro-3-methylbenzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.0042
N'-(naphthalene-2-sulfonyl)benzohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.00014
N'-([1,1'-biphenyl]-3-carbonyl)-2-fluorobenzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000038
N-(2-fluoro-3-methyl-5-(2H-1,2,3-triazol-2-yl)benzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.000052
N-(2-fluoro-3-methyl-5-propoxybenzoyl)benzenesulfonohydrazide
Homo sapiens
pH and temperature not specified in the publication
0.0041
N-[5-[(5-[[5-([4-[(5-[[5-([5-[(5-[[3-(dimethylamino)propyl]carbamoyl]-1-methyl-1H-pyrrol-3-yl)carbamoyl]-1-methyl-1H-pyrrol-3-yl]carbamoyl)-1-methyl-1H-pyrrol-3-yl]carbamoyl]-1-methyl-1H-pyrrol-3-yl)amino]-4-oxobutyl]carbamoyl)-1-methyl-1H-pyrrol-3-yl]carbamoyl]-1-methyl-1H-pyrrol-3-yl)carbamoyl]-1-methyl-1H-pyrrol-3-yl]-4-[(N-[[2-(2-[4-[(4Z)-4-[[5-(2,3-dimethyl-6-nitrophenyl)furan-2-yl]methylidene]-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl]benzamido]ethoxy)ethoxy]acetyl]-beta-alanyl)amino]-1-methyl-1H-pyrrole-2-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000011
NK13650A
Homo sapiens
pH and temperature not specified in the publication
0.000022
NK13650B
Homo sapiens
pH and temperature not specified in the publication
0.002
NU9056
Homo sapiens
pH and temperature not specified in the publication
0.00007
peptide conjugate Boc-C5-CoA
Homo sapiens
pH and temperature not specified in the publication
-
0.0003
peptide conjugate H3-CoA-20
Homo sapiens
pH and temperature not specified in the publication
-
0.00662 - 0.01759
peptide conjugate H4-K16-CoA
-
0.002 - 0.02
Plumbagin
0.0016 - 0.00974
PU139
0.000023
[histone H4]-L-lysine12-CoA
Homo sapiens
at pH 8.0 and 30°C
-
0.0072
[histone H4]-L-lysine16-CoA
Homo sapiens
at pH 8.0 and 30°C
-
0.000083
[histone H4]-L-lysine5-CoA
Homo sapiens
at pH 8.0 and 30°C
-
0.0026
[histone H4]-L-lysine8-CoA
Homo sapiens
at pH 8.0 and 30°C
-
additional information
additional information
-
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
additional information
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
7.6
-
assay at
7.9
assay at
additional information
-
reaction kinetic is pH-dependent
pH RANGE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
6 - 9.5
-
PCAF protein
8 - 9
activity range, inactive below
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
22 - 37
-
assay at
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
high expression öevel of CBP/p300 in hepatocarcinoma tissue
Manually annotated by BRENDA team
-
HBO1
Manually annotated by BRENDA team
-
from brain tumor
Manually annotated by BRENDA team
high expression öevel of CBP/p300 in hepatocarcinoma tissue
Manually annotated by BRENDA team
-
P300/CBP-associated factor expression level analysis
Manually annotated by BRENDA team
-
colon tumor cell line
Manually annotated by BRENDA team
-
human embryonic kidney A293 cells
Manually annotated by BRENDA team
-
from neuronal tissue
Manually annotated by BRENDA team
-
neuroblastoma
Manually annotated by BRENDA team
in immune-related disease, HBO1 is upregulated in synovial fibroblasts, which are the key pathogenic factors contributing to the development and progression of rheumatoid arthritis
Manually annotated by BRENDA team
additional information
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY hide
GeneOntology No.
LITERATURE
SOURCE
-
catalytic site facing the lumen of the endoplasmic reticulum/endoplasmic reticulum Goli intermediate compartment (ER/ERGIC)
Manually annotated by BRENDA team
-
catalytic site facing the lumen of the endoplasmic reticulum/endoplasmic reticulum Goli intermediate compartment (ER/ERGIC)
Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
evolution
malfunction
enzyme inhibition significantly augments TRAIL-induced apoptotic sensitivity, which is accompanied by reduced levels of survivin, in Hep-G2, HLE and SK-HEP1 cells. Enzyme inhibition significantly decreases invasion of Huh7, HLE and SK-HEP1 cells. The level of matrix metallopeptidase 15 (MMP15) mRNA expression is significantly reduced, whereas the level of laminin alpha 3 (LAMA3) and secreted phosphoprotein 1 (SPP1) mRNA expression is significantly increased in Huh7 cells following exposure to enzyme inhibitor C646
physiological function
evolution
malfunction
metabolism
physiological function
additional information
UNIPROT
ENTRY NAME
ORGANISM
NO. OF AA
NO. OF TRANSM. HELICES
MOLECULAR WEIGHT[Da]
SOURCE
SEQUENCE
LOCALIZATION PREDICTION?
