Any feedback?
Please rate this page
(all_enzymes.php)
(0/150)

BRENDA support

3.1.1.4: phospholipase A2

This is an abbreviated version!
For detailed information about phospholipase A2, go to the full flat file.

Word Map on EC 3.1.1.4

Reaction

phosphatidylcholine
+
H2O
=
1-acylglycerophosphocholine
 +
a carboxylate

Synonyms

1-CysPrx, 1-cysteine peroxiredoxin, 14 kDa phospholipase A2, A2-IIA, Acanmyotoxin-1, acidic Asp49 phospholipase A2, acidic Ca2+-independent phospholipase A2, acidic phospholipase A2, ACS, adiponutrin, AdPLA, Agkistrotoxin, AgkTx-II, aiPLA2, alpha-type phospholipase A2, amdI1, Ammodytin I2, ammodytoxin A, APLA, APP-D-49, Arg49 phospholipase A2, Arg49 phospholipase A2 homologue, Asp49 basic myotoxic PLA2, Asp49 PLA2, Asp49-PLA2, ASPLA1, ASPLA10, ASPLA11, ASPLA12, ASPLA13, ASPLA14, ASPLA15, ASPLA16, ASPLA17, ASPLA2, ASPLA3, ASPLA4, ASPLA5, ASPLA6, ASPLA7, ASPLA8, ASPLA9, Ats-PLA2-alpha, AtsPLA2-alpha, AtsPLA2-gamma, ATX, BaltPLA2, basic Asp49 PLA2, Basic protein I/II, BaTX, BinTx-I, BinTx-II, BJ-PLA2, Bj-V, BJUPLA2, Bothropstoxin-I, BPI/BPII, BthTX, BthTX-1, BthTX-I, BthTX-II, bvPLA2, Ca+2-independent PLA2, Ca2+ independent PLA2, Ca2+-independent iPLA2, Ca2+-independent phospholipase A2, Ca2+-independent PLA2, CaI-PLA2, calcium-d-independent cytosolic PLA2, calcium-dependent cytosolic PLA2, calcium-independent group VIA iPLA2, calcium-independent phospholipase A2, Caudoxin, Cdt PLA2, class XIB phospholipase A2, ColTx-I, cPLA2, cPLA2 alpha, cPLA2-alpha, cPLA2-gamma, cPLA2-zeta2, cPLA2alpha, cPLA2beta, cPLA2delta, cPLA2epsilon, cPLA2zeta, cPm09, Cr-IV 1, Cro, crotapotin, crotoxin, CTX, cytoplasmic phospholipase A2, cytosolic calcium-dependent PLA2, cytosolic cPLA2, cytosolic gIVaPLA2, cytosolic group IVA cPLA2, cytosolic group IVa phospholipase A2, cytosolic phospholipase A2, cytosolic phospholipase A2 alpha, cytosolic phospholipase A2-alpha, cytosolic phospholipase A2alpha, cytosolic PLA2, cytotoxin ExoU, Daboxin P, DrK-aI, DrK-aII, DrK-bI, DrK-bII, DrPLA2, DsM-bI, DsM-S1, Enhancing factor, exoenzyme U, ExoU, ExoU-specific PLA2, GIA cobra venom PLA2, GIIA, GIIA PLA2, GIIA sPLA2, GIIC sPLA2, GIID, GIID sPLA2, GIIE, GIIE sPLA2, GIIF, GIIF sPLA2, GIII sPLA2, GIIIsPLA2, GIVA, GIVA cPLA2, GIVA phospholipase A2, GIVA PLA2, GIVD cPLA2delta, GIVF, Gln49-PLA2, group IA PLA2, Group IB phospholipase A2, group IB PLA2, group II snake venom phospholipase A2, Group IIA phospholipase A2, group IIA PLA2, group IIA secretory phospholipase A2, group IIA secretory PLA2, group IID secretory phospholipase A2, group III Glu62-phospholipase A2, group III PLA2, group III sPLA2, group IV cPLA2, group IVA cPLA2, group IVA cytosolic phospholipase A2, group IVA phospholipase A2, group IVA PLA2, group IVB phospholipase A2, Group V phospholipase A2, group V secreted phospholipase A2, Group VI phospholipase A2, Group VIA Ankyrin-1, Group VIA Ankyrin-2, group VIA calcium-independent phospholipase A, group VIA cPLA2, group VIA phospholipase A2, Group VIA PLA2, Group VIA-3, group X secreted phospholipase A2, GS2, GV sPLA2, GVI PLA2, GVIA, GVIA iPLA2, GVIA PLA2, GVIA-iPLA2, GVIIA PLA2, GX, GX sPLA2, GXII sPLA2, GXIIA, GXIII sPLA2, hGX sPLA2, hIBPLA2, hIIAPLA2, human group IB PLA2, human group IIA phospholipase A2, IB PLA2, immune-associated phospholipase A2, imperatoxin, intercro, IPLA-1, iPLA2, iPLA2-gamma, jerdoxin, lecithinase A, lipoprotein associated phospholipase A2, lipoprotein-associated phospholipase A2, lipoprotein-associated PLA2, LLPL, LM-PLA2-I, LM-PLA2-II, LmTX-I, LmTX-II, Lp-PLA2, Lpla2, Lys49 phospholipase A2 homologue, Lys49-phospholipase A2 homologue, Lys49-PLA2, lysophospholipase, lysosomal phospholipase A2, lysosomal PLA2, mAoPlaA, marine snail digestive phospholipase A2, megacin A-216, MiDCA1, milleporin-1, MjTX-II, More, MP-III 4R, mSDPL, MsPLA2-I, Muscarinic inhibitor, mycotoxin II, myotoxic Asp49-phospholipase A2, myotoxic phospholipase A2, Myotoxin, myotoxin I, NAJPLA-2A, NAJPLA-2B, NAJPLA-2C, natratoxin, neuropathy target esterase, neutral anticoagulant secretory phospholipase A2, Nigexine, NK-PLA2-I, NK-PLA2-II, NN-X-PLA2, NN-XI-PLA2, NN-XIa-PLA2, NND-IV-PLA2, Non-pancreatic secretory phospholipase A2, Notechis 11'2, Notexin, notexinII-1, NPLA, NPS-PLA2, OHV A-PLA2, OHV-APLA2, OPLA2, PAF acetyl hydrolase/oxidized lipid LpPLA2, PAF-AH, pancreatic phospholipase A2, pancreatic-type PLA2, patatin, peroxiredoxin 6, pgPLA 1a/pgPLA 2a, PhlA, phosphatidase, phosphatide 2-acylhydrolase, phosphatidolipase, Phosphatidylcholine 2-acylhydrolase, Phosphatidylcholine 2-acylhydrolase GIIC, Phosphatidylcholine 2-acylhydrolase GIID, Phosphatidylcholine 2-acylhydrolase GIIE, Phosphatidylcholine 2-acylhydrolase GIIF, Phosphatidylcholine 2-acylhydrolase GIII, Phosphatidylcholine 2-acylhydrolase GX, Phosphatidylcholine 2-acylhydrolase GXII, Phosphatidylcholine 2-acylhydrolase GXIII, phospholipase A, phospholipase A2, phospholipase A2 D49, phospholipase A2 gamma, Phospholipase A2 inhibitor, phospholipase A2 neurotoxin, phospholipase