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Literature summary for 3.5.1.98 extracted from

  • Jones, P.; Altamura, S.; De Francesco, R.; Paz, O.G.; Kinzel, O.; Mesiti, G.; Monteagudo, E.; Pescatore, G.; Rowley, M.; Verdirame, M.; Steinkuehler, C.
    A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo (2008), J. Med. Chem., 51, 2350-2353.
    View publication on PubMed
Search for more literature for 3.5.1.98

Application

Application Comment Organism
medicine HDAC inhibitors offer a promising strategy for cancer therapy Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(2S)-8-oxo-2-[(3-piperidin-1-ylpropanoyl)amino]-N-quinolin-3-ylnonanamide
-
 Homo sapiens
1-methyl-N-[(1S)-7-oxo-1-[(4-phenyl-1,3-thiazol-2-yl)carbamoyl]octyl]piperidine-2-carboxamide
-
 Homo sapiens
2-(5-methoxy-2-methyl-1H-indol-3-yl)-N-[(1S)-7-oxo-1-(5-phenyl-1H-imidazol-2-yl)nonyl]acetamide
-
 Homo sapiens
2-(5-methoxy-2-methyl-1H-indol-3-yl)-N-[(1S)-7-oxo-1-(5-phenyl-1H-imidazol-2-yl)octyl]acetamide
-
 Homo sapiens
apicidin
-
 Homo sapiens
azumamide A
-
 Homo sapiens
azumamide E
-
 Homo sapiens
FK-228
-
 Homo sapiens
FR235222
-
 Homo sapiens
HC-toxin
-
 Homo sapiens
LBH-589
-
 Homo sapiens
MGCD-0103
-
 Homo sapiens
MS-275
-
 Homo sapiens
N-[(1S)-1-(6-chloro-1H-benzimidazol-2-yl)-7-oxooctyl]-2-(5-methoxy-2-methyl-1H-indol-3-yl)acetamide
-
 Homo sapiens
PXD-101
-
 Homo sapiens
vorinostat
-
 Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Zn2+
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
additional information Homo sapiens the acetylation status of lysine residues in nucleosomal proteins is tightly controlled by two counteracting enzyme families, the histone acetyl transferases and the histone deacetylases, HDACs ?
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
A-2780 cell
-
 Homo sapiens
-
A-549 cell
-
 Homo sapiens
-
G-401 cell
-
 Homo sapiens
-
HCT-116 cell
-
 Homo sapiens
-
HeLa cell
-
 Homo sapiens
-
renal epithelium cell line
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information the acetylation status of lysine residues in nucleosomal proteins is tightly controlled by two counteracting enzyme families, the histone acetyl transferases and the histone deacetylases, HDACs Homo sapiens ?
-
 ?