EP300_HUMAN
2414
0
264161
Swiss-Prot
other Location (Reliability: 2)
PDB
SCOP
CATH
UNIPROT
ORGANISM
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
20000
-
SDS-PAGE, rough estimation from figure
28000
-
SDS-PAGE
additional information
SUBUNIT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
monomer
active form
additional information
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
acetylation
phosphoprotein
additional information
CRYSTALLIZATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
in complex with acetyl coenzyme A and histone H4 peptide, i.e. residues 1-20, to 1.9 A resolution. The cofactor and the side chain of lysine 12 of histone H4 peptide are placed in the canyon between the central and C-terminal domains. Histone H4 peptide adopts a well-defined conformation and establishes an extensive set of interactions with the enzyme including invariant residues Glu64 and Trp199, which together govern substrate-binding specificity. There is a cumulative effect of the active-site residues Glu187, Glu276, and Asp277 on deprotonation of the epsilon-amino group of reactive Lys12 for direct attack of the acetyl group of the cofactor
in complex with BRPF2, sitting drop vapor diffusion method, using 2% (w/v) tacsimate (pH 8.0), 0.1 M Tris-HCl (pH 8.5) and 12% (w/v) polyethylene glycol 3350
modeling of the initial complex between acetyltransferase Gcn5, acetyl-CoA and histone H3 and 20 ns molecular dynamics simulation. Glu80 acts as the general base for deprotonation of residue Lys171 from H3. Glu80, water180 and Lys171 form a proton-wire for the deprotonation process of Lys171. Both loop alpha7-beta7 and loop alpha1-alpha2 play a critical role in binding substrate H3
the X-ray crystal structures of yeast Esa1 (yEsa1/KAT5) bound to a bisubstrate H4K16CoA inhibitor and human MOF (hMOF/KAT8/MYST1) reveal that they are autoacetylated at a strictly conserved lysine residue in MYST proteins
-
visualization of multifunctional transcription activator p300 by atomic force microscopy. p300 is almost prolate ellipsoidal in shape, having several bulges. The functionally significant N-terminal and C-terminal regions are located near one end and centre of the molecule, respectively. The presence of N- and C-terminal regions near the central portion of the prolate ellipsoid suggests that all four domain could exist spatially close near the central portion of the molecule and hence capable of binding all four domains simultaneously. The complex between p300 and tumor suppressor protein p53 is elongated in shape. p53 binds at the central region of p300
-
PROTEIN VARIANTS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
C746A
-
site-directed mutagenesis, mutation in the HAT domain, leads to only slightly reduced catalytic activity, but highly reduced cyclin D1 transcription in the cells
D277N
strong decrease in catalytic efficiency
D551G/V582A/D639E
-
random and site-directed mutagenesis
D62A
4fold increase in Km value
D639V
-
random mutagenesis
E187Q
strong decrease in catalytic efficiency
E276Q
strong decrease in catalytic efficiency
E611K
-
random mutagenesis
E649D
-
random mutagenesis
E64A
6fold increase in Km value
E742Q
-
site-directed mutagenesis, mutation in the HAT domain, leads to only slightly reduced catalytic activity, but highly reduced cyclin D1 transcription in the cells
F605L
-
random mutagenesis
G485
-
a HBO1 mutant, which contains a mutation of an invariant glycine in the histone acetyltransferase domain that abolishes enzymatic activity
G923/925D
-
site-directed mutagenesis, mutation in the HAT domain, leads to only slightly reduced catalytic activity, but highly reduced cyclin D1 transcription in the cells
H524Q
-
random mutagenesis
H592R
-
random mutagenesis
H600R
-
random mutagenesis
I511T/M529I
-
random and site-directed mutagenesis
K1358A
-
site directed mutagenesis of lysine 1358 of the p300 acetyltransferase domain reveals that inhibitor binds via a hydrogen bond to this lysine residue in the wild-type, in the mutant no binding leads to total loss of acetyltransferase activity
K136R
K274R
-
mutant is catalytically inactive
K542E/D601G/Y612C
-
random and site-directed mutagenesis
K542E/D639E
-
random and site-directed mutagenesis
K627R/D639E
-
random and site-directed mutagenesis
L503P/D601G
-
random and site-directed mutagenesis
L503P/D601G/Y612C
-
random and site-directed mutagenesis
N504I/Q519L/V572A/V582A
-
random and site-directed mutagenesis
P655R
-
random mutagenesis
Q519R
-
random mutagenesis
R82A/Y122F
S1834A
-
site-directed mutagenesis, the mutant shows no histone acetylation and ICAM-1 gene expression, overview
S1834E
-
site-directed mutagenesis, the mutant shows no histone acetylation and ICAM-1 gene expression, overview
T535A/D551G
-
random and site-directed mutagenesis
T612G
site-directed mutagenesis, the mutant is able to activate a series of alkynyl and azido acyl-CoA for histone acylation. Residue Thr612 is conserved in the PCAF/GCN5 family
V582A
-
random mutagenesis
V582A/D639E
-
random and site-directed mutagenesis
V582A/Y612C
-
random and site-directed mutagenesis
V582D
-
random mutagenesis
V582D/D639V
-
random and site-directed mutagenesis
W199A
3fold increase in Km value
Y1467F
-
the mutant shows a 150fold reduction in catalytic activity relative to wild-type enzyme
Y612C
-
random mutagenesis
Y612C/P655R
-
random and site-directed mutagenesis
Y638A
-
mutant of PCAF catalytic domain, increased Km and decreased kcat compared to wild-type
additional information
TEMPERATURE STABILITY
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
95
30 min, inactivation
GENERAL STABILITY
ORGANISM
UNIPROT
LITERATURE
acetyl-CoA stabilizes the enzyme form PCAF
-
PURIFICATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
cells are lysed after centrifugation in 100 mM Tris-HCl buffer, pH 7.6, immunoprecipitation, affinity purification with ProFound c-Myc-Tag IP/Co-IP kit, subcellular fractionation of homogenized cells in 10 mM triethanolamine, 10 mM acetic acid, 250 mM sucrose, 1 mM EDTA, and 1 mM dithiothreitol, pH 7.4, centrifuged, membrane pellet resuspended in 5% Nycodenz and layered on top of a Nycodenz solution gradient in 10 mM HEPES, pH 7.4, fractions collected and further concentrated by ultracentrifugation
-
HisTrap column chromatography and Superdex 75 gel filtration
Ni-NTA column chromatography and Superdex S200 gel filtration
Ni-NTA resin column chromatography
recombinant Atac2 fused to two HA and two FLAG tags from nuclear extracts of HEK-293 cells and murine C2C12 cells by M2-agarose affinity chromatography and gel filtration
recombinant catalytic domain of PCAF protein from E. coli
-
recombinant enzyme domains of PCAF and Gcn5
-
recombinant from Sf9 insect cells via baculovirus infection, FLAG-tagged MORF protein
recombinant GST- and FLAG-tagged KAT6B histone acetyltransferase domain from Escherichia coli by affinity chromatography
recombinant GST-tagged enzyme from Escherichia coli by glutathione affinity chromatography
-
recombinant His-tagged ARD1/Naa10 from Escherichia coli by nickel affinity chromatography, anion exchange chromatography, and gel filtration. After purification, rhARD1/NAA10 mainly exists in a high oligomeric state and has only a few monomers. Recombinant GST-tagged enzyme from Escherichia coli strain BL21 by glutathione affinity chromatography