A2 PA-11, phospholipase A2alpha, phospholipase A2IValpha, phospholipase A2s, phospholipin, pkP5, Pla, PLA1, PLA2, PLA2 CM2, PLA2 neurotoxin, PLA2-10, PLA2-1B, PLA2-2A, PLA2-2C, PLA2-H, PLA2-I, PLA2-L, PLA2-V, PLA2-VI, PLA2-VII, PLA2alpha, PLA2G1B, PLA2G2D, Pla2g4a, Pla2g4b, PLA2G4C, PLA2G4D, PLA2G6, PLA2IID, PLA2III, PLA2IValpha, PLA2s, platelet activating factor acetyl hydrolase, platelet activating factor acetyl hydrolase/oxidized lipid LpPLA2, platelet-activating factor acetylhydrolase, platlet-activating factor acetylhydrolase, plpA, ppPLA2, Prdx6, promutoxin, PrTX-1, PrTX-I, PrTX-III, Pt-PLA1, Pt-PLA2, R49 PLA2, RVV acidic PLA2-I, RVV-7, RVVA-PLA2-I, SCO1048 protein, Scol/Pla, secreted group IID phospholipase A2, secreted human phospholipase A2, secreted phospholipase A2, secreted phospholipaseA2 neurotoxin, secreted phospholipases A2, secreted PLA2, secreted sPLA2, secretory Ca2+-dependent PLA2, secretory phospholipase, secretory phospholipase A2, secretory phospholipase A2 group IIA, secretory phospholipase A2 type IB, secretory phospholipase A2 type IIA, secretory phospholipase A2-alpha, secretory PLA2s, Secretory-type PLA, stroma-associated homolog, snake presynoptic phospholipase A2 neurotoxin, SPAN, specific phospholipase A2, sPLA(2), sPLA(2)-IID, sPLA(2)-IIE, sPLA(2)-IIF, sPLA-V, sPLA2, sPLA2 GIB, sPLA2 GIIA, sPLA2 IB, sPLA2 type IIA, sPLA2(IIA), sPLA2-IB, sPLA2-IIA, sPLA2-IID, sPLA2-IIE, sPLA2-IIF, sPLA2-V, sPLA2-X, sPLA2:, sPLA2IB2, svPLA2, taipoxin, textilotoxin, thrombin inhibitor from Naja haje, TI-Nh, TMV-K49, toxin I, Toxin VI, Toxin VI:5, TPP, trimorphin, TTS-2.2, Tx-1, TX-I, type III cytotoxin, type VIIA PLA2, zhaoermiatoxin

ECTree

     3 Hydrolases
         3.1 Acting on ester bonds
             3.1.1 Carboxylic-ester hydrolases
                3.1.1.4 phospholipase A2

Inhibitors

Inhibitors on EC 3.1.1.4 - phospholipase A2

Please wait a moment until all data is loaded. This message will disappear when all data is loaded.
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(+-)-3-O-[4-(4,5-dihydro-5-oxo-1,2,4-4H-oxadiazol-3-yl)phenyl]-2-O-tetradecyl-1-O-triphenylmethylglycerol
(2-(2-amino-2-oxoethyl)-5-propyl-1H-indol-7-yl)acetic acid
-
(2-(4-((3-(diphenylmethyl)-2,4-dioxo-3,4-dihydroquinazolin-1(2H)-yl)methyl)phenyl)-1,3-oxazol-4-yl)acetic acid
-
-
(2E,4E,6S)-6-[(2-oxohexadecanoyl)amino]deca-2,4-dienoic acid
-
reduces the cellular release of arachidonic acid by 6%
(2E,4S)-4-[(2-oxohexadecanoyl)amino]oct-2-enoic acid
-
reduces the cellular release of arachidonic acid by 74%
(3-aminooxalyl-1-benzyl-2-ethyl-6-methyl-1H-indol-4-yl)oxyacetic acid methyl ester
-
LY374388, potent sPLA2 inhibitor
(3E)-3-[(3aS,7aS)-3-methyl-2-oxo-6-(propan-2-ylidene)hexahydro-1-benzofuran-7(4H)-ylidene]propanoic acid
-
non-competitive inhibition
(3R,3aS,5aS,8bR)-3,5a,5b-trimethyl-3a,4,5,5a,5b,8b-hexahydro-2H-cyclopenta[2,3]cyclopropa[1,2-g]benzofuran-2,6(3H)-dione
-
non-competitive inhibition
(3R,3aS,5aS,9bR)-3,5a,9-trimethyl-3a,4,5,5a-tetrahydronaphtho[1,2-b]furan-2,8(3H,9bH)-dione
-
non-competitive inhibition
(3R,3aS,6R,8S,9bS)-6,8-dihydroxy-3,6,9-trimethyl-3,3a,4,5,6,6a,7,8-octahydroazuleno[4,5-b]furan-2(9bH)-one
-
non-competitive inhibition
(3R,3aS,6R,8S,9bS)-8-hydroxy-3,6,9-trimethyl-2-oxo-2,3,3a,4,5,6,6a,7,8,9b-decahydroazuleno[4,5-b]furan-6-yl acetate
-
-
(3R,3aS,6R,9bS)-3,6,9-trimethyl-2,8-dioxo-2,3,3a,4,5,6,6a,7,8,9b-decahydroazuleno[4,5-b]furan-6-yl acetate
-
-
(3R,3aS,6R,9bS)-6-hydroxy-3,6,9-trimethyl-3a,4,5,6,6a,7-hexahydroazuleno[4,5-b]furan-2,8(3H,9bH)-dione
-
-
(3S)-4-[(4-benzylphenyl)sulfanyl]-3-[(7-phenylheptanoyl)amino]butane-1-sulfonic acid
bioisosteric replacements, binding energy of -22.05 kJ/mol
(3S)-4-[(4-benzylphenyl)sulfanyl]-3-[(7-phenylheptanoyl)amino]butyl phosphonic acid
bioisosteric replacements, binding energy of -19.76 kJ/mol
(3S)-4-[(4-benzylphenyl)sulfanyl]-3-[[7-(4-hydroxyphenyl)heptanoyl]amino]butane-1-sulfonic acid
bioisosteric replacements, molecular structure is characterized by a chiral centre of absolute (R)-configuration, four carbons in the R1 chain, a hydroxyl group as a substituent in the para-position of the phenyl ring in R1 chain and a sulphonate group instead of the carboxylate group, indicates the highest binding energy (-29.1 kJ/mol) than all the other analogues and the prototype
(3S)-5a-(1-bromo-1-methylethyl)-3-methyl-3,3a,5,5a,8,9b-hexahydro-4H-furo[2,3-f]chromene-2,7-dione
-
non-competitive inhibition
(4-((3-(diphenylmethyl)-2,4-dioxo-3,4-dihydroquinazolin-1(2H)-yl)methyl)phenoxy)acetic acid
-
-
(4-((3-(diphenylmethyl)-2,4-dioxo-3,4-dihydroquinazolin-1(2H)-yl)methyl)phenyl)acetic acid
-
-
(4-((6-bromo-1-(diphenylmethyl)-2,4-dioxo-1,4-dihydroquinazolin-3(2H)-yl)methyl)phenyl)acetic acid
-
-
(4R)-5-[(4-benzylphenyl)sulfanyl]-4-[(7-phenylheptanoyl)amino]pentanoic acid
(R)-configuration of FPL67047XX, binding energy of -19.5 kJ/mol
(4R)-6-methyl-4-[(2-oxohexadecanoyl)amino]heptanoic acid
-
reduces the cellular release of arachidonic acid by 62%
(4S)-4-[(2-oxododecanoyl)amino]octanoic acid
