Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(2E,4E,6S)-6-[(2-oxohexadecanoyl)amino]deca-2,4-dienoic acid | reduces the cellular release of arachidonic acid by 6% | Homo sapiens | |
(2E,4S)-4-[(2-oxohexadecanoyl)amino]oct-2-enoic acid | reduces the cellular release of arachidonic acid by 74% | Homo sapiens | |
(4R)-6-methyl-4-[(2-oxohexadecanoyl)amino]heptanoic acid | reduces the cellular release of arachidonic acid by 62% | Homo sapiens | |
(4S)-4-[(2-oxododecanoyl)amino]octanoic acid | reduces the cellular release of arachidonic acid by 56% | Homo sapiens | |
(4S)-4-[(2-oxohexadecanoyl)amino]octanoic acid | reduces the cellular release of arachidonic acid by 79% | Homo sapiens | |
(5S)-5-[(2-oxohexadecanoyl)amino]nonanoic acid | reduces the cellular release of arachidonic acid by 59% | Homo sapiens | |
(S)-2-(2-(2-oxohexadecanamido)hexanamido)acetic acid | contains a free carboxyl group, inhibits GIVA cPLA2 without affecting the activity of the other intracellular enzyme GVIA iPLA2 | Homo sapiens | |
(S)-2-(2-(2-oxohexadecanamido)hexyloxy)acetic acid | selectively inhibits GIVA cPLA2, due to its free carboxyl group. Most potent inhibitor of GIVA cPLA2. Reduces the cellular release of arachidonic acid by 68% | Homo sapiens | |
(S)-2-(3-methyl-2-(2-oxohexadecanamido)butanamido)acetic acid | contains a free carboxyl group, inhibits GIVA cPLA2 without affecting the activity of the other intracellular enzyme GVIA iPLA2 | Homo sapiens | |
(S)-ethyl 2-(2-(2-oxohexadecanamido)hexanamido)acetate | ethyl ester based on Nle-Gly dipeptide, potent inhibition of GVIA iPLA2, inhibits GIVA cPLA2 (73%) and GV sPLA2 (63%) | Homo sapiens | |
(S)-ethyl 2-(2-(2-oxohexadecanamido)hexyloxy)acetate | preferentially inhibits GVIA iPLA2, is a potent inhibitor of GVIA iPLA2, inhibits GIVA cPLA2 by 52% and GV sPLA2 by 81% | Homo sapiens | |
(S)-methyl 2-(2-(2-oxohexadecanamido)hexanamido)acetate | methyl ester based on dipeptide Nle-Gly, inhibits both GIVA cPLA2 and GVIA iPLA2, showing a small preference for GIVA cPLA2, inhibits GV sPLA2 by 65% | Homo sapiens | |
(S)-methyl 2-(3-methyl-2-(2-oxohexadecanamido)butanamido)acetate | methyl ester based on dipeptide Val-Gly, inhibits activity of GIVA cPLA2 by 25% | Homo sapiens | |
(S)-tert-butyl 2-(2-(2-oxohexadecanamido)hexanamido)acetate | tert-butyl ester based on Nle-Gly dipeptide, potent inhibition of GVIA iPLA2, inhibits GIVA cPLA2 (72%) and GV sPLA2 (59%) | Homo sapiens | |
(S)-tert-butyl 2-(2-(2-oxohexadecanamido)hexyloxy)acetate | preferentially inhibits GVIA iPLA2 (81% inhibition), inhibits GIVA cPLA2 by 44% and GV sPLA2 by 57% | Homo sapiens | |
(S)-tert-butyl 2-(3-methyl-2-(2-oxohexadecanamido)butanamido)acetate | tert-butyl ester based on dipeptide Val-Gly, inhibits both GIVA cPLA2 and GVIA iPLA2, showing a small preference for GIVA cPLA2, reduces GV sPLA2 activity by 78%. Reduces the cellular release of arachidonic acid by 30% | Homo sapiens | |
4-[(2-oxohexadecanoyl)amino]butanoic acid | reduces the cellular release of arachidonic acid by 52% | Homo sapiens | |
AX006 | inhibits GIVA cPLA2 | Homo sapiens | |
AX048 | inhibits GIVA cPLA2 and GVIA iPLA2 | Homo sapiens | |
ethyl (2E,4S)-4-[(2-oxohexadecanoyl)amino]oct-2-enoate | reduces the cellular release of arachidonic acid by 16% | Homo sapiens | |
methyl N-(2-oxohexadecanoyl)glycinate | reduces the cellular release of arachidonic acid by 30% | Homo sapiens | |
additional information | replacement of the amino acid unit of a 2-oxoamide inhibitor by a dipeptide unit may shift the selectivity in favour of GVIA iPLA2 | Homo sapiens | |
N-(2-oxododecanoyl)-L-norleucine | reduces the cellular release of arachidonic acid by 21% | Homo sapiens | |
tert-butyl 5-[(2-oxohexadecanoyl)amino]pentanoate | reduces the cellular release of arachidonic acid by 11% | Homo sapiens |
Localization | Comment | Organism | GeneOntology No. | Textmining |
---|
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
macrophage | primary lung macrophage | Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
1-palmitoyl-2-arachidonoylglycerophosphocholine + H2O | GIVA cPLA2 substrate and GIVA iPLA2 | Homo sapiens | 1-palmitoyl-glycerophosphorylcholine + arachidonic acid | - |
? | |
dipalmitoyl-phosphatidylcholine + H2O | GIVA iPLA2 and GV sPLA2 | Homo sapiens | 1-palmitoyl-glycerophosphocholine + palmitic acid | - |
? |
Synonyms | Comment | Organism |
---|---|---|
GIVA cPLA2 | - |
Homo sapiens |
GV sPLA2 | - |
Homo sapiens |
GVIA iPLA2 | - |
Homo sapiens |
phospholipase A2 | - |
Homo sapiens |
secretory phospholipase A2 | - |
Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.002 | - |
at 37°C, pH not specified in the publication | Homo sapiens | (S)-2-(2-(2-oxohexadecanamido)hexyloxy)acetic acid | |
0.007 | - |
at 37°C, pH not specified in the publication | Homo sapiens | (5S)-5-[(2-oxohexadecanoyl)amino]nonanoic acid | |
0.01 | - |
at 37°C, pH not specified in the publication | Homo sapiens | (4S)-4-[(2-oxododecanoyl)amino]octanoic acid | |
0.025 | - |
at 37°C, pH not specified in the publication | Homo sapiens | 4-[(2-oxohexadecanoyl)amino]butanoic acid | |
0.025 | - |
at 37°C, pH not specified in the publication | Homo sapiens | (4R)-6-methyl-4-[(2-oxohexadecanoyl)amino]heptanoic acid | |
0.025 | - |
at 37°C, pH not specified in the publication | Homo sapiens | (4S)-4-[(2-oxohexadecanoyl)amino]octanoic acid | |
0.025 | - |
at 37°C, pH not specified in the publication | Homo sapiens | (2E,4S)-4-[(2-oxohexadecanoyl)amino]oct-2-enoic acid |