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Literature summary for 3.5.1.98 extracted from

  • Henkes, L.M.; Haus, P.; Jaeger, F.; Ludwig, J.; Meyer-Almes, F.J.
    Synthesis and biochemical analysis of 2,2,3,3,4,4,5,5,6,6,7,7-dodecafluoro-N-hydroxy-octanediamides as inhibitors of human histone deacetylases (2012), Bioorg. Med. Chem., 20, 985-995.
    View publication on PubMed
Search for more literature for 3.5.1.98

Cloned(Commentary)

Cloned (Comment) Organism
recombinant HDAC1, HDAC8, HDAC6 and HDAC7 Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
docking studies of the representative compound 4 to the homology model of HDAC1 and the X-ray structures of HDAH, PDB 1ZZ1, and HDAC8, PDB 1T67 Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
2,2,3,3,4,4,5,5,6,6,7,7-dodecafluorooctanedioic acid (3,4-dimethylphenyl)-amide hydroxyamide
-
 Homo sapiens
2,2,3,3,4,4,5,5,6,6,7,7-dodecafluorooctanedioic acid biphenyl-2-ylamide hydroxyamide
-
 Homo sapiens
2,2,3,3,4,4,5,5,6,6,7,7-dodecafluorooctanedioic acid hydroxyamide (4-phenylthiazol-2-yl)amide
-
 Homo sapiens
2,2,3,3,4,4,5,5,6,6,7,7-dodecafluorooctanedioic acid hydroxyamide phenyl-amide competitive. Significant but rather unselective inhibition of cellular HDACs Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.03
-
 benzyloxycarbonyl-L-Lys(trifluoroacetyl)-7-amido-4-methylcoumarin isoform HDAC8, 37°C, pH not specified in the publication Homo sapiens
0.061
-
 benzyloxycarbonyl-L-Lys(trifluoroacetyl)-7-amido-4-methylcoumarin isoform HDAC7, 37°C, pH not specified in the publication Homo sapiens
0.078
-
 benzyloxycarbonyl-L-Lys(acetyl)-7-amido-4-methylcoumarin isoform HDAC1, 37°C, pH not specified in the publication Homo sapiens
0.099
-
 benzyloxycarbonyl-L-Lys(acetyl)-7-amido-4-methylcoumarin isoform HDAC6, 37°C, pH not specified in the publication Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
K-562 cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
benzyloxycarbonyl-L-Lys(acetyl)-7-amido-4-methylcoumarin + H2O
-
 Homo sapiens benzyloxycarbonyl-L-Lys-7-amido-4-methylcoumarin + acetate
-
 ?
benzyloxycarbonyl-L-Lys(trifluoroacetyl)-7-amido-4-methylcoumarin + H2O
-
 Homo sapiens benzyloxycarbonyl-L-Lys-7-amido-4-methylcoumarin + trifluoroacetate
-
 ?

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0014
-
 2,2,3,3,4,4,5,5,6,6,7,7-dodecafluorooctanedioic acid hydroxyamide (4-phenylthiazol-2-yl)amide isoform HDAC7, 37°C, pH not specified in the publication Homo sapiens
0.0015
-
 2,2,3,3,4,4,5,5,6,6,7,7-dodecafluorooctanedioic acid hydroxyamide (4-phenylthiazol-2-yl)amide isoform HDAC8, 37°C, pH not specified in the publication Homo sapiens
0.0026
-
 2,2,3,3,4,4,5,5,6,6,7,7-dodecafluorooctanedioic acid hydroxyamide (4-phenylthiazol-2-yl)amide isoform HDAC1, 37°C, pH not specified in the publication Homo sapiens
0.0033
-
 2,2,3,3,4,4,5,5,6,6,7,7-dodecafluorooctanedioic acid (3,4-dimethylphenyl)-amide hydroxyamide isoform HDAC7, 37°C, pH not specified in the publication Homo sapiens
0.0053
-
 2,2,3,3,4,4,5,5,6,6,7,7-dodecafluorooctanedioic acid biphenyl-2-ylamide hydroxyamide isoform HDAC8, 37°C, pH not specified in the publication Homo sapiens
0.0054
-
 2,2,3,3,4,4,5,5,6,6,7,7-dodecafluorooctanedioic acid hydroxyamide (4-phenylthiazol-2-yl)amide isoform HDAC6, 37°C, pH not specified in the publication Homo sapiens
0.0088
-
 2,2,3,3,4,4,5,5,6,6,7,7-dodecafluorooctanedioic acid (3,4-dimethylphenyl)-amide hydroxyamide isoform HDAC1, 37°C, pH not specified in the publication Homo sapiens
0.0092
-
 2,2,3,3,4,4,5,5,6,6,7,7-dodecafluorooctanedioic acid biphenyl-2-ylamide hydroxyamide isoform HDAC6, 37°C, pH not specified in the publication Homo sapiens
0.011
-
 2,2,3,3,4,4,5,5,6,6,7,7-dodecafluorooctanedioic acid hydroxyamide phenyl-amide isoform HDAC6, 37°C, pH not specified in the publication Homo sapiens
0.011
-
 2,2,3,3,4,4,5,5,6,6,7,7-dodecafluorooctanedioic acid hydroxyamide phenyl-amide isoform HDAC7, 37°C, pH not specified in the publication Homo sapiens
0.014
-
 2,2,3,3,4,4,5,5,6,6,7,7-dodecafluorooctanedioic acid biphenyl-2-ylamide hydroxyamide isoform HDAC7, 37°C, pH not specified in the publication Homo sapiens
0.014
-
 2,2,3,3,4,4,5,5,6,6,7,7-dodecafluorooctanedioic acid (3,4-dimethylphenyl)-amide hydroxyamide isoform HDAC8, 37°C, pH not specified in the publication Homo sapiens
0.017
-
 2,2,3,3,4,4,5,5,6,6,7,7-dodecafluorooctanedioic acid hydroxyamide phenyl-amide isoform HDAC8, 37°C, pH not specified in the publication Homo sapiens
0.024
-
 2,2,3,3,4,4,5,5,6,6,7,7-dodecafluorooctanedioic acid (3,4-dimethylphenyl)-amide hydroxyamide isoform HDAC6, 37°C, pH not specified in the publication Homo sapiens
0.029
-
 2,2,3,3,4,4,5,5,6,6,7,7-dodecafluorooctanedioic acid hydroxyamide phenyl-amide isoform HDAC1, 37°C, pH not specified in the publication Homo sapiens
0.049
-
 2,2,3,3,4,4,5,5,6,6,7,7-dodecafluorooctanedioic acid biphenyl-2-ylamide hydroxyamide isoform HDAC1, 37°C, pH not specified in the publication Homo sapiens