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Literature summary for 2.3.1.48 extracted from

  • Ghizzoni, M.; Haisma, H.J.; Dekker, F.J.
    Reactivity of isothiazolones and isothiazolone-1-oxides in the inhibition of the PCAF histone acetyltransferase (2009), Eur. J. Med. Chem., 44, 4855-4861.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
2-tert-butyl-5-(dodecylthio)isothiazol-3(2H)-one-1-oxide
-
Homo sapiens
2-tert-butyl-5-chloroisothiazol-3(2H)-one 1-oxide
-
Homo sapiens
4,5-dichloro-2-ethylisothiazol-3(2H)-one
-
Homo sapiens
4,5-dichloro-2-ethylisothiazol-3(2H)-one-1-oxide
-
Homo sapiens
5-chloro-2-ethyl-4-methylisothiazol-3(2H)-one
-
Homo sapiens
5-chloro-2-ethyl-4-methylisothiazol-3(2H)-one-1-oxide
-
Homo sapiens
5-chloro-2-ethylisothiazol-3(2H)-one
-
Homo sapiens
5-chloro-2-ethylisothiazol-3(2H)-one-1-oxide
-
Homo sapiens
methyl 3-(4,5-dichloro-1-oxido-3-oxoisothiazol-2(3H)-yl)propanoate
-
Homo sapiens
methyl 3-(4,5-dichloro-3-oxoisothiazol-2(3H)-yl)propanoate
-
Homo sapiens
methyl 3-(5-chloro-1-oxido-3-oxoisothiazol-2(3H)-yl)propanoate
-
Homo sapiens
methyl 3-(5-chloro-3-oxoisothiazol-2(3H)-yl)propanoate
-
Homo sapiens
methyl 3-(5-chloro-4-methyl-1-oxido-3-oxoisothiazol-2(3H)-yl)propanoate
-
Homo sapiens
methyl 3-(5-chloro-4-methyl-3-oxoisothiazol-2(3H)-yl)propanoate
-
Homo sapiens
methyl 3-[4-chloro-5-(dodecylthio)-1-oxido-3-oxoisothiazol-2(3H)-yl]propanoate
-
Homo sapiens
methyl 3-[5-(dodecylthio)-1-oxido-3-oxoisothiazol-2(3H)-yl] propanoate
-
Homo sapiens
additional information inhibitory potencies of isothiazolones and isothiazolone-1-oxides on PCAF and growth inhibition of Hep-G2 cancer cells, overview Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
commercial preparation
-
Homo sapiens
-
Hep-G2 cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
acetyl-CoA + histone H3
-
Homo sapiens CoA + acetylhistone H3
-
?

Synonyms

Synonyms Comment Organism
p300/CBP associated factor
-
Homo sapiens
PCAF
-
Homo sapiens

Cofactor

Cofactor Comment Organism Structure
acetyl-CoA
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0018
-
-
Homo sapiens methyl 3-(5-chloro-3-oxoisothiazol-2(3H)-yl)propanoate
0.0024
-
-
Homo sapiens 4,5-dichloro-2-ethylisothiazol-3(2H)-one
0.0026
-
-
Homo sapiens methyl 3-(4,5-dichloro-3-oxoisothiazol-2(3H)-yl)propanoate
0.003
-
-
Homo sapiens 5-chloro-2-ethylisothiazol-3(2H)-one
0.0056
-
-
Homo sapiens methyl 3-(5-chloro-1-oxido-3-oxoisothiazol-2(3H)-yl)propanoate
0.01
-
above Homo sapiens 5-chloro-2-ethyl-4-methylisothiazol-3(2H)-one
0.01
-
above Homo sapiens methyl 3-(5-chloro-4-methyl-3-oxoisothiazol-2(3H)-yl)propanoate
0.01
-
above Homo sapiens 5-chloro-2-ethylisothiazol-3(2H)-one-1-oxide
0.01
-
above Homo sapiens 4,5-dichloro-2-ethylisothiazol-3(2H)-one-1-oxide
0.01
-
above Homo sapiens 5-chloro-2-ethyl-4-methylisothiazol-3(2H)-one-1-oxide
0.01
-
above Homo sapiens methyl 3-(4,5-dichloro-1-oxido-3-oxoisothiazol-2(3H)-yl)propanoate
0.01
-
above Homo sapiens methyl 3-(5-chloro-4-methyl-1-oxido-3-oxoisothiazol-2(3H)-yl)propanoate
0.01
-
above Homo sapiens 2-tert-butyl-5-chloroisothiazol-3(2H)-one 1-oxide
0.01
-
above Homo sapiens 2-tert-butyl-5-(dodecylthio)isothiazol-3(2H)-one-1-oxide
0.01
-
above Homo sapiens methyl 3-[5-(dodecylthio)-1-oxido-3-oxoisothiazol-2(3H)-yl] propanoate
0.01
-
above Homo sapiens methyl 3-[4-chloro-5-(dodecylthio)-1-oxido-3-oxoisothiazol-2(3H)-yl]propanoate