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Literature summary for 3.5.1.98 extracted from

  • Guan, P.; Sun, F.; Hou, X.; Wang, F.; Yi, F.; Xu, W.; Fang, H.
    Design, synthesis and preliminary bioactivity studies of 1,3,4-thiadiazole hydroxamic acid derivatives as novel histone deacetylase inhibitors (2012), Bioorg. Med. Chem., 20, 3865-3872.
    View publication on PubMed
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Inhibitors

Inhibitors Comment Organism Structure
(E)-N1-hydroxy-N5-(5-styryl-1,3,4-thiadiazol-2-yl)glutaramide antiproliferative activities against MDA-MB-231 and K562 cell lines, IC50 0.0059 and 0.00675 microM, respectively Homo sapiens
additional information presence of 5-6 carbon units between the Zn2+ binding group and the 1,3,4-thiadiazole ring is optimal for inhibitory potency Homo sapiens
N1-(5-benzyl-1,3,4-thiadiazol-2-yl)-N7-hydroxyheptanediamide antiproliferative activities against MDA-MB-231 and K562 cell lines, IC50 0.0061 and 0.0122 microM, respectively Homo sapiens
N1-(5-benzyl-1,3,4-thiadiazol-2-yl)-N8-hydroxyoctanediamide antiproliferative activities against MDA-MB-231 and K562 cell lines, IC50 0.00298 and 0.0091 microM, respectively Homo sapiens
N1-hydroxy-N7-(5-phenyl-1,3,4-thiadiazol-2-yl)heptanediamide antiproliferative activities against MDA-MB-231 and K562 cell lines, IC50 0.0055 and 0.0129 microM, respectively Homo sapiens
N1-hydroxy-N8-(5-phenyl-1,3,4-thiadiazol-2-yl)octanediamide
-
 Homo sapiens
suberoylanilide hydroxamic acid i.e. SAHA, antiproliferative activities against MDA-MB-231 and K562 cell lines, IC50 0.00132 and 0.00169 microM, respectively Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
HeLa cell
-
 Homo sapiens
-
K-562 cell
-
 Homo sapiens
-
MDA-MB-231 cell
-
 Homo sapiens
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000089
-
 HDAC from HeLa cell nucleus extracts, mainly including HDAC1 and HDAC2, 37°C, pH not specified in the publication Homo sapiens N1-hydroxy-N7-(5-phenyl-1,3,4-thiadiazol-2-yl)heptanediamide
0.00015
-
 HDAC from HeLa cell nucleus extracts, mainly including HDAC1 and HDAC2, 37°C, pH not specified in the publication Homo sapiens suberoylanilide hydroxamic acid
0.00016
-
 HDAC from HeLa cell nucleus extracts, mainly including HDAC1 and HDAC2, 37°C, pH not specified in the publication Homo sapiens (E)-N1-hydroxy-N5-(5-styryl-1,3,4-thiadiazol-2-yl)glutaramide
0.00022
-
 HDAC from HeLa cell nucleus extracts, mainly including HDAC1 and HDAC2, 37°C, pH not specified in the publication Homo sapiens N1-(5-benzyl-1,3,4-thiadiazol-2-yl)-N7-hydroxyheptanediamide
0.00026
-
 HDAC from HeLa cell nucleus extracts, mainly including HDAC1 and HDAC2, 37°C, pH not specified in the publication Homo sapiens N1-(5-benzyl-1,3,4-thiadiazol-2-yl)-N8-hydroxyoctanediamide
0.00027
-
 HDAC from HeLa cell nucleus extracts, mainly including HDAC1 and HDAC2, 37°C, pH not specified in the publication Homo sapiens N1-hydroxy-N8-(5-phenyl-1,3,4-thiadiazol-2-yl)octanediamide