-
reduces the cellular release of arachidonic acid by 56%
(4S)-4-[(2-oxohexadecanoyl)amino]nonanoic acid
-
-
(4S)-4-[(2-oxohexadecanoyl)amino]octanoic acid
-
reduces the cellular release of arachidonic acid by 79%
(4S)-5-[(4-benzylphenyl)sulfanyl]-4-[(5-phenylpentanoyl)amino]pentanoic acid
decreased carbon chain length between the amide group and the aromatic ring of the R1 chain, binding energy of -22.02 kJ/mol
(4S)-5-[(4-benzylphenyl)sulfanyl]-4-[[7-(4-hydroxyphenyl)heptanoyl]amino]pentanoic acid
substituents in the para-position of the aromatic ring R1, higher binding energy (-27.61 kJ/mol) than the prototype and all the other analogues except structure 9
(4S)-5-[(4-benzylphenyl)sulfanyl]-4-[[7-(4-methoxyphenyl)heptanoyl]amino]pentanoic acid
substituents in the para-position of the aromatic ring R1, binding energy of -22.23 kJ/mol
(4S)-5-[(4-benzylphenyl)sulfanyl]-4-[[7-(4-nitrophenyl)heptanoyl]amino]pentanoic acid
substituents in the para-position of the aromatic ring R1, binding energy of -20.25 kJ/mol
(5S)-5-[(2-oxohexadecanoyl)amino]decanoic acid
-
-
(5S)-5-[(2-oxohexadecanoyl)amino]nonanoic acid
-
reduces the cellular release of arachidonic acid by 59%
(6E)-6-(bromomethylene)-3-(1-naphthyl)tetrahydro-2H-pyran-2-one
-
i.e. BEL, bromoenol lactone suicide inhibitor, alkylates Cys-residues
(6Z,9Z,12Z,15Z)-1,1,1-trifluorohenicosa-6,9,12,15-tetraen-2-one
(9Z)-9-(hydroxyimino)-9H-fluorene-4-carboxamide
-
inhibition of phospholipase A2 activity of cytotoxin ExoU
(E)-6-(bromomethylene)-3-(1-naphthalenyl)-2H-tetrahydropyran-2-one
-
-
(R)-4-(7-phenylheptanamido)octanoic acid
-
-
(R)-gamma-norleucine
-
a highly selective inhibitor of isozyme GV sPLA2
(R)-methyl 6-methyl-4-(2-oxohexadecanamido)heptanoate
-
-
(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
(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%
(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
(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%)
(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%
(S)-ethyl 6-(2-oxohexadecanamido)decanoate
-
-
(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%
(S)-methyl 2-(3-methyl-2-(2-oxohexadecanamido)butanamido)acetate
-
methyl ester based on dipeptide Val-Gly, inhibits activity of GIVA cPLA2 by 25%
(S)-methyl 4-(2-oxohexadecanamido)octanoate
-
-
(S)-methyl 4-(7-phenylheptanamido)octanoate
-
-
(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%)
(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%
(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%
(S)-tert-butyl 4-(2-oxohexadecanamido)pentanoate
-
-
(S,2E,4E)-6-(2-oxohexadecanamido)deca-2,4-dienoic acid
-
-
(S,2E,4E)-ethyl 6-(2-oxohexadecanamido)deca-2,4-dienoate
-
-
([1-[amino(oxo)acetyl]-3-(biphenyl-2-ylmethyl)-2-(2-methylpropyl)indolizin-8-yl]oxy)acetic acid
([3-[amino(oxo)acetyl]-1-benzyl-2-(2-methylpropyl)-1H-benzo[g]indol-4-yl]oxy)acetic acid
1,1,1,2,2-pentafluoro-5-(4-hexyloxy-phenyl)-pentan-3-one
-
-
1,1,1,2,2-pentafluoro-7-phenyl-heptan-3-one
-
a selective inhibitor of GVIA iPLA2
1,1,1,2,2-pentafluoro-8-phenyl-octan-3-one
-
-
1,1,1,2,2-pentafluoro-9-phenyl-nonan-3-one
-
-
1,1,1,2,2-pentafluoro-octadecan-3-one
-
-
1,1,1,3,3-pentafluoro-6-phenyl-hexane-2,2-diol
-
-
1,1,1,3-tetrafluoro-heptadecan-2-one
-
-
1,1,1-trifluoro-4-(4-hexyloxy-phenyl)-butan-2-one
-
-
1,1,1-trifluoro-6-(4-hexyloxy-phenyl)-hexan-2-one
-
-
1,1,1-trifluoro-6-phenylhexan-2-one
-
-
1,1,1-trifluoro-7-phenylheptan-2-one
-
-
1,1,1-trifluoro-8-phenyloctan-2-one
-
-
1,1,1-trifluoroheptadecan-2-one
-
-
1,2-Didecanoin
1,2-dipalmitoyl-phosphatidylcholine
-
large unilamellar vesicles, inhibits hydrolysis of 1,2-dipalmitoyl-phosphatidylcholine small unilamellar vesicles
1,3,5-trihydroxybenzene
-
potent inhibition of enzymatic activity and endemic activity of PLA2, binding structure, overview
1,3-dihydroxy benzene
-
potent inhibition of enzymatic activity and endemic activity of PLA2, binding structure, overview
1-(1H-indazol-1-yl)-3-(4-phenoxyphenoxy)propan-2-one
-
-
1-(2-dimethylaminoethyl)-5-[3-(4-octylphenoxy)-2-oxopropoxy]indole-2-carboxylic acid
-
-
1-(4-carboxybenzyl)-5-[3-(4-octylphenoxy)-2-oxopropoxy]indole-2-carboxylic acid
-
-
1-(4-octylphenoxy)-3-[5-(1H-tetrazol-5-yl)indol-1-yl]propan-2-one
-
inhibits isozyme cPLA2alpha
1-(5-nitro-1H-indazol-1-yl)-3-(4-phenoxyphenoxy)propan-2-one
-
-
1-(9H-fluoren-4-ylcarbonyl)piperidine
-
inhibition of phospholipase A2 activity of cytotoxin ExoU
1-(carboxymethyl)-5-[3-(4-octylphenoxy)-2-oxopropoxy]indole-2-carboxylic acid
-
-
1-(carboxypentyl)-5-[3-(4-octylphenoxy)-2-oxopropoxy]indole-2-carboxylic acid
-
-
1-(carboxypropyl)-5-[3-(4-octylphenoxy)-2-oxopropoxy]indole-2-carboxylic acid
-
-
1-benzyl-5-[3-(4-octylphenoxy)-2-oxopropoxy]-indole-2-carboxylic acid
-
-
1-bromo-2-octanone
-
-
1-H-indole-3-glyoxamide
-
varespladib methyl, potent sPLA2 inhibitor
1-hexadecyl-3-(trifluoroethyl)-sn-glycero-2-phosphomethanol
i.e. MJ33
1-hexadecyl-3-trifluoroethylglycero-sn-2-phosphomethanol
1-hexyl-5-[3-(4-octylphenoxy)-2-oxopropoxy]indole-2-carboxylic acid