recombinant His-tagged catalytic domain of PCAF protein from E. coli
-
recombinant His-tagged enzyme and GST-tagged enzyme from Escherichia coli strain BL21 by nickel and glutathione affinity chromatography, respectively
recombinant His-tagged hARD1/NAA10 enzyme by nickel affinity chromatography, with or without anion exchange chromatography, followed by gel filtration, and dialysis, the lysine acetylation activity of hARD1/NAA10 is well maintained until the elution step, but dramatically diminished after overnight dialysis. rhARD1/NAA10 aggregates during purification
CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
ATAC2, DNA and amino acid sequence determination and analysis, Atac2 fused to two HA and two FLAG tags is stably expressed in nuclei of HEK-293 cells and in murine C2C12 cells
expressed in Escherichia coli
-
expressed in Escherichia coli BL21(DE3) cells
expressed in Escherichia coli BL21-CodonPlus (DE3)-RIL cells
expression in HEK-293 cell
-
expression of full-length MORF and PCAF proteins in Sf9 cells
-
expression of His6-tagged enzyme in Spodoptora frugiperda Sf21 cell using the baculovirus infection system
-
expression of isoform a in Escherichia coli
expression of MORF protein as FLAG-tagged protein in Sf9 insect cells via baculovirus infection, and as Gal4-fusion protein in 293T cells, amino acid sequence
expression of mutant HATG485. Coexpression of HBO1 and Jade-1
-
expression of the catalytic domain of PCAF protein, amino acid residues 493-658, in Escherichia coli BL21 (DE3)
-
expression of the GST-tagged enzyme in Escherichia coli
-
expression of wild-type and inactive mutant Tip60 in HeLa cells and 293T cells
-
expression of wild-type and mutant enzymes in Spodoptera frugiperda Sf9 cells using the baculovirus expression system, genetic regulation of enzyme expression, overview
-
gene ARD1, recombinant expression in HEK-293 cells, stable recombinant overexpression of GFP-tagged enzyme in MEF cells, recombinant expression of His-tagged enzyme and of GST-tagged enzyme in Escherichia coli strain BL21
gene GCN5, recombinant expression in HEK-293T cells
gene KAT2A, recombinant expression in HeLa cells, overexpressed Flag-KAT2A does not associate with SQSTM1
gene KAT6B, genotyping in small cell lung cancer cell lines, recombinant expression of GST- and FLAG-tagged KAT6B histone acetyltransferase domain in Escherichia coli
gene KAT7, sequence comparisons, expression analysis
gene NAA10, recombinant expression of His-tagged ARD1/Naa10 in Escherichia coli strain BL21, recombinant expression of GST-tagged enzyme in Escherichia coli strain BL21
in vitro transcription and translation of p300 by rabbit reticulocyte extracts, transient expression of an enzyme-GAL4 reporter gene construct in 293T cells, in HeLa cells, and in KG1 cells
-
MYST1, sequence comparison, phylogenetic tree
overexpression of enzyme domain PCAF amino acid residues 493-658 in Escherichia coli
-
overexpression of recombinant histone acetyltransferase domain of p300/CBP-associated factor, residues 157–657, in Escherichia coli
-
PCR-amplification, stable transfection of CHO cells, with myc-tag, overexpressing enzyme
-
real-time RT-PCR analysis
-
recombinant expression of His-tagged hARD1/NAA10
recombinant p300 is expressed in baculovirus, and K1358A HAT mutant gene is expressed in Escherichia coli BL21
-
recombinant PCAF expressed in baculovirus
-
stable overexpression of FLAG-tagged MOF-conbtaining complex subunits in HEK293/FRT or HeLa S3 cells, overview
T7-coupled in vitro transcription and translation of FLAG-tagged enzyme
-
EXPRESSION
ORGANISM
UNIPROT
LITERATURE
the enzyme activity is upregulated in hepatocellular carcinoma compared to non-malignant liver tissues
although downregulation of UHRF1 by RNA interference enhances Tip60 expression, a significant decrease of the level of acetylated H2AK5 is observed
-
down-regulation of p300 by siRNA prevents UV-induced matrix metalloproteinase MMP-1 expression and inhibits UV-enhanced phosphorylation of H2AX, p53 level, and acetyl-H3
-
down-regulation of Tip60 and DNMT1 by RNA interference, dramatically reduced the levels of acetylated H2AK5
-
downregulation by RNA interference decreases the MYST1 content in human cells and results in lowered Lys16 acetylation in histone H4
Gcn5 is upregulated in human malignancies including non-small-cell lung cancer (NSCLC), colon cancer, and glioma
in immune-related disease, HBO1 is upregulated in synovial fibroblasts, which are the key pathogenic factors contributing to the development and progression of rheumatoid arthritis
transfected cells increase acetyltransferase activity 2fold, and by the treatment with the lipid second messenger ceramide
-
transfected cells increase acetyltransferase activity 3fold, and by the treatment with the lipid second messenger ceramide
-
UV irradiation of cultured human dermal fibroblasts induces matrix metalloproteinase MMP-1 expression and increases the level of phosphorylation of H2AX, p53 and the acetylation of histone H3
-
APPLICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
medicine
CBP/p300 could be a promising therapeutic target in hepatocellular carcinoma
analysis
-
methods for the analysis of histone acetyltransferase activity in vitro
drug development
HBO1 is a potential anti-cancer target, design of HBO1-targeting molecules and their applications
medicine
REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Herrera, J.E.; Bergel, M.; Yang, X.J.; Nakatani, Y.; Bustin, M.
The histone acetyltransferase activity of human GCN5 and PCAF is stabilized by coenzymes
J. Biol. Chem.
272
27253-27258
1997
Homo sapiens, Homo sapiens GCN5
Manually annotated by BRENDA team
Berger, S.L.
Gene activation by histone and factor acetyltransferases
Curr. Opin. Cell Biol.
11
336-341
1999
Saccharomyces cerevisiae, Homo sapiens, Tetrahymena sp., Homo sapiens GCN5
Manually annotated by BRENDA team
Champagne, N.; Bertos, N.R.; Pelletier, N.; Wang, A.H.; Vezmar, M.; Yang, Y.; Heng, H.H.; Yang, X.J.
Identification of a human histone acetyltransferase related to monocytic leukemia zinc finger protein
J. Biol. Chem.
274
28528-28536
1999
Homo sapiens, Homo sapiens (Q8WYB5)
Manually annotated by BRENDA team
Tanner, K.G.; Langer, M.R.; Denu, J.M.
Kinetic mechanism of human histone acetyltransferase P/CAF
Biochemistry
39
11961-11969
2000
Homo sapiens
Manually annotated by BRENDA team
Lau, O.D.; Courtney, A.D.; Vassilev, A.; Marzilli, L.A.; Cotter, R.J.; Nakatani, Y.; Cole, P.A.
P300/CBP-associated factor histone acetyltransferase processing of a peptide substrate. Kinetic analysis of the catalytic mechanism
J. Biol. Chem.
275
21953-21959
2000
Homo sapiens
Manually annotated by BRENDA team
Trievel, R.C.; Li, F.Y.; Marmorstein, R.
Application of a fluorescent histone acetyltransferase assay to probe the substrate specificity of the human p300/CBP-associated factor
Anal. Biochem.
287
319-328
2000
Saccharomyces cerevisiae, Homo sapiens, Tetrahymena thermophila, Homo sapiens GCN5, Tetrahymena thermophila GCN5
Manually annotated by BRENDA team
Poux, A.N.; Cebrat, M.; Kim, C.M.; Cole, P.A.; Marmorstein, R.