Synonyms

Synonyms Comment Organism
HDAC
-
 Homo sapiens
histone deacetylase
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000026
-
 HDAC1 Homo sapiens 2-(5-methoxy-2-methyl-1H-indol-3-yl)-N-[(1S)-7-oxo-1-(5-phenyl-1H-imidazol-2-yl)nonyl]acetamide
0.00003
-
 HDAC1 Homo sapiens vorinostat
0.000043
-
 HDAC6 Homo sapiens vorinostat
0.000044
-
 HDAC1 Homo sapiens apicidin
0.000048
-
 HDAC3 Homo sapiens 2-(5-methoxy-2-methyl-1H-indol-3-yl)-N-[(1S)-7-oxo-1-(5-phenyl-1H-imidazol-2-yl)nonyl]acetamide
0.000055
-
 HDAC1 Homo sapiens 1-methyl-N-[(1S)-7-oxo-1-[(4-phenyl-1,3-thiazol-2-yl)carbamoyl]octyl]piperidine-2-carboxamide
0.000057
-
 HDAC3 Homo sapiens vorinostat
0.000059
-
 HDAC1 Homo sapiens 2-(5-methoxy-2-methyl-1H-indol-3-yl)-N-[(1S)-7-oxo-1-(5-phenyl-1H-imidazol-2-yl)octyl]acetamide
0.000059
-
 HDAC2 Homo sapiens 2-(5-methoxy-2-methyl-1H-indol-3-yl)-N-[(1S)-7-oxo-1-(5-phenyl-1H-imidazol-2-yl)nonyl]acetamide
0.000082
-
 HDAC2 Homo sapiens vorinostat
0.00011
-
 HDAC2 Homo sapiens 2-(5-methoxy-2-methyl-1H-indol-3-yl)-N-[(1S)-7-oxo-1-(5-phenyl-1H-imidazol-2-yl)octyl]acetamide
0.00012
-
 HDAC1 Homo sapiens MS-275
0.00012
-
 HDAC3 Homo sapiens 2-(5-methoxy-2-methyl-1H-indol-3-yl)-N-[(1S)-7-oxo-1-(5-phenyl-1H-imidazol-2-yl)octyl]acetamide
0.00014
-
 HDAC1 Homo sapiens (2S)-8-oxo-2-[(3-piperidin-1-ylpropanoyl)amino]-N-quinolin-3-ylnonanamide
0.00025
-
 HDAC2 Homo sapiens MS-275
0.00034
-
 HDAC6 Homo sapiens 2-(5-methoxy-2-methyl-1H-indol-3-yl)-N-[(1S)-7-oxo-1-(5-phenyl-1H-imidazol-2-yl)octyl]acetamide
0.0004
-
 HDAC3 Homo sapiens MS-275
0.00067
-
 HDAC1 Homo sapiens N-[(1S)-1-(6-chloro-1H-benzimidazol-2-yl)-7-oxooctyl]-2-(5-methoxy-2-methyl-1H-indol-3-yl)acetamide
0.00088
-
 HDAC2 Homo sapiens N-[(1S)-1-(6-chloro-1H-benzimidazol-2-yl)-7-oxooctyl]-2-(5-methoxy-2-methyl-1H-indol-3-yl)acetamide
0.00097
-
 HDAC6 Homo sapiens N-[(1S)-1-(6-chloro-1H-benzimidazol-2-yl)-7-oxooctyl]-2-(5-methoxy-2-methyl-1H-indol-3-yl)acetamide
0.001
-
 HDAC3 Homo sapiens N-[(1S)-1-(6-chloro-1H-benzimidazol-2-yl)-7-oxooctyl]-2-(5-methoxy-2-methyl-1H-indol-3-yl)acetamide
0.0017
-
 HDAC8 Homo sapiens vorinostat
0.005
-
 HDAC8, larger than 0.005 Homo sapiens 2-(5-methoxy-2-methyl-1H-indol-3-yl)-N-[(1S)-7-oxo-1-(5-phenyl-1H-imidazol-2-yl)octyl]acetamide
0.01
-
 HDAC5, larger than 0.010 Homo sapiens MS-275
0.01
-
 HDAC5, larger than 0.010 Homo sapiens 2-(5-methoxy-2-methyl-1H-indol-3-yl)-N-[(1S)-7-oxo-1-(5-phenyl-1H-imidazol-2-yl)octyl]acetamide
0.01
-
 HDAC5, larger than 0.010 Homo sapiens N-[(1S)-1-(6-chloro-1H-benzimidazol-2-yl)-7-oxooctyl]-2-(5-methoxy-2-methyl-1H-indol-3-yl)acetamide
0.01
-
 HDAC5, larger than 0.010 Homo sapiens 2-(5-methoxy-2-methyl-1H-indol-3-yl)-N-[(1S)-7-oxo-1-(5-phenyl-1H-imidazol-2-yl)nonyl]acetamide
0.01
-
 HDAC6, larger than 0.010 Homo sapiens MS-275
0.01
-
 HDAC7, larger than 0.010 Homo sapiens MS-275
0.01
-
 HDAC7, larger than 0.010 Homo sapiens vorinostat
0.01
-
 HDAC7, larger than 0.010 Homo sapiens 2-(5-methoxy-2-methyl-1H-indol-3-yl)-N-[(1S)-7-oxo-1-(5-phenyl-1H-imidazol-2-yl)octyl]acetamide
0.01
-
 HDAC7, larger than 0.010 Homo sapiens N-[(1S)-1-(6-chloro-1H-benzimidazol-2-yl)-7-oxooctyl]-2-(5-methoxy-2-methyl-1H-indol-3-yl)acetamide
0.01
-
 HDAC7, larger than 0.010 Homo sapiens 2-(5-methoxy-2-methyl-1H-indol-3-yl)-N-[(1S)-7-oxo-1-(5-phenyl-1H-imidazol-2-yl)nonyl]acetamide
0.01
-
 HDAC8, larger than 0.010 Homo sapiens MS-275
0.01
-
 HDAC8, larger than 0.010 Homo sapiens N-[(1S)-1-(6-chloro-1H-benzimidazol-2-yl)-7-oxooctyl]-2-(5-methoxy-2-methyl-1H-indol-3-yl)acetamide