-
-
1-methyl 5-[3-(4-octylphenoxy)-2-oxopropoxy]-indole-2-carboxylic acid
-
-
1-palmitoyl-2-arachidonoyl-sn-glycero-3-phosphocholine
-
competitive inhibition of platelet activating factor hydrolysis
1-palmitylthio-2-palmitoylamido-1,2-dideoxy-sn-glycero-3-phosphorylcholine
1-sn-phosphoglycerides
-
-
1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazole-5-carboxylic acid
-
-
1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-benzotriazole-5-carboxylic acid
-
43% metabolic stability in an assay with rat liver microsomes. Thermodynamic solubility is less than 1 microg/ml at pH 7.4
1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-benzotriazole-6-carboxylic acid
-
44% metabolic stability in an assay with rat liver microsomes. Thermodynamic solubility is 2 microg/ml at pH 7.4
1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-carboxylic acid
-
1-[3-(4-octylphenoxy)-2-oxopropyl]-2,3-dihydro-1H-indole-5-carboxylic acid
-
-
1-[3-(4-octylphenoxy)-2-oxopropyl]benzimidazole-5-carboxylic acid
-
49% metabolic stability in an assay with rat liver microsomes, possesses the best thermodynamic solubility (22 microg/ml at pH 7.4)
1-[3-(4-octylphenoxy)-2-oxopropyl]benzimidazole-6-carboxylic acid
-
40% metabolic stability in an assay with rat liver microsomes. Thermodynamic solubility is 7 microg/ml at pH 7.4
1-[3-(4-octylphenoxy)-2-oxopropyl]indazole-5-carboxylic acid
-
reveals the highest cPLA2a inhibitory potency, is 7fold more active than the lead 1-[3-(4-octylphenoxy)-2-oxopropyl]indole-5-carboxylic acid, is the metabolically most stable compound in an assay with rat liver microsomes (64% stability). Thermodynamic solubility is less than 1 microg/ml at pH 7.4
1-[3-(4-octylphenoxy)-2-oxopropyl]indazole-6-carboxylic acid
-
36% metabolic stability in an assay with rat liver microsomes. Thermodynamic solubility is 5 microg/ml at pH 7.4
1-[3-(4-octylphenoxy)-2-oxopropyl]indole-5-carboxylic acid
-
is 7fold less active than 1-[3-(4-octylphenoxy)-2-oxopropyl]indazole-5-carboxylic acid, is the metabolically most stable compound in an assay with rat liver microsomes (65% stability). Thermodynamic solubility is less than 1 microg/ml at pH 7.4
1-[3-(4-octylphenoxy)-2-oxopropyl]indole-5-sulfonamide
-
inhibits isozyme cPLA2alpha
1-[3-(4-octylphenoxy)-2-oxopropyl]indole-6-carboxylic acid
-
39% metabolic stability in an assay with rat liver microsomes. Thermodynamic solubility is less than 1 microg/ml at pH 7.4
1-[3-[4-(decyloxy)phenoxy]-2-oxopropyl]-3-(methoxycarbonyl)-1H-indole-5-carboxylic acid
-
-
1-[5-(morpholine-4-carbonyl)indol-1-yl]-3-(4-octylphenoxy)propan-2-one
-
inhibits isozyme cPLA2alpha
2,2'-biphenyl-3,4'-diylbis(4H-chromen-4-one)
slight inhibition
2,2'-biphenyl-4,4'-diylbis(4H-chromen-4-one)
slight inhibition
2,2'-diphenyl-4H,4'H-6,6'-bichromene-4,4'-dione
slight inhibition
2,4,6-trihydroxy acetophenone
-
potent inhibition of enzymatic activity and endemic activity of PLA2, binding structure, overview
2,4-dihydroxy acetophenone
-
binding structure, overview
2,6-dihydroxy acetophenone
-
binding structure, overview
2-((6-bromo-1-(diphenylmethyl)-2,4-dioxo-1,4-dihydroquinazolin-3(2H)-yl)methyl)cyclopropanecarboxylic acid
-
-
2-(1-benzyl-2-ethyl-4-methoxy-1H-benzo[g]indol-3-yl)-2-oxoacetamide
2-(3-(2-amino-2-oxoacetyl)-1-benzyl-2-ethyl-1H-6,7-benzoindol-4-yloxy)acetic acid
2-([3-[amino(oxo)acetyl]-1-benzyl-2-(2-methylpropyl)-1H-benzo[g]indol-4-yl]oxy)-N-(phenylsulfonyl)acetamide
2-([3-[amino(oxo)acetyl]-1-benzyl-2-(2-methylpropyl)-1H-indol-4-yl]oxy)-N-(methylsulfonyl)propanamide
-
-
2-([3-[amino(oxo)acetyl]-1-benzyl-2-(2-methylpropyl)-1H-indol-4-yl]oxy)-N-(phenylsulfonyl)acetamide
2-([3-[amino(oxo)acetyl]-1-benzyl-2-(2-methylpropyl)-1H-indol-4-yl]oxy)-N-(phenylsulfonyl)propanamide
-
-
2-([3-[amino(oxo)acetyl]-1-benzyl-2-(2-methylpropyl)-1H-indol-4-yl]oxy)-N-[(2-chlorophenyl)sulfonyl]propanamide
-
-
2-([3-[amino(oxo)acetyl]-1-benzyl-2-(2-methylpropyl)-1H-indol-4-yl]oxy)-N-[(2-methylphenyl)sulfonyl]propanamide
-
-
2-([3-[amino(oxo)acetyl]-1-benzyl-2-(2-methylpropyl)-1H-indol-4-yl]oxy)-N-[(3-chlorophenyl)sulfonyl]propanamide
-
-
2-([3-[amino(oxo)acetyl]-1-benzyl-2-(2-methylpropyl)-1H-indol-4-yl]oxy)-N-[(4-chlorophenyl)sulfonyl]propanamide
-
-
2-([3-[amino(oxo)acetyl]-1-benzyl-2-(2-methylpropyl)-1H-indol-4-yl]oxy)-N-[(4-methylphenyl)sulfonyl]propanamide
-
-
2-([3-[amino(oxo)acetyl]-1-benzyl-2-(2-methylpropyl)-1H-indol-4-yl]oxy)-N-[(trifluoromethyl)sulfonyl]propanamide
-
-
2-([3-[amino(oxo)acetyl]-1-benzyl-2-(2-methylpropyl)-1H-indol-4-yl]oxy)-N-[[2-(trifluoromethyl)phenyl]sulfonyl]propanamide
-
-
2-([3-[amino(oxo)acetyl]-1-benzyl-2-ethyl-1H-benzo[g]indol-4-yl]oxy)-N-(phenylsulfonyl)acetamide
2-([3-[amino(oxo)acetyl]-1-benzyl-2-ethyl-1H-indol-4-yl]oxy)-N-(phenylsulfonyl)acetamide
2-hydroxy-N-[1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]acetamide
-
-
2-mercaptoethanol
2-methoxy-N-[1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]acetamide
-
-
2-nitrobenzenesulfonyl fluoride
Bothrops spp.