Structure of the GCN5 histone acetyltransferase bound to a bisubstrate inhibitor
Proc. Natl. Acad. Sci. USA
99
14065-14070
2002
Homo sapiens, Tetrahymena thermophila, Homo sapiens GCN5
Manually annotated by BRENDA team
Hasan, S.; Hottiger, M.O.
Histone acetyl transferases: a role in DNA repair and DNA replication
J. Mol. Med.
80
463-474
2002
Arabidopsis thaliana, Saccharomyces cerevisiae, Drosophila melanogaster, Homo sapiens, Mus musculus, Tetrahymena thermophila, Homo sapiens GCN5
Manually annotated by BRENDA team
Langer, M.R.; Fry, C.J.; Peterson, C.L.; Denu, J.M.
Modulating acetyl-CoA binding in the GCN5 family of histone acetyltransferases
J. Biol. Chem.
277
27337-27344
2002
Saccharomyces cerevisiae, Homo sapiens, Tetrahymena thermophila, Homo sapiens GCN5, Tetrahymena thermophila GCN5
Manually annotated by BRENDA team
Lemercier, C.; Legube, G.; Caron, C.; Louwagie, M.; Garin, J.; Trouche, D.; Khochbin, S.
Tip60 acetyltransferase activity is controlled by phosphorylation
J. Biol. Chem.
278
4713-4718
2003
Homo sapiens
Manually annotated by BRENDA team
Pelletier, N.; Champagne, N.; Lim, H.; Yang, X.J.
Expression, purification, and analysis of MOZ and MORF histone acetyltransferases
Methods
31
24-32
2003
Homo sapiens
Manually annotated by BRENDA team
Benson, L.J.; Annunziato, A.T.
In vitro analysis of histone acetyltransferase activity
Methods
33
45-52
2004
Saccharomyces cerevisiae, Homo sapiens
Manually annotated by BRENDA team
Taipale, M.; Rea, S.; Richter, K.; Vilar, A.; Lichter, P.; Imhof, A.; Akhtar, A.
hMOF histone acetyltransferase is required for histone H4 lysine 16 acetylation in mammalian cells
Mol. Cell. Biol.
25
6798-6810
2005
Homo sapiens
Manually annotated by BRENDA team
Carrozza, M.J.; Utley, R.T.; Workman, J.L.; Cote, J.
The diverse functions of histone acetyltransferase complexes
Trends Genet.
19
321-329
2003
Saccharomyces cerevisiae, Homo sapiens
Manually annotated by BRENDA team
Karanam, B.; Jiang, L.; Wang, L.; Kelleher, N.L.; Cole, P.A.
Kinetic and mass spectrometric analysis of p300 histone acetyltransferase domain autoacetylation
J. Biol. Chem.
281
40292-40301
2006
Homo sapiens
Manually annotated by BRENDA team
Mai, A.; Rotili, D.; Tarantino, D.; Ornaghi, P.; Tosi, F.; Vicidomini, C.; Sbardella, G.; Nebbioso, A.; Miceli, M.; Altucci, L.; Filetici, P.
Small-molecule inhibitors of histone acetyltransferase activity: identification and biological properties
J. Med. Chem.
49
6897-6907
2006
Saccharomyces cerevisiae, Homo sapiens
Manually annotated by BRENDA team
Mantelingu, K.; Kishore, A.H.; Balasubramanyam, K.; Kumar, G.V.; Altaf, M.; Swamy, S.N.; Selvi, R.; Das, C.; Narayana, C.; Rangappa, K.S.; Kundu, T.K.
Activation of p300 histone acetyltransferase by small molecules altering enzyme structure: probed by surface-enhanced Raman spectroscopy
J. Phys. Chem. B
111
4527-4534
2007
Homo sapiens
Manually annotated by BRENDA team
Stimson, L.; Rowlands, M.G.; Newbatt, Y.M.; Smith, N.F.; Raynaud, F.I.; Rogers, P.; Bavetsias, V.; Gorsuch, S.; Jarman, M.; Bannister, A.; Kouzarides, T.; McDonald, E.; Workman, P.; Aherne, G.W.
Isothiazolones as inhibitors of PCAF and p300 histone acetyltransferase activity
Mol. Cancer Ther.
4
1521-1532
2005
Homo sapiens
Manually annotated by BRENDA team
Hilton, T.L.; Li, Y.; Dunphy, E.L.; Wang, E.H.
TAF1 histone acetyltransferase activity in Sp1 activation of the cyclin D1 promoter
Mol. Cell. Biol.
25
4321-4332
2005
Homo sapiens
Manually annotated by BRENDA team
Guidez, F.; Howell, L.; Isalan, M.; Cebrat, M.; Alani, R.M.; Ivins, S.; Hormaeche, I.; McConnell, M.J.; Pierce, S.; Cole, P.A.; Licht, J.; Zelent, A.
Histone acetyltransferase activity of p300 is required for transcriptional repression by the promyelocytic leukemia zinc finger protein
Mol. Cell. Biol.
25
5552-5566
2005
Homo sapiens
Manually annotated by BRENDA team
Huang, W.C.; Chen, C.C.
Akt phosphorylation of p300 at Ser-1834 is essential for its histone acetyltransferase and transcriptional activity
Mol. Cell. Biol.
25
6592-6602
2005
Homo sapiens
Manually annotated by BRENDA team
Gong, J.; Zhu, J.; Goodman, O.B.; Pestell, R.G.; Schlegel, P.N.; Nanus, D.M.; Shen, R.
Activation of p300 histone acetyltransferase activity and acetylation of the androgen receptor by bombesin in prostate cancer cells
Oncogene
25
2011-2021
2006
Homo sapiens
Manually annotated by BRENDA team
Sun, Y.; Jiang, X.; Chen, S.; Fernandes, N.; Price, B.D.
A role for the Tip60 histone acetyltransferase in the acetylation and activation of ATM
Proc. Natl. Acad. Sci. USA
102
13182-13187
2005
Homo sapiens
Manually annotated by BRENDA team
Lee, Y.H.; Hong, S.W.; Jun, W.; Cho, H.Y.; Kim, H.C.; Jung, M.G.; Wong, J.; Kim, H.I.; Kim, C.H.; Yoon, H.G.
Anti-histone acetyltransferase activity from allspice extracts inhibits androgen receptor-dependent prostate cancer cell growth
Biosci. Biotechnol. Biochem.
71
2712-2719
2007
Homo sapiens
Manually annotated by BRENDA team
Sung, B.; Pandey, M.K.; Ahn, K.S.; Yi, T.; Chaturvedi, M.M.; Liu, M.; Aggarwal, B.B.
