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Literature summary extracted from

  • Wang, J.; Williams, E.T.; Bourgea, J.; Wong, Y.N.; Patten, C.J.
    Characterization of recombinant human carboxylesterases: fluorescein diacetate as a probe substrate for human carboxylesterase 2 (2011), Drug Metab. Dispos., 39, 1329-1333.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
3.1.1.1 expressed in baculovirus-infected High Five insect cells Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.1.1.1 bis(4-nitrophenyl)phosphate potent inhibitor Homo sapiens
3.1.1.1 loperamide inhibitor of isoform CES2 Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
3.1.1.1 0.00194
-
 fluorescein diacetate isoform CES1-b, in 0.1 M potassium phosphate buffer, pH 7.4, at 37°C Homo sapiens
3.1.1.1 0.00431
-
 fluorescein diacetate isoform CES1-c, in 0.1 M potassium phosphate buffer, pH 7.4, at 37°C Homo sapiens
3.1.1.1 0.00482
-
 fluorescein diacetate isoform CES2, in 0.1 M potassium phosphate buffer, pH 7.4, at 37°C Homo sapiens
3.1.1.1 0.173
-
 4-nitrophenyl acetate isoform CES2, in 0.1 M potassium phosphate buffer, pH 7.4, at 37°C Homo sapiens
3.1.1.1 0.208
-
 4-nitrophenyl acetate isoform CES1-b, in 0.1 M potassium phosphate buffer, pH 7.4, at 37°C Homo sapiens
3.1.1.1 0.441
-
 4-nitrophenyl acetate isoform CES1-c, in 0.1 M potassium phosphate buffer, pH 7.4, at 37°C Homo sapiens

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
3.1.1.1 microsome
-
 Homo sapiens
-
-

Organism

EC Number Organism UniProt Comment Textmining
3.1.1.1 Homo sapiens
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.1.1.1 liver CES1-b is the predominant form in human liver Homo sapiens
-
3.1.1.1 small intestine
-
 Homo sapiens
-

Specific Activity [micromol/min/mg]

EC Number Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
3.1.1.1 0.099
-
 isoform CES2, using methyl 4-nitrobenzoate as substrate, in 0.1 M potassium phosphate buffer, pH 7.4, at 37°C Homo sapiens
3.1.1.1 0.281
-
 isoform CES1-c, fluorescein diacetate as substrate, in 0.1 M potassium phosphate buffer, pH 7.4, at 37°C Homo sapiens
3.1.1.1 0.357
-
 isoform CES1-b, using fluorescein diacetate as substrate, in 0.1 M potassium phosphate buffer, pH 7.4, at 37°C Homo sapiens
3.1.1.1 0.68
-
 isoform CES1-c, methyl 4-nitrobenzoate as substrate, in 0.1 M potassium phosphate buffer, pH 7.4, at 37°C Homo sapiens
3.1.1.1 0.682
-
 isoform CES2, using 4-nitrophenyl acetate as substrate, in 0.1 M potassium phosphate buffer, pH 7.4, at 37°C Homo sapiens
3.1.1.1 0.957
-
 isoform CES1-b, using methyl 4-nitrobenzoate as substrate, in 0.1 M potassium phosphate buffer, pH 7.4, at 37°C Homo sapiens
3.1.1.1 1.4
-
 isoform CES1-c, using 4-nitrophenyl acetate as substrate, in 0.1 M potassium phosphate buffer, pH 7.4, at 37°C Homo sapiens
3.1.1.1 1.43
-
 isoform CES1-b, using 4-nitrophenyl acetate as substrate, in 0.1 M potassium phosphate buffer, pH 7.4, at 37°C Homo sapiens
3.1.1.1 13.8
-
 isoform CES2, using fluorescein diacetate as substrate, in 0.1 M potassium phosphate buffer, pH 7.4, at 37°C Homo sapiens

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.1.1.1 4-nitrophenyl acetate + H2O substrate for both isoform CES1 and CES2 Homo sapiens 4-nitrophenol + acetate
-
 ?
3.1.1.1 fluorescein diacetate + H2O specific probe substrate for isoform CES2 Homo sapiens ?
-
 ?
3.1.1.1 methyl 4-nitrobenzoate + H2O specific substrate for isoform ES1 Homo sapiens 4-nitrobenzoate + methanol
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.1.1.1 carboxylesterase 2
-
 Homo sapiens
3.1.1.1 CES1 isoform Homo sapiens
3.1.1.1 CES1-b carboxylesterase 1 form b Homo sapiens
3.1.1.1 CES1-c carboxylesterase 1 form c Homo sapiens
3.1.1.1 CES2 isoform Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.1.1.1 0.0000104
-
 isoform CES2, in 0.1 M potassium phosphate buffer, pH 7.4, at 37°C Homo sapiens bis(4-nitrophenyl)phosphate
3.1.1.1 0.0000236
-
 isoform CES1-b, in 0.1 M potassium phosphate buffer, pH 7.4, at 37°C Homo sapiens bis(4-nitrophenyl)phosphate
3.1.1.1 0.000287
-
 isoform CES2, in 0.1 M potassium phosphate buffer, pH 7.4, at 37°C Homo sapiens loperamide
3.1.1.1 0.000788
-
 isoform CES1-c, in 0.1 M potassium phosphate buffer, pH 7.4, at 37°C Homo sapiens bis(4-nitrophenyl)phosphate
3.1.1.1 0.1
-
 IC50 above 0.1 mM, isoform CES1-b, in 0.1 M potassium phosphate buffer, pH 7.4, at 37°C Homo sapiens loperamide
3.1.1.1 0.1
-
 IC50 above 0.1 mM, isoform CES1-c, in 0.1 M potassium phosphate buffer, pH 7.4, at 37°C Homo sapiens loperamide