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Literature summary extracted from

  • 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 (2005), Mol. Cancer Ther., 4, 1521-1532.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.3.1.48 expression of the GST-tagged enzyme in Escherichia coli Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.3.1.48 CCT004463 in vivo cell proliferation inhibition Homo sapiens
2.3.1.48 CCT004464 in vivo cell proliferation inhibition Homo sapiens
2.3.1.48 CCT004465 in vivo cell proliferation inhibition Homo sapiens
2.3.1.48 CCT004466 in vivo cell proliferation inhibition Homo sapiens
2.3.1.48 CCT004467 in vivo cell proliferation inhibition Homo sapiens
2.3.1.48 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 Homo sapiens
2.3.1.48 CCT077792 IC50: 0.0027-0.015 mM, in vivo cell proliferation inhibition Homo sapiens
2.3.1.48 CCT077796 IC50: 0.0187-0.0202 mM, in vivo cell proliferation inhibition Homo sapiens
2.3.1.48 CCT079769 IC50: 0.0547 mM, in vivo cell proliferation inhibition Homo sapiens
2.3.1.48 H3-CoA-20 IC50: 0.034-0.064 mM Homo sapiens
2.3.1.48 isothiazolone binds irreversibly to proteins via thiol interactions Homo sapiens
2.3.1.48 Lys-CoA IC50: 310-420 nM Homo sapiens
2.3.1.48 additional information inhibitory potency of N-substituted isothiazolone-based compounds, in vivo cell proliferation inhibition, overview Homo sapiens

Localization

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

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.3.1.48 histone H3 + acetyl-CoA Homo sapiens acetylation of Lys9, and Lys14 acetyl-histone H3 + CoA
-
 ?
2.3.1.48 histone H4 + acetyl-CoA Homo sapiens
-
 acetyl-histone H4 + CoA
-
 ?
2.3.1.48 additional information Homo sapiens deregulated HAT activity plays a role in the development of a range of cancers ?
-
 ?

Organism

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

Purification (Commentary)

EC Number Purification (Comment) Organism
2.3.1.48 recombinant GST-tagged enzyme from Escherichia coli by glutathione affinity chromatography Homo sapiens

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.3.1.48 HCT-116 cell colon tumor cell line Homo sapiens
-
2.3.1.48 HT-29 cell colon tumor cell line Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.3.1.48 histone H3 + acetyl-CoA acetylation of Lys9, and Lys14 Homo sapiens acetyl-histone H3 + CoA
-
 ?
2.3.1.48 histone H4 + acetyl-CoA
-
 Homo sapiens acetyl-histone H4 + CoA
-
 ?
2.3.1.48 histone H4 + acetyl-CoA acetylation of Lys5, Lys8, and Lys12 Homo sapiens acetyl-histone H4 + CoA
-
 ?
2.3.1.48 additional information deregulated HAT activity plays a role in the development of a range of cancers Homo sapiens ?
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.3.1.48 HAT
-
 Homo sapiens
2.3.1.48 p300 HAT
-
 Homo sapiens
2.3.1.48 p300 histone acetyltransferase
-
 Homo sapiens

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
2.3.1.48 30
-
 assay at Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
2.3.1.48 8
-
 assay at Homo sapiens

Cofactor

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

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.3.1.48 0.00031 0.00042 IC50: 310-420 nM Homo sapiens Lys-CoA
2.3.1.48 0.0022 0.0073 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 Homo sapiens CCT077791
2.3.1.48 0.0027 0.015 IC50: 0.0027-0.015 mM, in vivo cell proliferation inhibition Homo sapiens CCT077792
2.3.1.48 0.0187 0.0202 IC50: 0.0187-0.0202 mM, in vivo cell proliferation inhibition Homo sapiens CCT077796
2.3.1.48 0.034 0.064 IC50: 0.034-0.064 mM Homo sapiens H3-CoA-20
2.3.1.48 0.0547
-
 IC50: 0.0547 mM, in vivo cell proliferation inhibition Homo sapiens CCT079769