Anacardic acid (6-nonadecyl salicylic acid), an inhibitor of histone acetyltransferase, suppresses expression of nuclear factor-kappaB-regulated gene products involved in cell survival, proliferation, invasion, and inflammation through inhibition of the i
Blood
111
4880-4891
2008
Homo sapiens
Manually annotated by BRENDA team
Souto, J.A.; Conte, M.; Alvarez, R.; Nebbioso, A.; Carafa, V.; Altucci, L.; de Lera, A.R.
Synthesis of benzamides related to anacardic acid and their histone acetyltransferase (HAT) inhibitory activities
ChemMedChem
3
1435-1442
2008
Homo sapiens
Manually annotated by BRENDA team
Tahan, F.; Jazrawi, E.; Moodley, T.; Rovati, G.E.; Adcock, I.M.
Montelukast inhibits tumour necrosis factor-alpha-mediated interleukin-8 expression through inhibition of nuclear factor-kappaB p65-associated histone acetyltransferase activity
Clin. Exp. Allergy
38
805-811
2008
Homo sapiens
Manually annotated by BRENDA team
Buczek-Thomas, J.A.; Hsia, E.; Rich, C.B.; Foster, J.A.; Nugent, M.A.
Inhibition of histone acetyltransferase by glycosaminoglycans
J. Cell. Biochem.
105
108-120
2008
Homo sapiens
Manually annotated by BRENDA team
Costi, R.; Di Santo, R.; Artico, M.; Miele, G.; Valentini, P.; Novellino, E.; Cereseto, A.
Cinnamoyl compounds as simple molecules that inhibit p300 histone acetyltransferase
J. Med. Chem.
50
1973-1977
2007
Homo sapiens
Manually annotated by BRENDA team
Achour, M.; Fuhrmann, G.; Alhosin, M.; Ronde, P.; Chataigneau, T.; Mousli, M.; Schini-Kerth, V.B.; Bronner, C.
UHRF1 recruits the histone acetyltransferase Tip60 and controls its expression and activity
Biochem. Biophys. Res. Commun.
390
523-528
2009
Homo sapiens
Manually annotated by BRENDA team
Dmitriev, R.I.; Shakhparonov, M.I.; Pestov, N.B.
Structure and function of MYST1 histone acetyltransferase in the interactome of animal cells
Biochemistry (Moscow)
73
839-852
2008
Drosophila melanogaster, Homo sapiens (Q9H7Z6)
Manually annotated by BRENDA team
Voss, A.K.; Thomas, T.
MYST family histone acetyltransferases take center stage in stem cells and development
Bioessays
31
1050-1061
2009
Arabidopsis thaliana, Danio rerio, Saccharomyces cerevisiae, Caenorhabditis elegans, Drosophila melanogaster, Homo sapiens, Mus musculus, Danio rerio zMoz
Manually annotated by BRENDA team
Mai, A.; Rotili, D.; Tarantino, D.; Nebbioso, A.; Castellano, S.; Sbardella, G.; Tini, M.; Altucci, L.
Identification of 4-hydroxyquinolines inhibitors of p300/CBP histone acetyltransferases
Bioorg. Med. Chem. Lett.
19
1132-1135
2009
Homo sapiens
Manually annotated by BRENDA team
Dekker, F.J.; Ghizzoni, M.; van der Meer, N.; Wisastra, R.; Haisma, H.J.
Inhibition of the PCAF histone acetyl transferase and cell proliferation by isothiazolones
Bioorg. Med. Chem.
17
460-466
2009
Homo sapiens (Q92831)
Manually annotated by BRENDA team
Gorsuch, S.; Bavetsias, V.; Rowlands, M.G.; Aherne, G.W.; Workman, P.; Jarman, M.; McDonald, E.
Synthesis of isothiazol-3-one derivatives as inhibitors of histone acetyltransferases (HATs)
Bioorg. Med. Chem.
17
467-474
2009
Homo sapiens
Manually annotated by BRENDA team
Berndsen, C.E.; Denu, J.M.
Catalysis and substrate selection by histone/protein lysine acetyltransferases
Curr. Opin. Struct. Biol.
18
682-689
2008
Saccharomyces cerevisiae, Homo sapiens, Tetrahymena sp., Tetrahymena sp. GCN5
Manually annotated by BRENDA team
Ghizzoni, M.; Haisma, H.J.; Dekker, F.J.
Reactivity of isothiazolones and isothiazolone-1-oxides in the inhibition of the PCAF histone acetyltransferase
Eur. J. Med. Chem.
44
4855-4861
2009
Homo sapiens
Manually annotated by BRENDA team
Leemhuis, H.; Nightingale, K.P.; Hollfelder, F.
Directed evolution of a histone acetyltransferase - enhancing thermostability, whilst maintaining catalytic activity and substrate specificity
FEBS J.
275
5635-5647
2008
Homo sapiens
Manually annotated by BRENDA team
Iizuka, M.; Takahashi, Y.; Mizzen, C.A.; Cook, R.G.; Fujita, M.; Allis, C.D.; Frierson, H.F.; Fukusato, T.; Smith, M.M.
Histone acetyltransferase Hbo1: catalytic activity, cellular abundance, and links to primary cancers
Gene
436
108-114
2009
Homo sapiens
Manually annotated by BRENDA team
Miotto, B.; Struhl, K.
HBO1 histone acetylase is a coactivator of the replication licensing factor Cdt1
Genes Dev.
22
2633-2638
2008
Homo sapiens
Manually annotated by BRENDA team
Karukurichi, K.R.; Wang, L.; Uzasci, L.; Manlandro, C.M.; Wang, Q.; Cole, P.A.
Analysis of p300/CBP histone acetyltransferase regulation using circular permutation and semisynthesis
J. Am. Chem. Soc.
132
1222-1223
2010
Homo sapiens
Manually annotated by BRENDA team
Chen, W.; Bacanamwo, M.; Harrison, D.G.
Activation of p300 histone acetyltransferase activity is an early endothelial response to laminar shear stress and is essential for stimulation of endothelial nitric-oxide synthase mRNA transcription
J. Biol. Chem.
283
16293-16298
2008
Homo sapiens
Manually annotated by BRENDA team
Ravindra, K.C.; Selvi, B.R.; Arif, M.; Reddy, B.A.; Thanuja, G.R.; Agrawal, S.; Pradhan, S.K.; Nagashayana, N.; Dasgupta, D.; Kundu, T.K.
Inhibition of lysine acetyltransferase KAT3B/p300 activity by a naturally occurring hydroxynaphthoquinone, plumbagin
J. Biol. Chem.
284
24453-24464
2009
Homo sapiens, Mus musculus
Manually annotated by BRENDA team
Ko, M.H.; Puglielli, L.
