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Literature summary for 2.8.2.15 extracted from

  • Senggunprai, L.; Yoshinari, K.; Yamazoe, Y.
    Inhibitory effects of kynurenic acid, a tryptophan metabolite, and its derivatives on cytosolic sulfotransferases (2009), Biochem. J., 422, 455-462.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Escherichia coli BL21(DE3) cells Mus musculus
expressed in Escherichia coli BL21(DE3) cells Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
2,6-Dichloro-4-nitrophenol non-specific SULT inhibitor Homo sapiens
5,7-dichlorokynurenic acid
-
Homo sapiens
5,7-dichlorokynurenic acid
-
Mus musculus
gavestinel i.e. 4,6-dichloro-3-[(1E)-3-oxo-3-(phenylamino)-1-propenyl]-1H-indole-2-carboxylic acid sodium salt Homo sapiens
gavestinel i.e. 4,6-dichloro-3-[(1E)-3-oxo-3-(phenylamino)-1-propenyl]-1H-indole-2-carboxylic acid sodium salt Mus musculus
Kynurenic acid exhibits selective inhibitory effects on Sult1b1-mediated sulfation of various compounds with IC50 values in the low micromolar range Homo sapiens
Kynurenic acid
-
Mus musculus
L689,560 i.e. trans-2-carboxy-5,7-dichloro-4-phenylaminocarboxylamino-1,2,3,4-tetrahydroquinoline Homo sapiens
L689,560 i.e. trans-2-carboxy-5,7-dichloro-4-phenylaminocarboxylamino-1,2,3,4-tetrahydroquinoline Mus musculus
L701,324 i.e. 7-chloro-4-hydroxy-3(3-phenoxy)phenyl-2(H)-quinolinone Homo sapiens
L701,324 i.e. 7-chloro-4-hydroxy-3(3-phenoxy)phenyl-2(H)-quinolinone Mus musculus
Mefenamic acid
-
Homo sapiens
Mefenamic acid
-
Mus musculus

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0012
-
1-naphthol isoform SULT1B1, in 50 mM Tris/HCl buffer, pH 7.4, 1 mM dithiothreitol, 5 mM MgCl2, and 1 mg/ml bovine serum albumin, at 37°C Homo sapiens
0.0051
-
dehydroepiandrosterone isoform SULT2A1, in 50 mM Tris/HCl buffer, pH 7.4, 1 mM dithiothreitol, 5 mM MgCl2, and 1 mg/ml bovine serum albumin, at 37°C Mus musculus
0.0063
-
xanthurenic acid isoform SULT1B1, in 50 mM Tris/HCl buffer, pH 7.4, 1 mM dithiothreitol, 5 mM MgCl2, and 1 mg/ml bovine serum albumin, at 37°C Homo sapiens
0.015
-
xanthurenic acid isoform Sult1d1, in 50 mM Tris/HCl buffer, pH 7.4, 1 mM dithiothreitol, 5 mM MgCl2, and 1 mg/ml bovine serum albumin, at 37°C Mus musculus
0.0209
-
3,4-dihydroxyphenylacetic acid isoform Sult1d1, in 50 mM Tris/HCl buffer, pH 7.4, 1 mM dithiothreitol, 5 mM MgCl2, and 1 mg/ml bovine serum albumin, at 37°C Mus musculus
0.0399
-
4-nitrophenol isoform SULT1B1, in 50 mM Tris/HCl buffer, pH 7.4, 1 mM dithiothreitol, 5 mM MgCl2, and 1 mg/ml bovine serum albumin, at 37°C Homo sapiens
0.145
-
L-triiodothyronine isoform SULT1B1, in 50 mM Tris/HCl buffer, pH 7.4, 1 mM dithiothreitol, 5 mM MgCl2, and 1 mg/ml bovine serum albumin, at 37°C Homo sapiens
0.206
-
xanthurenic acid isoform SULT1C2, in 50 mM Tris/HCl buffer, pH 7.4, 1 mM dithiothreitol, 5 mM MgCl2, and 1 mg/ml bovine serum albumin, at 37°C Homo sapiens
0.238
-
3-(10,11-dihydro-5H-dibenzo[b,f]azepin-5-yl)-N-methylpropan-1-amine isoform Sult2a1, in 50 mM Tris/HCl buffer, pH 10.0, 1 mM dithiothreitol, 5 mM MgCl2, and 1 mg/ml bovine serum albumin, at 37°C Mus musculus

Localization

Localization Comment Organism GeneOntology No. Textmining
cytosol
-
Mus musculus 5829
-
cytosol
-
Homo sapiens 5829
-

