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Literature summary for 2.5.1.18 extracted from

  • Ricci, G.; De Maria, F.; Antonini, G.; Turella, P.; Bullo, A.; Stella, L.; Filomeni, G.; Federici, G.; Caccuri, A.M.
    7-Nitro-2,1,3-benzoxadiazole derivatives, a new class of suicide inhibitors for glutathione S-transferases. Mechanism of action of potential anticancer drugs (2005), J. Biol. Chem., 280, 26397-26405.
    View publication on PubMed
Search for more literature for 2.5.1.18

Inhibitors

Inhibitors Comment Organism Structure
2-(7-nitro-2,1,3-benzoxadiazol-4-ylthio)imidazole
-
 Homo sapiens
3-(7-nitro-2,1,3-benzoxadiazol-4-ylthio)propionic acid
-
 Homo sapiens
4-(7-nitro-2,1,3-benzoxadiazol-4-ylthio)butanol
-
 Homo sapiens
6-(7-nitro-2,1,3-benzoxadiazol-4-ylamino)hexanol
-
 Homo sapiens
6-(7-nitro-2,1,3-benzoxadiazol-4-ylthio)hexanol
-
 Homo sapiens
7-nitro-2,1,3-benzoxadiazole derivatives non-GSH peptidomimetic compounds, suicide inhibitors of the enzyme, binding structure and mechanism, overview, the compounds show strong GST inhibition and accumulation in tumor cells avoiding the extrusion mechanisms mediated by the multidrug resistance protein pumps Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
additional information
-
 additional information stopped flow rapid kinetics, overview Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
 isozymes GSTA1-1, GSTM2-2, and GSTP1-1
-

Source Tissue

Source Tissue Comment Organism Textmining
GLC-4 cell a small cell lung carcinoma cell line Homo sapiens
-
Hep-G2 cell a hepatic carcinoma cell line Homo sapiens
-
K-562 cell a myeloid leukemia cell line Homo sapiens
-

Synonyms

Synonyms Comment Organism
glutathione S-transferase
-
 Homo sapiens
GST
-
 Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
25
-
 assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
6.5
-
 assay at Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
additional information
-
 additional information inhibition kinetics Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00001
-
 pH 6.5, 25°C, recombinant isoyzme GSTP1-1 Homo sapiens 6-(7-nitro-2,1,3-benzoxadiazol-4-ylthio)hexanol
0.00001
-
 pH 6.5, 25°C, recombinant isoyzme GSTP1-1 Homo sapiens 2-(7-nitro-2,1,3-benzoxadiazol-4-ylthio)imidazole
0.00003
-
 pH 6.5, 25°C, recombinant isoyzme GSTP1-1 Homo sapiens 4-(7-nitro-2,1,3-benzoxadiazol-4-ylthio)butanol
0.0003
-
 pH 6.5, 25°C, recombinant isoyzme GSTP1-1 Homo sapiens 3-(7-nitro-2,1,3-benzoxadiazol-4-ylthio)propionic acid
0.0008
-
 pH 6.5, 25°C, recombinant isoyzme GSTM2-2 Homo sapiens 6-(7-nitro-2,1,3-benzoxadiazol-4-ylthio)hexanol
0.0018
-
 pH 6.5, 25°C, recombinant isoyzme GSTP1-1 Homo sapiens 6-(7-nitro-2,1,3-benzoxadiazol-4-ylamino)hexanol
0.002
-
 pH 6.5, 25°C, recombinant isoyzme GSTM2-2 Homo sapiens 4-(7-nitro-2,1,3-benzoxadiazol-4-ylthio)butanol
0.0057
-
 pH 6.5, 25°C, recombinant isoyzme GSTM2-2 Homo sapiens 3-(7-nitro-2,1,3-benzoxadiazol-4-ylthio)propionic acid
0.0063
-
 pH 6.5, 25°C, recombinant isoyzme GSTM2-2 Homo sapiens 2-(7-nitro-2,1,3-benzoxadiazol-4-ylthio)imidazole
0.011
-
 pH 6.5, 25°C, recombinant isoyzme GSTA1-1 Homo sapiens 2-(7-nitro-2,1,3-benzoxadiazol-4-ylthio)imidazole
0.025
-
 pH 6.5, 25°C, recombinant isoyzme GSTA1-1 Homo sapiens 6-(7-nitro-2,1,3-benzoxadiazol-4-ylthio)hexanol
0.056
-
 pH 6.5, 25°C, recombinant isoyzme GSTA1-1 Homo sapiens 4-(7-nitro-2,1,3-benzoxadiazol-4-ylthio)butanol
0.066
-
 pH 6.5, 25°C, recombinant isoyzme GSTA1-1 Homo sapiens 3-(7-nitro-2,1,3-benzoxadiazol-4-ylthio)propionic acid
0.1
-
 above, pH 6.5, 25°C, recombinant isoyzme GSTA1-1 Homo sapiens 6-(7-nitro-2,1,3-benzoxadiazol-4-ylamino)hexanol
0.1
-
 above, pH 6.5, 25°C, recombinant isoyzme GSTM2-2 Homo sapiens 6-(7-nitro-2,1,3-benzoxadiazol-4-ylamino)hexanol