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Literature summary extracted from

  • 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 (2011), Bioorg. Med. Chem., 19, 3678-3689.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.3.1.48 overexpression of recombinant histone acetyltransferase domain of p300/CBP-associated factor, residues 157–657, in Escherichia coli Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.3.1.48 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 Homo sapiens
2.3.1.48 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 Homo sapiens
2.3.1.48 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 Homo sapiens
2.3.1.48 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 Homo sapiens

Organism

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

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.3.1.48 acetyl-CoA + histone H3 peptide residues 1-21 of human histone H3 Homo sapiens CoA + actylhistone H3
-
 ?
2.3.1.48 acetyl-CoA + histone H4 peptide residues 2-24 of human histone H4 Homo sapiens CoA + actylhistone H4
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.3.1.48 P300/CBP-associated factor
-
 Homo sapiens
2.3.1.48 PCAF
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.3.1.48 0.00072
-
 substrate histone H4 peptide, pH 7.5, 30°C Homo sapiens 2-(4-fluorophenyl)isothiazolo[5,4-b]pyridin-3(2H)-one
2.3.1.48 0.00164
-
 substrate histone H3 peptide, pH 7.5, 30°C Homo sapiens 2-(4-fluorophenyl)isothiazolo[5,4-b]pyridin-3(2H)-one
2.3.1.48 0.00463
-
 substrate histone H3 peptide, pH 7.5, 30°C Homo sapiens 2-(4-methylphenyl)isothiazolo[5,4-b]pyridin-3(2H)-one
2.3.1.48 0.00503
-
 substrate histone H3 peptide, pH 7.5, 30°C Homo sapiens 2-(3-methoxyphenyl)isothiazolo[5,4-b]pyridin-3(2H)-one
2.3.1.48 0.0255
-
 substrate histone H3 peptide, pH 7.5, 30°C Homo sapiens 2-(4-(trifluoromethyl)benzyl)isothiazolo[5,4-b]pyridin-3(2H)-one
2.3.1.48 0.13
-
 substrate histone H3 peptide, pH 7.5, 30°C Homo sapiens 2-(4-(trifluoromethyl)benzyl)isothiazolo[5,4-b]pyridin-3(2H)-one