-
BthTX-I: myotoxic activity reduced to 75% and the cytotoxic activity reduced to 76%
2-oxo-N-(4-oxooctyl)hexadecanamide
-
-
2-tetradecanoylaminohexanol-1-phosphocholine
-
competitive inhibition, R-enantiomer is a more potent inhibitor
2-tetradecanoylaminohexanol-1-phosphoethanolamine
-
competitive inhibition, R-enantiomer is a more potent inhibitor
2-tetradecanoylaminohexanol-1-phosphoglycol
-
competitive inhibition, R-enantiomer is a more potent inhibitor
2-[1-benzyl-2-(2-methylpropyl)-4-(2-oxopropoxy)-1H-indol-3-yl]-2-oxoacetamide
2-[1-benzyl-4-(2-oxopropoxy)-2-propyl-1H-indol-3-yl]-2-oxoacetamide
2-[3-(biphenyl-2-ylmethyl)-2-ethyl-8-(2-oxopropoxy)indolizin-1-yl]-2-oxoacetamide
2-[3-(biphenyl-2-ylmethyl)-2-ethyl-8-methoxyindolizin-1-yl]-2-oxoacetamide
25-O-acetyl-petrosaspongiolide M
an anti-inflammatory marine natural product
3,3'-[[2-(pentyloxy)propane-1,3-diyl]bis(oxybenzene-4,1-diylethane-2,1-diyl)]bis(1,2,4-oxadiazol-5(4H)-one)
3,3'-[[2-(tetradecyloxy)propane-1,3-diyl]bis(oxybenzene-4,1-diylethane-2,1-diyl)]bis(1,2,4-oxadiazol-5(4H)-one)
3,3'-[[2-(tetradecyloxy)propane-1,3-diyl]bis(oxybenzene-4,1-diylmethanediyl)]bis(1,2,4-oxadiazol-5(4H)-one)
3,3'-[[3-(tetradecyloxy)propane-1,2-diyl]bis(oxybenzene-4,1-diylethane-2,1-diyl)]bis(1,2,4-oxadiazol-5(4H)-one)
3,3'-[[3-(tetradecyloxy)propane-1,2-diyl]bis(oxybenzene-4,1-diylmethanediyl)]bis(1,2,4-oxadiazol-5(4H)-one)
3,4-dichloroisocoumarin
3,5-Dibromosalicylate
3,5-diiodosalicylate
3-(((2E)-4-(7-chloro-3-(diphenylmethyl)-2,4-dioxo-3,4-dihydroquinazolin-1(2H)-yl)but-2-en-1-yl)oxy)benzoic acid
-
-
3-(1-benzyl-2,5-dimethylpyrrol-3-yl)-3-(4-fluorophenyl)-3H-isobenzofuran-1-one
-
18% inhibition at 0.033 mM
3-(1-[3-(4-octylphenoxy)-2-oxopropyl]indol-5-yl)-4,5-dihydro-1,2,4-oxadiazol-5-one
-
inhibits isozyme cPLA2alpha
3-(2,5-dimethyl-1-phenylpyrrol-3-yl)-3-(4-fluorophenyl)-3H-isobenzofuran-1-one
-
40% inhibition at 0.033 mM
3-(2,5-dimethylpyrrol-3-yl)-3-(4-fluorophenyl)-3H-isobenzofuran-1-one
-
35% inhibition at 0.033 mM
3-(2-methylpropanoyl)-1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indole-5-carboxylic acid
-
3-(2-methylpropanoyl)-1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-carboxylic acid
-
3-(2-[4-[(4-tetradecylpiperazin-1-yl)carbonyl]phenyl]ethyl)-1,2,4-oxadiazol-5(4H)-one
3-(3-acetamido-2-benzyl-2-ethylindolyl-5-oxy)propane phosphonic acid
-
LY311727, IC50 value of 36 nM, group IIa and V sPLA2
3-(3-carboxypropanoyl)-1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-carboxylic acid
-
3-(3-[4-[(4-tetradecylpiperazin-1-yl)carbonyl]phenyl]propyl)-1,2,4-oxadiazol-5(4H)-one
3-(4-fluorophenyl)-3-(1,2,5-trimethylpyrrol-3-yl)-3H-isobenzofuran-1-one
-
36% inhibition at 0.033 mM
3-(4-fluorophenyl)-3-[1-(3-hydroxyphenyl)-2,5-dimethylpyrrol-3-yl]-3H-isobenzofuran-1-one
-
30% inhibition at 0.033 mM
3-(4-fluorophenyl)-3-[1-(4-hydroxyphenyl)-2,5-dimethylpyrrol-3-yl]-3H-isobenzofuran-1-one
-
60% inhibition at 0.033 mM
3-(4-hydroxybutanoyl)-1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-carboxylic acid
-
3-(4-methoxybutanoyl)-1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-carboxylic acid
-
3-(5-carboxypentanoyl)-1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-carboxylic acid
-
3-(6-hydroxyhexanoyl)-1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-carboxylic acid
-
3-(6-methoxyhexanoyl)-1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-carboxylic acid
-
3-butanoyl-1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-carboxylic acid
-
3-hexanoyl-1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-carboxylic acid
-
3-pyrrol-3-yl-3H-isobenzofuran-1-one
-
synthesis and inhibitory potency of derivatives, overview
3-[(3-cholamidopropyl)-dimethylammonio]-1-propanesulfonate
-
-
3-[1-(3,4-dihydroxyphenyl)-2,5-dimethylpyrrol-3-yl]-3-(4-fluorophenyl)-3H-isobenzofuran-1-one
-
20% inhibition at 0.033 mM
3-[1-(4-aminophenyl)-2,5-dimethylpyrrol-3-yl]-3-(4-fluorophenyl)-3H-isobenzofuran-1-one
-
55% inhibition at 0.033 mM
3-[1-benzyl-3-(carbamoylmethyl)-2-ethylindol-5-yl]oxypropylphosphonic acid
-
LY311727, potent sPLA2 inhibitor
3-[2,5-dimethyl-1-(4-methylaminophenyl)pyrrol-3-yl]-3-(4-fluorophenyl)-3H-isobenzofuran-1-one
-
36% inhibition at 0.033 mM
3-[2-[2-(2,2-diphenylethyl)-3,5-dioxo-1,2,4-oxadiazolidin-4-yl]ethoxy]benzoate
-
-
3-[4'-(hydroxyimino-p-tolyl-methyl)-phenyl]-4-phenyl-sydnone
3-[4'-(hydroxyimino-p-tolyl-methyl)-phenyl]-sydnone
3-[4'-(hydroxyimino-phenyl-methyl)-phenyl]-4-phenyl-sydnone
3-[4'-(hydroxyimino-phenyl-methyl)-phenyl]-sydnone
3-[4-(4-hexadecylpiperazin-1-yl)benzyl]-1,2,4-oxadiazol-5(4H)-one
3-[4-(4-octadecylpiperazin-1-yl)benzyl]-1,2,4-oxadiazol-5(4H)-one
3-[4-(4-oxo-4H-chromen-2-yl)phenyl]-2-phenyl-4H-chromen-4-one
slight inhibition
3-[4-(4-tetradecylpiperazin-1-yl)benzyl]-1,2,4-oxadiazol-5(4H)-one