Two endoplasmic reticulum (ER)/ER intermediate compartment-based lysine acetyltransferases post-translationally regulate BACE1 levels
J. Biol. Chem.
284
2482-2492
2009
Homo sapiens
Manually annotated by BRENDA team
Cai, Y.; Jin, J.; Swanson, S.K.; Cole, M.D.; Choi, S.H.; Florens, L.; Washburn, M.P.; Conaway, J.W.; Conaway, R.C.
Subunit composition and substrate specificity of a MOF-containing histone acetyltransferase distinct from the male-specific lethal (MSL) complex
J. Biol. Chem.
285
4268-4272
2009
Homo sapiens, Homo sapiens (Q9H7Z6)
Manually annotated by BRENDA team
Arif, M.; Pradhan, S.K.; Thanuja, G.R.; Vedamurthy, B.M.; Agrawal, S.; Dasgupta, D.; Kundu, T.K.
Mechanism of p300 specific histone acetyltransferase inhibition by small molecules
J. Med. Chem.
52
267-277
2009
Homo sapiens (Q92831)
Manually annotated by BRENDA team
Guelman, S.; Kozuka, K.; Mao, Y.; Pham, V.; Solloway, M.J.; Wang, J.; Wu, J.; Lill, J.R.; Zha, J.
The double-histone-acetyltransferase complex ATAC is essential for mammalian development
Mol. Cell. Biol.
29
1176-1188
2009
Mus musculus, Homo sapiens (Q9H8E8)
Manually annotated by BRENDA team
Miotto, B.; Struhl, K.
HBO1 histone acetylase activity is essential for DNA replication licensing and inhibited by geminin
Mol. Cell
37
57-66
2010
Homo sapiens
Manually annotated by BRENDA team
Kim, M.K.; Shin, J.M.; Eun, H.C.; Chung, J.H.
The role of p300 histone acetyltransferase in UV-induced histone modifications and MMP-1 gene transcription
PLoS ONE
4
e4864
2009
Homo sapiens
Manually annotated by BRENDA team
Furdas, S.D.; Shekfeh, S.; Bissinger, E.M.; Wagner, J.M.; Schlimme, S.; Valkov, V.; Hendzel, M.; Jung, M.; Sippl, W.
Synthesis and biological testing of novel pyridoisothiazolones as histone acetyltransferase inhibitors
Bioorg. Med. Chem.
19
3678-3689
2011
Homo sapiens
Manually annotated by BRENDA team
Milite, C.; Castellano, S.; Benedetti, R.; Tosco, A.; Ciliberti, C.; Vicidomini, C.; Boully, L.; Franci, G.; Altucci, L.; Mai, A.; Sbardella, G.
Modulation of the activity of histone acetyltransferases by long chain alkylidenemalonates (LoCAMs)
Bioorg. Med. Chem.
19
3690-3701
2011
Homo sapiens
Manually annotated by BRENDA team
Yuan, H.; Rossetto, D.; Mellert, H.; Dang, W.; Srinivasan, M.; Johnson, J.; Hodawadekar, S.; Ding, E.C.; Speicher, K.; Abshiru, N.; Perry, R.; Wu, J.; Yang, C.; Zheng, Y.G.; Speicher, D.W.; Thibault, P.; Verreault, A.; Johnson, F.B.; Berger, S.L.; Sternglanz, R.; McMahon, S.B.; Cote, J.; Marmorstein, R.
MYST protein acetyltransferase activity requires active site lysine autoacetylation
EMBO J.
31
58-70
2012
Homo sapiens, Saccharomyces cerevisiae (Q08649), Saccharomyces cerevisiae
Manually annotated by BRENDA team
Banerjee, S.; M, A.; Rakshit, T.; Roy, N.S.; Kundu, T.K.; Roy, S.; Mukhopadhyay, R.
Structural features of human histone acetyltransferase p300 and its complex with p53
FEBS Lett.
586
3793-3798
2012
Homo sapiens
Manually annotated by BRENDA team
He, T.; Hong, S.Y.; Huang, L.; Xue, W.; Yu, Z.; Kwon, H.; Kirk, M.; Ding, S.J.; Su, K.; Zhang, Z.
Histone acetyltransferase p300 acetylates Pax5 and strongly enhances Pax5-mediated transcriptional activity
J. Biol. Chem.
286
14137-14145
2011
Homo sapiens
Manually annotated by BRENDA team
Li, Y.; Jaramillo-Lambert, A.; Hao, J.; Yang, Y.; Zhu, W.
The stability of histone acetyltransferase general control non-derepressible (Gcn) 5 is regulated by Cullin4-RING E3 ubiquitin ligase
J. Biol. Chem.
286
41344-41352
2011
Homo sapiens
Manually annotated by BRENDA team
Zhao, H.; Jin, S.; Gewirtz, A.M.
The histone acetyltransferase TIP60 interacts with c-Myb and inactivates its transcriptional activity in human leukemia
J. Biol. Chem.
287
925-934
2012
Homo sapiens
Manually annotated by BRENDA team
Mehta, K.R.; Yang, C.Y.; Montclare, J.K.
Modulating substrate specificity of histone acetyltransferase with unnatural amino acids
Mol. Biosyst.
7
3050-3055
2011
Homo sapiens (Q09472), Homo sapiens
Manually annotated by BRENDA team
Li, Y.; Jaramillo-Lambert, A.N.; Yang, Y.; Williams, R.; Lee, N.H.; Zhu, W.
And-1 is required for the stability of histone acetyltransferase Gcn5
Oncogene
31
643-652
2012
Homo sapiens
Manually annotated by BRENDA team
Jiang, J.; Lu, J.; Lu, D.; Liang, Z.; Li, L.; Ouyang, S.; Kong, X.; Jiang, H.; Shen, B.; Luo, C.
Investigation of the acetylation mechanism by GCN5 histone acetyltransferase
PLoS ONE
7
e36660
2012
Homo sapiens (Q92830)
Manually annotated by BRENDA team
Wu, H.; Moshkina, N.; Min, J.; Zeng, H.; Joshua, J.; Zhou, M.M.; Plotnikov, A.N.
Structural basis for substrate specificity and catalysis of human histone acetyltransferase 1
Proc. Natl. Acad. Sci. USA
109
8925-8930
2012
Homo sapiens (O14929), Homo sapiens
Manually annotated by BRENDA team
Liu, Z.; Luo, X.; Liu, L.; Zhao, W.; Guo, S.; Guo, Y.; Wang, N.; He, H.; Liao, X.; Ma, W.; Zhou, H.; Zhang, T.