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
3'-phosphoadenylyl sulfate + 1-naphthol Mus musculus
-
adenosine 3',5'-bisphosphate + 1-naphthyl sulfate
-
?
3'-phosphoadenylyl sulfate + 1-naphthol Homo sapiens
-
adenosine 3',5'-bisphosphate + 1-naphthyl sulfate
-
?
3'-phosphoadenylyl sulfate + 3,4-dihydroxyphenylacetic acid Mus musculus
-
adenosine 3',5'-bisphosphate + ?
-
?
3'-phosphoadenylyl sulfate + 3,4-dihydroxyphenylacetic acid Homo sapiens
-
adenosine 3',5'-bisphosphate + ?
-
?
3'-phosphoadenylyl sulfate + 4-nitrophenol Mus musculus
-
adenosine 3',5'-bisphosphate + 4-nitrophenyl sulfate
-
?
3'-phosphoadenylyl sulfate + 4-nitrophenol Homo sapiens
-
adenosine 3',5'-bisphosphate + 4-nitrophenyl sulfate
-
?
3'-phosphoadenylyl sulfate + beta-estradiol Mus musculus
-
adenosine 3',5'-bisphosphate + beta-estradiol 3-sulfate
-
?
3'-phosphoadenylyl sulfate + beta-estradiol Homo sapiens
-
adenosine 3',5'-bisphosphate + beta-estradiol 3-sulfate
-
?
3'-phosphoadenylyl sulfate + dehydroepiandrosterone Mus musculus
-
adenosine 3',5'-bisphosphate + ?
-
?
3'-phosphoadenylyl sulfate + dehydroepiandrosterone Homo sapiens
-
adenosine 3',5'-bisphosphate + ?
-
?
3'-phosphoadenylyl sulfate + desipramine Mus musculus
-
adenosine 3',5'-bisphosphate + ?
-
?
3'-phosphoadenylyl sulfate + desipramine Homo sapiens
-
adenosine 3',5'-bisphosphate + ?
-
?
3'-phosphoadenylyl sulfate + L-triiodothyronine Mus musculus
-
adenosine 3',5'-bisphosphate + ?
-
?
3'-phosphoadenylyl sulfate + L-triiodothyronine Homo sapiens
-
adenosine 3',5'-bisphosphate + ?
-
?
3'-phosphoadenylyl sulfate + xanthurenic acid Mus musculus
-
adenosine 3',5'-bisphosphate + ?
-
?
3'-phosphoadenylyl sulfate + xanthurenic acid Homo sapiens
-
adenosine 3',5'-bisphosphate + ?
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Mus musculus
-
-
-

Purification (Commentary)

Purification (Comment) Organism
Ni-NTA agarose column chromatography Mus musculus
Ni-NTA agarose column chromatography Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3'-phosphoadenylyl sulfate + 1-naphthol
-
Mus musculus adenosine 3',5'-bisphosphate + 1-naphthyl sulfate
-
?
3'-phosphoadenylyl sulfate + 1-naphthol
-
Homo sapiens adenosine 3',5'-bisphosphate + 1-naphthyl sulfate
-
?
3'-phosphoadenylyl sulfate + 3,4-dihydroxyphenylacetic acid
-
Mus musculus adenosine 3',5'-bisphosphate + ?
-
?
3'-phosphoadenylyl sulfate + 3,4-dihydroxyphenylacetic acid
-
Homo sapiens adenosine 3',5'-bisphosphate + ?
-
?
3'-phosphoadenylyl sulfate + 4-nitrophenol
-
Mus musculus adenosine 3',5'-bisphosphate + 4-nitrophenyl sulfate
-
?
3'-phosphoadenylyl sulfate + 4-nitrophenol
-
Homo sapiens adenosine 3',5'-bisphosphate + 4-nitrophenyl sulfate
-
?
3'-phosphoadenylyl sulfate + beta-estradiol
-
Mus musculus adenosine 3',5'-bisphosphate + beta-estradiol 3-sulfate
-
?
3'-phosphoadenylyl sulfate + beta-estradiol
-
Homo sapiens adenosine 3',5'-bisphosphate + beta-estradiol 3-sulfate
-
?
3'-phosphoadenylyl sulfate + dehydroepiandrosterone
-
Mus musculus adenosine 3',5'-bisphosphate + ?
-
?
3'-phosphoadenylyl sulfate + dehydroepiandrosterone
-
Homo sapiens adenosine 3',5'-bisphosphate + ?
-
?
3'-phosphoadenylyl sulfate + desipramine
-
Mus musculus adenosine 3',5'-bisphosphate + ?
-
?
3'-phosphoadenylyl sulfate + desipramine
-
Homo sapiens adenosine 3',5'-bisphosphate + ?
-
?
3'-phosphoadenylyl sulfate + L-triiodothyronine
-
Mus musculus adenosine 3',5'-bisphosphate + ?
-
?
3'-phosphoadenylyl sulfate + L-triiodothyronine
-
Homo sapiens adenosine 3',5'-bisphosphate + ?
-
?
3'-phosphoadenylyl sulfate + xanthurenic acid
-
Mus musculus adenosine 3',5'-bisphosphate + ?
-
?
3'-phosphoadenylyl sulfate + xanthurenic acid
-
Homo sapiens adenosine 3',5'-bisphosphate + ?
-
?