3-[4-(tetradecyloxy)benzyl]-1,2,4-oxadiazol-5(4H)-one
3-[4-[(4-docosylpiperazin-1-yl)carbonyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
3-[4-[(4-hexadecylpiperazin-1-yl)carbonyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
3-[4-[(4-hexadecylpiperazin-1-yl)carbonyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
3-[4-[(4-hexadecylpiperazin-1-yl)methyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
3-[4-[(4-hexadecylpiperazin-1-yl)methyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
3-[4-[(4-icosylpiperazin-1-yl)carbonyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
3-[4-[(4-octadecylpiperazin-1-yl)carbonyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
3-[4-[(4-octadecylpiperazin-1-yl)carbonyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
3-[4-[(4-octadecylpiperazin-1-yl)methyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
3-[4-[(4-octadecylpiperazin-1-yl)methyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
3-[4-[(4-tetradecylpiperazin-1-yl)carbonyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
3-[4-[(4-tetradecylpiperazin-1-yl)carbonyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
3-[4-[(4-tetradecylpiperazin-1-yl)methyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
3-[4-[(4-tetradecylpiperazin-1-yl)methyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
3-[4-[3-(4-butylphenoxy)-2-(tetradecyloxy)propoxy]benzyl]-1,2,4-oxadiazol-5(4H)-one
3-[4-[3-(4-methylphenoxy)-2-(tetradecyloxy)propoxy]benzyl]-1,2,4-oxadiazol-5(4H)-one
3-[4-[3-(decyloxy)-2-(tetradecyloxy)propoxy]benzyl]-1,2,4-oxadiazol-5(4H)-one
3-[4-[3-(diphenylmethoxy)-2-(tetradecyloxy)propoxy]benzyl]-1,2,4-oxadiazol-5(4H)-one
3-[4-[3-(pentyloxy)-2-(tetradecyloxy)propoxy]benzyl]-1,2,4-oxadiazol-5(4H)-one
3-[4-[3-ethoxy-2-(tetradecyloxy)propoxy]benzyl]-1,2,4-oxadiazol-5(4H)-one
3-[4-[hydroxyimino-(4'-n-butyl-phenyl)-methyl]-phenyl]-4-phenyl-sydnone
3-[4-[hydroxyimino-(4'-n-butyl-phenyl)-methyl]-phenyl]-sydnone
3-[4-[hydroxyimino-(4'-n-propyl-phenyl)-methyl]-phenyl]-4-phenylsydnone
3-[4-[hydroxyimino-(4'-n-propyl-phenyl)-methyl]-phenyl]-sydnone
4-(((2E)-4-(1-(diphenylmethyl)-2,4-dioxo-1,4-dihydroquinazolin-3(2H)-yl)but-2-en-1-yl)oxy)benzoic acid
-
-
4-(((2E)-4-(1-(diphenylmethyl)-6-fluoro-2,4-dioxo-1,4-dihydroquinazolin-3(2H)-yl)but-2-en-1-yl)oxy)benzoic acid
-
-
4-(((2E)-4-(3-(diphenylmethyl)-2,4-dioxo-3,4-dihydroquinazolin-1(2H)-yl)but-2-en-1-yl)oxy)benzoic acid
-
-
4-(((2E)-4-(3-(diphenylmethyl)-2,4-dioxo-7-(1H-1,2,4-triazol-1-yl)-3,4-dihydroquinazolin-1(2H)-yl)but-2-en-1-yl)oxy)benzoic acid
-
-
4-(((2E)-4-(3-(diphenylmethyl)-2,4-dioxo-7-(phenylthio)-3,4-dihydroquinazolin-1(2H)-yl)but-2-en-1-yl)oxy)benzoic acid
-
-
4-(((2E)-4-(3-(diphenylmethyl)-2,4-dioxo-7-phenoxy-3,4-dihydroquinazolin-1(2H)-yl)but-2-en-1-yl)oxy)benzoic acid
-
-
4-(((2E)-4-(3-(diphenylmethyl)-2,4-dioxo-7-thiomorpholin-4-yl-3,4-dihydroquinazolin-1(2H)-yl)but-2-en-1-yl)oxy)benzoic acid
-
-
4-(((2E)-4-(3-(diphenylmethyl)-6-fluoro-2,4-dioxo-3,4-dihydroquinazolin-1(2H)-yl)but-2-en-1-yl)oxy)benzoic acid
-
-
4-(((2E)-4-(3-(diphenylmethyl)-7-(4-(methoxycarbonyl)piperidin-1-yl)-2,4-dioxo-3,4-dihydroquinazolin-1(2H)-yl)but-2-en-1-yl)oxy)benzoic acid
-
-
4-(((2E)-4-(3-(diphenylmethyl)-7-(methylsulfonyl)-2,4-dioxo-3,4-dihydroquinazolin-1(2H)-yl)but-2-en-1-yl)oxy)benzoic acid
-
-
4-(((2E)-4-(3-(diphenylmethyl)-7-(methylthio)-2,4-dioxo-3,4-dihydroquinazolin-1(2H)-yl)but-2-en-1-yl)oxy)benzoic acid
-
-
4-(((2E)-4-(3-(diphenylmethyl)-7-fluoro-2,4-dioxo-3,4-dihydroquinazolin-1(2H)-yl)but-2-en-1-yl)oxy)benzoic acid
-
-
4-(((2E)-4-(3-(diphenylmethyl)-7-methoxy-2,4-dioxo-3,4-dihydroquinazolin-1(2H)-yl)but-2-en-1-yl)oxy)benzoic acid
-
-
4-(((2E)-4-(3-(diphenylmethyl)-7-methyl-2,4-dioxo-3,4-dihydroquinazolin-1(2H)-yl)but-2-en-1-yl)oxy)benzoic acid
-
-
4-(((2E)-4-(3-(diphenylmethyl)-7-morpholin-4-yl-2,4-dioxo-3,4-dihydroquinazolin-1(2H)-yl)but-2-en-1-yl)oxy)benzoic acid
-
-
4-(((2E)-4-(3-(diphenylmethyl)-7-nitro-2,4-dioxo-3,4-dihydroquinazolin-1(2H)-yl)but-2-en-1-yl)oxy)benzoic acid
-
-
4-(((2E)-4-(6-chloro-3-(diphenylmethyl)-2,4-dioxo-3,4-dihydroquinazolin-1(2H)-yl)but-2-en-1-yl)oxy)benzoic acid
-
-
4-(((2E)-4-(7-amino-3-(diphenylmethyl)-2,4-dioxo-3,4-dihydroquinazolin-1(2H)-yl)but-2-en-1-yl)oxy)benzoic acid
-
-
4-(((2E)-4-(7-chloro-1-(diphenylmethyl)-2,4-dioxo-1,4-dihydroquinazolin-3(2H)-yl)but-2-en-1-yl)oxy)benzoic acid
-
-
4-(((2E)-4-(7-chloro-3-(diphenylmethyl)-2,4-dioxo-3,4-dihydroquinazolin-1(2H)-yl)but-2-en-1-yl)oxy)benzoic acid
-
-
4-(((2E)-4-[1-(diphenylmethyl)-2,4-dioxo-1,4-dihydroquinazolin-3(2H)-yl]but-2-en-1-yl)oxy)benzoic acid
-
-
4-(((2E)-4-[3-(diphenylmethyl)-2,4-dioxo-3,4-dihydroquinazolin-1(2H)-yl]but-2-en-1-yl)oxy)benzoic acid
-
-
4-(((2E)-4-[3-(diphenylmethyl)-2,4-dioxo-7-(1H-1,2,4-triazol-1-yl)-3,4-dihydroquinazolin-1(2H)-yl]but-2-en-1-yl)oxy)benzoic acid
