Literature summary extracted from
Wang, Y.; Chanda, P.; Jones, P.G.; Kennedy, J.D.
A fluorescence-based assay for monoacylglycerol lipase compatible with inhibitor screening (2008), Assay Drug Dev. Technol., 6, 387-393.
Activating Compound
EC Number |
Activating Compound |
Comment |
Organism |
Structure |
---|
3.1.1.23 |
bovine serum albumin |
MAGL activity increases with increasing concentration up to 1% |
Homo sapiens |
|
3.1.1.23 |
additional information |
dimethyl sulfoxide concentrations up to 10% of the final assay volume have no effect on MAGL activity, the inclusion of dimethyl sulfoxide in the assay can increase the solubility of hydrophobic compounds |
Homo sapiens |
|
Cloned(Commentary)
EC Number |
Cloned (Comment) |
Organism |
---|
3.1.1.23 |
into vector pColdII with a His6 tag at the N-terminus. Expression in Escherichia coli BL21 (DE3) competent cells |
Homo sapiens |
Inhibitors
EC Number |
Inhibitors |
Comment |
Organism |
Structure |
---|
3.1.1.23 |
additional information |
URB754 does not inhibit MAGL activity at concentrations up to 0.100 mM. Assay buffer alone or heat-denatured MAGL protein has no significant activity against 7-hydroxycoumarinyl-arachidonate |
Homo sapiens |
|
3.1.1.23 |
N-arachidonyl maleimide |
potent irreversible inhibitor of MAGL, inhibits in a dose-dependent manner |
Homo sapiens |
|
3.1.1.23 |
URB602 |
specific inhibitor of MAGL, inhibits in a dose-dependent manner |
Homo sapiens |
|
KM Value [mM]
EC Number |
KM Value [mM] |
KM Value Maximum [mM] |
Substrate |
Comment |
Organism |
Structure |
---|
3.1.1.23 |
0.0098 |
- |
7-hydroxycoumarinyl arachidonate |
at pH 8 and 25°C, in 10% dimethyl sulfoxide |
Homo sapiens |
|
Molecular Weight [Da]
EC Number |
Molecular Weight [Da] |
Molecular Weight Maximum [Da] |
Comment |
Organism |
---|
3.1.1.23 |
33000 |
- |
x * 33000, MAGL-His6 protein, SDS-PAGE |
Homo sapiens |
Organism
EC Number |
Organism |
UniProt |
Comment |
Textmining |
---|
3.1.1.23 |
Homo sapiens |
- |
- |
- |
Purification (Commentary)
EC Number |
Purification (Comment) |
Organism |
---|
3.1.1.23 |
MAGL-His6 protein purified on nickel-nitrilotriacetic acid column, more than 90% pure |
Homo sapiens |
Substrates and Products (Substrate)
EC Number |
Substrates |
Comment Substrates |
Organism |
Products |
Comment (Products) |
Rev. |
Reac. |
---|
3.1.1.23 |
7-hydroxycoumarinyl arachidonate |
- |
Homo sapiens |
arachidonic acid + 7-hydroxycoumarin |
- |
? |
|
Subunits
EC Number |
Subunits |
Comment |
Organism |
---|
3.1.1.23 |
? |
x * 33000, MAGL-His6 protein, SDS-PAGE |
Homo sapiens |
Synonyms
EC Number |
Synonyms |
Comment |
Organism |
---|
3.1.1.23 |
MAGL |
- |
Homo sapiens |
3.1.1.23 |
monoacylglycerol lipase |
- |
Homo sapiens |
pH Range
EC Number |
pH Minimum |
pH Maximum |
Comment |
Organism |
---|
3.1.1.23 |
8 |
10 |
activity peak of 7-hydroxycoumarinyl-arachidonate hydrolysis by MAGL |
Homo sapiens |
IC50 Value
EC Number |
IC50 Value |
IC50 Value Maximum |
Comment |
Organism |
Inhibitor |
Structure |
---|
3.1.1.23 |
0.000155 |
- |
in 50 mM HEPES buffer, pH 8, 1 mM EDTA, and 10% dimethyl sulfoxide at 25°C for 60 min |
Homo sapiens |
N-arachidonyl maleimide |
|
3.1.1.23 |
0.0031 |
- |
in 50 mM HEPES buffer, pH 8, 1 mM EDTA, and 10% dimethyl sulfoxide at 25°C for 60 min |
Homo sapiens |
URB602 |
|