Histone acetyltransferase p300 promotes MKL1-mediated transactivation of catechol-O-methyltransferase gene
Acta Biochim. Biophys. Sin. (Shanghai)
45
1002-1010
2013
Homo sapiens
Manually annotated by BRENDA team
Secci, D.; Carradori, S.; Bizzarri, B.; Bolasco, A.; Ballario, P.; Patramani, Z.; Fragapane, P.; Vernarecci, S.; Canzonetta, C.; Filetici, P.
Synthesis of a novel series of thiazole-based histone acetyltransferase inhibitors
Bioorg. Med. Chem.
22
1680-1689
2014
Saccharomyces cerevisiae, Homo sapiens
Manually annotated by BRENDA team
Simo-Riudalbas, L.; Perez-Salvia, M.; Setien, F.; Villanueva, A.; Moutinho, C.; Martinez-Cardus, A.; Moran, S.; Berdasco, M.; Gomez, A.; Vidal, E.; Soler, M.; Heyn, H.; Vaquero, A.; de la Torre, C.; Barcelo-Batllori, S.; Vidal, A.; Roz, L.; Pastorino, U.; Szakszon, K.; Borck, G.; Moura, C.S.; Carneiro, F.; Zondervan, I.; Savola, S.; Iwakawa, R.; Kohno, T.; Yokota, J.; Esteller, M.
KAT6B is a tumor suppressor histone H3 lysine 23 acetyltransferase undergoing genomic loss in small cell lung cancer
Cancer Res.
75
3936-3945
2015
Homo sapiens (Q8WYB5), Homo sapiens
Manually annotated by BRENDA team
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
Eur. J. Med. Chem.
105
289-296
2015
Homo sapiens (Q09472), Homo sapiens (Q9H7Z6)
Manually annotated by BRENDA team
Carradori, S.; Rotili, D.; De Monte, C.; Lenoci, A.; D'Ascenzio, M.; Rodriguez, V.; Filetici, P.; Miceli, M.; Nebbioso, A.; Altucci, L.; Secci, D.; Mai, A.
Evaluation of a large library of (thiazol-2-yl)hydrazones and analogues as histone acetyltransferase inhibitors: enzyme and cellular studies
Eur. J. Med. Chem.
80
569-578
2014
Homo sapiens (Q92830), Homo sapiens
Manually annotated by BRENDA team
Inagaki, Y.; Shiraki, K.; Sugimoto, K.; Yada, T.; Tameda, M.; Ogura, S.; Yamamoto, N.; Takei, Y.; Ito, M.
Epigenetic regulation of proliferation and invasion in hepatocellular carcinoma cells by CBP/p300 histone acetyltransferase activity
Int. J. Oncol.
48
533-540
2016
Homo sapiens (Q09472), Homo sapiens (Q92793)
Manually annotated by BRENDA team
Chen, L.; Wei, T.; Si, X.; Wang, Q.; Li, Y.; Leng, Y.; Deng, A.; Chen, J.; Wang, G.; Zhu, S.; Kang, J.
Lysine acetyltransferase GCN5 potentiates the growth of non-small cell lung cancer via promotion of E2F1, cyclin D1, and cyclin E1 expression
J. Biol. Chem.
288
14510-14521
2013
Homo sapiens (Q92830)
Manually annotated by BRENDA team
Zheng, X.; Gai, X.; Ding, F.; Lu, Z.; Tu, K.; Yao, Y.; Liu, Q.
Histone acetyltransferase PCAF up-regulated cell apoptosis in hepatocellular carcinoma via acetylating histone H4 and inactivating AKT signaling
Mol. Cancer
12
96
2013
Homo sapiens
Manually annotated by BRENDA team
Fuellgrabe, J.; Lynch-Day, M.A.; Heldring, N.; Li, W.; Struijk, R.B.; Ma, Q.; Hermanson, O.; Rosenfeld, M.G.; Klionsky, D.J.; Joseph, B.
The histone H4 lysine 16 acetyltransferase hMOF regulates the outcome of autophagy
Nature
500
468-471
2013
Homo sapiens (Q9H7Z6)
Manually annotated by BRENDA team
Han, Z.; Chou, C.W.; Yang, X.; Bartlett, M.G.; Zheng, Y.G.
Profiling cellular substrates of lysine acetyltransferases GCN5 and p300 with orthogonal labeling and click chemistry
ACS Chem. Biol.
12
1547-1555
2017
Homo sapiens (Q09472), Homo sapiens (Q92830)
Manually annotated by BRENDA team
Shrimp, J.H.; Sorum, A.W.; Garlick, J.M.; Guasch, L.; Nicklaus, M.C.; Meier, J.L.
Characterizing the covalent targets of a small molecule inhibitor of the lysine acetyltransferase P300
ACS Med. Chem. Lett.
7
151-155
2016
Homo sapiens (Q09472)
Manually annotated by BRENDA team
Ouyang, C.; Mu, J.; Lu, Q.; Li, J.; Zhu, H.; Wang, Q.; Zou, M.H.; Xie, Z.
Autophagic degradation of KAT2A/GCN5 promotes directional migration of vascular smooth muscle cells by reducing TUBA/alpha-tubulin acetylation
Autophagy
2019
1-18
2019
Saccharomyces cerevisiae, Homo sapiens (Q92830), Homo sapiens, Saccharomyces cerevisiae D273-10B/A1, Saccharomyces cerevisiae W303-1A
Manually annotated by BRENDA team
Lan, R.; Wang, Q.
Deciphering structure, function and mechanism of lysine acetyltransferase HBO1 in protein acetylation, transcription regulation, DNA replication and its oncogenic properties in cancer
Cell. Mol. Life Sci.
77
637-649
2020
Homo sapiens (O95251), Mus musculus (Q5SVQ0)
Manually annotated by BRENDA team
Ngo, L.; Brown, T.; Zheng, Y.G.
Bisubstrate inhibitors to target histone acetyltransferase 1
Chem. Biol. Drug Des.
93
865-873
2019
Homo sapiens (O14929)
Manually annotated by BRENDA team
Madia, V.; Benedetti, R.; Barreca, M.; Ngo, L.; Pescatori, L.; Messore, A.; Pupo, G.; Saccoliti, F.; Valente, S.; Mai, A.; Scipione, L.; Zheng, Y.; Tintori, C.; Botta, M.; Cecchetti, V.; Altucci, L.; Di Santo, R.; Costi, R.
Structure-activity relationships on cinnamoyl derivatives as inhibitors of p300 histone acetyltransferase
ChemMedChem
12
1359-1368
2017
Homo sapiens (Q09472), Homo sapiens
Manually annotated by BRENDA team
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
Eur. J. Med. Chem.
157
867-876
2018
Homo sapiens (Q9H7Z6)
Manually annotated by BRENDA team
Huang, M.; Huang, J.; Zheng, Y.; Sun, Q.