-
-
4-(((2E)-4-[3-(diphenylmethyl)-7-fluoro-2,4-dioxo-3,4-dihydroquinazolin-1(2H)-yl]but-2-en-1-yl)oxy)benzoic acid
-
-
4-(((2E)-4-[3-(diphenylmethyl)-7-methoxy-2,4-dioxo-3,4-dihydroquinazolin-1(2H)-yl]but-2-en-1-yl)oxy)benzoic acid
-
-
4-(((2E)-4-[3-(diphenylmethyl)-7-nitro-2,4-dioxo-3,4-dihydroquinazolin-1(2H)-yl]but-2-en-1-yl)oxy)benzoic acid
-
-
4-(((2E)-4-[7-chloro-3-(diphenylmethyl)-2,4-dioxo-3,4-dihydroquinazolin-1(2H)-yl]but-2-en-1-yl)oxy)benzoic acid
-
-
4-(((2Z)-4-(1-(diphenylmethyl)-2,4-dioxo-1,4-dihydroquinazolin-3(2H)-yl)but-2-en-1-yl)oxy)benzoic acid
-
-
4-(((2Z)-4-(3-(diphenylmethyl)-2,4-dioxo-3,4-dihydroquinazolin-1(2H)-yl)but-2-en-1-yl)oxy)benzoic acid
-
-
4-(((2Z)-4-(3-(diphenylmethyl)-6-fluoro-2,4-dioxo-3,4-dihydroquinazolin-1(2H)-yl)but-2-en-1-yl)oxy)benzoic acid
-
-
4-(((2Z)-4-(6-bromo-3-(diphenylmethyl)-2,4-dioxo-3,4-dihydroquinazolin-1(2H)-yl)but-2-en-1-yl)oxy)benzoic acid
-
-
4-(((2Z)-4-(6-chloro-3-(diphenylmethyl)-2,4-dioxo-3,4-dihydroquinazolin-1(2H)-yl)but-2-en-1-yl)oxy)benzoic acid
-
-
4-(((2Z)-4-(7-chloro-1-(diphenylmethyl)-2,4-dioxo-1,4-dihydroquinazolin-3(2H)-yl)but-2-en-1-yl)oxy)benzoic acid
-
-
4-(((2Z)-4-(7-chloro-3-(diphenylmethyl)-2,4-dioxo-3,4-dihydroquinazolin-1(2H)-yl)but-2-en-1-yl)oxy)benzoic acid
-
-
4-(((E)-4-(3-benzhydryl-6-bromo-2,4-dioxo-3,4-dihydro-1(2H)-quinazolinyl)-2-butenyl)oxy)benzoic acid
-
-
4-((5-(3-(diphenylmethyl)-2,4-dioxo-3,4-dihydroquinazolin-1(2H)-yl)pentyl)oxy)benzoic acid
-
-
4-((6-(3-(diphenylmethyl)-2,4-dioxo-3,4-dihydroquinazolin-1(2H)-yl)hexyl)oxy)benzoic acid
-
-
4-((6-chloro-1-(diphenylmethyl)-2,4-dioxo-1,4-dihydroquinazolin-3(2H)-yl)methyl)benzoic acid
-
-
4-((7-(3-(diphenylmethyl)-2,4-dioxo-3,4-dihydroquinazolin-1(2H)-yl)heptyl)oxy)benzoic acid
-
-
4-((7-chloro-1-(diphenylmethyl)-2,4-dioxo-1,4-dihydroquinazolin-3(2H)-yl)methyl)benzoic acid
-
-
4-(2,4-dioxothiazolidin-5-ylidenemethyl)-N-(4-[1-(4-fluorophenyl)-3-one-1H-isobenzofuran-1-yl]-2,5-dimethyl-1-phenylpyrrol-3-ylmethyl)benzamide
-
-
4-(2-(1-(diphenylmethyl)-2,4-dioxo-1,4-dihydroquinazolin-3(2H)-yl)ethoxy)benzoic acid
-
-
4-(2-(1-benzyl-2,4-dioxo-1,4-dihydroquinazolin-3(2H)-yl)ethoxy)benzoic acid
-
-
4-(2-(7-chloro-1-(diphenylmethyl)-2,4-dioxo-1,4-dihydroquinazolin-3(2H)-yl)ethoxy)benzoic acid
-
-
4-(2-(7-chloro-3-(diphenylmethyl)-2,4-dioxo-3,4-dihydroquinazolin-1(2H)-yl)ethoxy)benzoic acid
-
-
4-(3-(3-(diphenylmethyl)-2,4-dioxo-3,4-dihydroquinazolin-1(2H)-yl)propoxy)benzoic acid
-
-
4-(3-[1-(4-fluorophenyl)-3-oxo-1,3-dihydroisobenzofuran-1-yl]-2,5-dimethylpyrrol-1-yl)benzamide
-
42% inhibition at 0.033 mM
4-(3-[1-(4-fluorophenyl)-3-oxo-1,3-dihydroisobenzofuran-1-yl]-2,5-dimethylpyrrol-1-yl)benzoic acid
-
51% inhibition at 0.033 mM
4-(4-((3-(diphenylmethyl)-2,4-dioxo-3,4-dihydroquinazolin-1(2H)-yl)methyl)phenoxy)butanoic acid
-
-
4-(4-(7-chloro-3-(diphenylmethyl)-2,4-dioxo-3,4-dihydroquinazolin-1(2H)-yl)butoxy)benzoic acid
-
-
4-(4-benzyloxy-phenyl)-1,1,1-trifluoro-butan-2-one
-
-
4-(4-decyloxy-phenyl)-1,1,1-trifluoro-butan-2-one
-
-
4-([(2E)-4-[2-(2,2-diphenylethyl)-3,5-dioxo-1,2,4-oxadiazolidin-4-yl]but-2-en-1-yl]oxy)benzoate
-
-
4-([(2E)-4-[3-(diphenylmethyl)-2,4,6-trioxo-5-prop-2-en-1-yl-1,3,5-triazinan-1-yl]but-2-en-1-yl]oxy)benzoic acid
-
-
4-([(2E)-4-[3-(diphenylmethyl)-5-ethyl-2,4,6-trioxo-1,3,5-triazinan-1-yl]but-2-en-1-yl]oxy)benzoic acid
-
-
4-([(2E)-4-[3-benzyl-5-(diphenylmethyl)-2,4,6-trioxo-1,3,5-triazinan-1-yl]but-2-en-1-yl]oxy)benzoic acid
-
-
4-([(2E)-4-[3-butyl-5-(diphenylmethyl)-2,4,6-trioxo-1,3,5-triazinan-1-yl]but-2-en-1-yl]oxy)benzoic acid
-
-
4-([4-[2-(2,2-diphenylethyl)-3,5-dioxo-1,2,4-oxadiazolidin-4-yl]but-2-yn-1-yl]oxy)benzoate
-
-
4-bromophenacyl bromide
4-[(2-oxohexadecanoyl)amino]butanoic acid
4-[2-aminoethyl]benzensulfonyl fluoride
-
pefabloc, inhibition of activity at 1 mM
4-[2-[2-(1-benzyl-2-phenylethyl)-3,5-dioxo-1,2,4-oxadiazolidin-4-yl]ethoxy]benzoate
-
-
4-[2-[2-(2,2-diphenylethyl)-3,5-dioxo-1,2,4-oxadiazolidin-4-yl]ethoxy]-2-hydroxybenzoate
-
-
4-[2-[2-(2,2-diphenylethyl)-3,5-dioxo-1,2,4-oxadiazolidin-4-yl]ethoxy]benzoate
-
-
4-[2-[2-(diphenylmethyl)-3,5-dioxo-1,2,4-oxadiazolidin-4-yl]ethoxy]benzoate
-
-
4-[2-[3-(2,2-diphenylethyl)-5-ethyl-2,4,6-trioxo-1,3,5-triazinan-1-yl]ethoxy]benzoic acid
-
-
4-[2-[3-(diphenylmethyl)-2,4,6-trioxo-5-phenyl-1,3,5-triazinan-1-yl]ethoxy]benzoic acid
-
-
4-[2-[3-(diphenylmethyl)-2,4,6-trioxo-5-prop-2-en-1-yl-1,3,5-triazinan-1-yl]ethoxy]benzoic acid
-
-
4-[2-[3-(diphenylmethyl)-5-ethyl-2,4,6-trioxo-1,3,5-triazinan-1-yl]ethoxy]benzoic acid
-
-
4-[2-[3-benzyl-5-(diphenylmethyl)-2,4,6-trioxo-1,3,5-triazinan-1-yl]ethoxy]benzoic acid
-
-
4-[2-[3-butyl-5-(diphenylmethyl)-2,4,6-trioxo-1,3,5-triazinan-1-yl]ethoxy]benzoic acid
-
-