Synonyms

Synonyms Comment Organism
cytosolic sulfotransferase
-
Mus musculus
cytosolic sulfotransferase
-
Homo sapiens
SULT1B1 isoform Homo sapiens
SULT1C2 isoform Homo sapiens
SULT1D1 isoform Mus musculus
SULT2A1 isoform Mus musculus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0012
-
isoform SULT1B1, using L-triiodothyronine as substrate, in 50 mM Tris/HCl buffer, pH 7.4, 1 mM dithiothreitol, 5 mM MgCl2, and 1 mg/ml bovine serum albumin, at 37°C Homo sapiens gavestinel
0.0017
-
isoform SULT1B1, using xanthurenic acid as substrate, in 50 mM Tris/HCl buffer, pH 7.4, 1 mM dithiothreitol, 5 mM MgCl2, and 1 mg/ml bovine serum albumin, at 37°C Homo sapiens gavestinel
0.005
-
IC50 above 0.005 mM, isoform SULT1B1, using L-triiodothyronine as substrate, in 50 mM Tris/HCl buffer, pH 7.4, 1 mM dithiothreitol, 5 mM MgCl2, and 1 mg/ml bovine serum albumin, at 37°C Homo sapiens Mefenamic acid
0.005
-
IC50 above 0.005 mM, isoform SULT1B1, using xanthurenic acid as substrate, in 50 mM Tris/HCl buffer, pH 7.4, 1 mM dithiothreitol, 5 mM MgCl2, and 1 mg/ml bovine serum albumin, at 37°C Homo sapiens Mefenamic acid
0.0337
-
isoform SULT1B1, using xanthurenic acid as substrate, in 50 mM Tris/HCl buffer, pH 7.4, 1 mM dithiothreitol, 5 mM MgCl2, and 1 mg/ml bovine serum albumin, at 37°C Homo sapiens Kynurenic acid
0.0342
-
isoform SULT1B1, using xanthurenic acid as substrate, in 50 mM Tris/HCl buffer, pH 7.4, 1 mM dithiothreitol, 5 mM MgCl2, and 1 mg/ml bovine serum albumin, at 37°C Homo sapiens 2,6-Dichloro-4-nitrophenol
0.0473
-
isoform SULT1B1, using xanthurenic acid as substrate, in 50 mM Tris/HCl buffer, pH 7.4, 1 mM dithiothreitol, 5 mM MgCl2, and 1 mg/ml bovine serum albumin, at 37°C Homo sapiens L689,560
0.0536
-
isoform SULT1B1, using L-triiodothyronine as substrate, in 50 mM Tris/HCl buffer, pH 7.4, 1 mM dithiothreitol, 5 mM MgCl2, and 1 mg/ml bovine serum albumin, at 37°C Homo sapiens L689,560
0.1642
-
isoform SULT1B1, using L-triiodothyronine as substrate, in 50 mM Tris/HCl buffer, pH 7.4, 1 mM dithiothreitol, 5 mM MgCl2, and 1 mg/ml bovine serum albumin, at 37°C Homo sapiens 5,7-dichlorokynurenic acid
0.2536
-
isoform SULT1B1, using xanthurenic acid as substrate, in 50 mM Tris/HCl buffer, pH 7.4, 1 mM dithiothreitol, 5 mM MgCl2, and 1 mg/ml bovine serum albumin, at 37°C Homo sapiens 5,7-dichlorokynurenic acid
9
-
isoform SULT1B1, using L-triiodothyronine as substrate, in 50 mM Tris/HCl buffer, pH 7.4, 1 mM dithiothreitol, 5 mM MgCl2, and 1 mg/ml bovine serum albumin, at 37°C Homo sapiens Kynurenic acid
24
-
isoform SULT1B1, using L-triiodothyronine as substrate, in 50 mM Tris/HCl buffer, pH 7.4, 1 mM dithiothreitol, 5 mM MgCl2, and 1 mg/ml bovine serum albumin, at 37°C Homo sapiens 2,6-Dichloro-4-nitrophenol