Histone acetyltransferase inhibitors An overview in synthesis, structure-activity relationship and molecular mechanism
Eur. J. Med. Chem.
178
259-286
2019
Homo sapiens
Manually annotated by BRENDA team
Liu, R.; Zhang, Z.; Yang, H.; Zhou, K.; Geng, M.; Zhou, W.; Zhang, M.; Huang, X.; Li, Y.
Design, synthesis, and biological evaluation of a new class of histone acetyltransferase p300 inhibitors
Eur. J. Med. Chem.
180
171-190
2019
Homo sapiens (Q09472), Homo sapiens
Manually annotated by BRENDA team
Fiorentino, F.; Mai, A.; Rotili, D.
Lysine acetyltransferase inhibitors structure-activity relationships and potential therapeutic implications
Future Med. Chem.
10
1067-1091
2018
Drosophila melanogaster (O02193), Drosophila melanogaster (P51123), Drosophila melanogaster (Q960X4), Homo sapiens (O15516), Homo sapiens (O95251), Homo sapiens (P21675), Homo sapiens (Q15788), Homo sapiens (Q8WYB5), Homo sapiens (Q92793), Homo sapiens (Q92794), Homo sapiens (Q92830), Homo sapiens (Q92831), Homo sapiens (Q92993), Homo sapiens (Q9BQG0), Homo sapiens (Q9H7Z6), Homo sapiens (Q9H9T3), Homo sapiens (Q9UKN8), Homo sapiens (Q9Y6Q9), Homo sapiens, Saccharomyces cerevisiae (P39979), Saccharomyces cerevisiae (P46677), Saccharomyces cerevisiae (P53114), Saccharomyces cerevisiae (Q06592), Saccharomyces cerevisiae (Q07794), Saccharomyces cerevisiae ATCC 204508 (P39979), Saccharomyces cerevisiae ATCC 204508 (P46677), Saccharomyces cerevisiae ATCC 204508 (P53114), Saccharomyces cerevisiae ATCC 204508 (Q06592), Saccharomyces cerevisiae ATCC 204508 (Q07794)
Manually annotated by BRENDA team
Thorsheim, K.; Persson, A.; Siegbahn, A.; Tykesson, E.; Westergren-Thorsson, G.; Mani, K.; Ellervik, U.
Disubstituted naphthyl beta-D-xylopyranosides Synthesis, GAG priming, and histone acetyltransferase (HAT) inhibition
Glycoconj. J.
33
245-257
2016
Homo sapiens
Manually annotated by BRENDA team
Inagaki, Y.; Shiraki, K.; Sugimoto, K.; Yada, T.; Tameda, M.; Ogura, S.; Yamamoto, N.; Takei, Y.; Ito, M.
Epigenetic regulation of proliferation and invasion in hepatocellular carcinoma cells by CBP/p300 histone acetyltransferase activity
Int. J. Oncol.
48
533-540
2016
Homo sapiens (Q09472)
Manually annotated by BRENDA team
Sivanandam, M.; Saravanan, K.; Kumaradhas, P.
Insights into intermolecular interactions, electrostatic properties and the stability of C646 in the binding pocket of p300 histone acetyltransferase enzyme A combined molecular dynamics and charge density study
J. Biomol. Struct. Dyn.
36
3246-3264
2018
Homo sapiens (Q09472)
Manually annotated by BRENDA team
Priebbenow, D.L.; Leaver, D.J.; Nguyen, N.; Cleary, B.; Lagiakos, H.R.; Sanchez, J.; Xue, L.; Huang, F.; Sun, Y.; Mujumdar, P.; Mudududdla, R.; Varghese, S.; Teguh, S.; Charman, S.A.; White, K.L.; Shackleford, D.M.; Katneni, K.; Cuellar, M.; Strasser, J.M.; Dahlin, J.L.; Walters, M.A.; Street, I.P.; Monahan, B.J.; Jarman, K.E.; Jousset Sabroux, H.; Falk, H.; Chung, M.C.; Hermans, S.J.; Downer, N.L.; Parker, M.W.; Voss, A.K.; Thomas, T.; Baell, J.B.
Discovery of acylsulfonohydrazide-derived inhibitors of the lysine acetyltransferase, KAT6A, as potent senescence-inducing anti-cancer agents
J. Med. Chem.
63
4655-4684
2020
Homo sapiens (Q92794)
Manually annotated by BRENDA team
Vo, T.T.L.; Park, J.H.; Lee, E.J.; Nguyen, Y.T.K.; Han, B.W.; Nguyen, H.T.T.; Mun, K.C.; Ha, E.; Kwon, T.K.; Kim, K.W.; Jeong, C.H.; Seo, J.H.
Characterization of lysine acetyltransferase activity of recombinant human ARD1/NAA10
Molecules
25
588
2020
Homo sapiens (P41227), Homo sapiens
Manually annotated by BRENDA team
Tao, Y.; Zhong, C.; Zhu, J.; Xu, S.; Ding, J.
Structural and mechanistic insights into regulation of HBO1 histone acetyltransferase activity by BRPF2
Nucleic Acids Res.
45
5707-5719
2017
Homo sapiens (O95251)
Manually annotated by BRENDA team
Lu Vo, T.; Park, J.; Seo, J.; Lee, E.; Choi, H.; Bae, S.; Le, H.; An, S.; Lee, H.; Wee, H.; Kim, K.
ARD1-mediated aurora kinase A acetylation promotes cell proliferation and migration
Oncotarget
8
57216-57230
2017
Homo sapiens (P41227)
Manually annotated by BRENDA team
Rollins, M.; Huard, S.; Morettin, A.; Takuski, J.; Pham, T.T.; Fullerton, M.D.; Cote, J.; Baetz, K.
Lysine acetyltransferase NuA4 and acetyl-CoA regulate glucose-deprived stress granule formation in Saccharomyces cerevisiae
PLoS Genet.
13
e1006626
2017
Saccharomyces cerevisiae (Q08649), Saccharomyces cerevisiae, Homo sapiens (Q92993), Homo sapiens, Saccharomyces cerevisiae BY4741 (Q08649)
Manually annotated by BRENDA team
Deng, W.; Wang, C.; Zhang, Y.; Xu, Y.; Zhang, S.; Liu, Z.; Xue, Y.
GPS-PAIL prediction of lysine acetyltransferase-specific modification sites from protein sequences
Sci. Rep.
6
39787
2016
Homo sapiens (O14929), Homo sapiens (Q09472), Homo sapiens (Q92793), Homo sapiens (Q92830), Homo sapiens (Q92831), Homo sapiens (Q92993), Homo sapiens (Q9H7Z6), Homo sapiens
Manually annotated by BRENDA team