4-[2-[5-chloro-1-(diphenylmethyl)-2-methyl-1H-indol-3-yl]ethoxy]benzoic acid
-
-
4-[2-[5-chloro-2-(2-[[(3,4-dichlorobenzyl)sulfonyl]amino]ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]ethoxy]benzoic acid
-
-
4-[3-[2-(2,2-diphenylethyl)-3,5-dioxo-1,2,4-oxadiazolidin-4-yl]propoxy]benzoate
-
-
4-[3-[5-chloro-2-(2-[[(3,4-dichlorobenzyl)sulfonyl]amino]ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl]benzoic acid
-
-
4-[4-[2-(2,2-diphenylethyl)-3,5-dioxo-1,2,4-oxadiazolidin-4-yl]butoxy]benzoate
-
-
4-[4-[2-([2-[bis(4-chlorophenyl)methoxy]ethyl]sulfonyl)ethoxy]phenyl]-1,1,1-trifluorobutan-2-one
-
-
5,5'-dithiobis-(2-nitrobenzoic acid)
-
can be reversed by dithiothreitol
5,8,11,14-Eicosatetraynoic acid
5-(1-[3-(4-octylphenoxy)-2-oxopropyl]indol-5-ylmethylidene)thiazolidine-2,4-dione
-
inhibits isozyme cPLA2alpha
5-(4-[3-(1-[4-fluorophenyl]-3-oxo-1,3-dihydroisobenzofuran-1-yl)-2,5-dimethyl-pyrrol-1-yl]benzylidene)thiazolidine-2,4-dione
-
76% inhibition at 0.033 mM
5-[3-(4-octylphenoxy)-2-oxopropoxy]-1-propylindole-2-carboxylic acid
-
-
5-[3-(4-octylphenoxy)-2-oxopropoxy]indole-2-carboxylic acid
-
-
6-(4-decyloxy-phenyl)-1,1,1-trifluoro-hexan-2-one
-
-
6-[3-(4-oxo-4H-chromen-2-yl)phenyl]-2-phenyl-4H-chromen-4-one
slight inhibition
6-[4-(4-oxo-4H-chromen-2-yl)phenyl]-2-phenyl-4H-chromen-4-one
slight inhibition
7,7-dimethyl-5,8-eicosadienoic acid
-
-
7-chloro-6-[4-(diethylamino)phenyl]-5,8-quinolinedione
-
competitive inhibitor
7-hydroxy-2-oxo-N-[(4Z,7Z,10Z,13Z)-19,19,19-trifluoro-18-oxononadeca-4,7,10,13-tetraen-1-yl]-2H-chromene-3-carboxamide
-
9-oxo-9H-fluorene-3-carboxamide
-
inhibition of phospholipase A2 activity of cytotoxin ExoU
9H-carbazole-4-carboxamide
-
inhibition of phospholipase A2 activity of cytotoxin ExoU
9H-fluoren-4-ol
-
inhibition of phospholipase A2 activity of cytotoxin ExoU
9H-fluorene-4-carboxamide
-
inhibition of phospholipase A2 activity of cytotoxin ExoU
AACOCF3
acalyphin
Acetic anhydride
-
loss of both enzymatic and toxic properties
Acetyl salicylate
acteoside
-
phenylethanoid glycoside isolated from Clerodendron trichotomum Thunberg, competitive. Acts on cytosolic Ca2+-dependent phospholipase A2 rather than secretory phospholipase A2
Ag+
-
plasmalogen-specific PLA2
AIPLAI
-
PLA2 inhibitor isolated from the methanol extract of Azadirachta indica
-
Al3+
-
can replace Ca2+, decreased activity
Ala-Arg-Ser-Ala-Arg
-
allyl 4-(2-oxohexadecanamido)butanoate
-
-
alpha-type phospholipase A2 inhibitor
-
i.e. PLIalpha, an about 75 kDa protein purified from the plasma of the Habu snake Protobothrop flavoviridis, a trimer of two homologous subunits, PLIalpha-A and PLIalpha-B, each of which contains one C-type lectin-like domain, subunit structure and inhibiton specificity, overview. The protein recovers from 6 M guanidine HCl treatment to about 33% inhibition of enzyme activity at 25°C
-
amentoflavone
slight inhibition
Anisic acid
ankyrin-iPLA2s
iPLA2-splice variant, contributes to formation of the iPLA2-tetrameric complex but possesses no active site
-
AnMIP
-
annexin A2
-
phosphorylation of Ser727 disrupts the inhibitory cPLA2alpha-annexin A2-p11 heterotetramer interaction, as annexin A2 complex annexin A2-p11 heterotetramer
-
annexin A2-p11 heterotetramer
-
annexin A2-p11 heterotetramer inhibits cPLA2alpha by interacting with Ser727, phosphorylation of Ser727 disrupts the inhibitory cPLA2alpha-annexin A2-p11 heterotetramer interaction as annexin A2 complex annexin A2-p11 heterotetramer. annexin A2-p11 heterotetramer inhibition of cPLA2alpha is independent of Ser505 phosphorylation
-
anti-peptide antibody
-
antiflammine
-
-
-
aplysulphurin A
arachidonoyl trifluoromethyl ketone
-
-
arachidonoyltrifluoromethyl ketone
-
-
arachidonyl trifluoromethyl ketone
arachidonyl trifluoromethylketone
-
causes inhibition to baseline level of gIVaPLA2 activity caused by IL-8/CXCL8
arachidonyltrifluoromethyl ketone
aristolochic acid
ATP
-
plasmalogen-specific PLA2
AX006
-
inhibits GIVA cPLA2
AX007
-
interacts with key residues that also exhibit changes in deuterium exchange upon inhibitor binding. Is bound mainly through contacts near the active site. Residues 481-495 and 543-553 exhibit an increase in exchange in the presence of the oxoamide, whereas 393-397 does not show any difference in exchange in the presence of the oxoamide in contrast to the inhibitor pyrrophenone
AX048
-
inhibits GIVA cPLA2 and GVIA iPLA2
AZ-1
cPLA2-alpha inhibitor, causes almost complete suppression of arachidonic acid release induced by various stimuli. Reduces by 70% the generation of platelet activating factor from macrophages
benzyl 4-(2-oxohexadecanamido)butanoate
-
-
Berberine
competitive inhibitor of phospholipase A2
biphenylene-1-carbonyl chloride
-
inhibition of phospholipase A2 activity of cytotoxin ExoU
bromoenol lactone
bromoenollactone
-
is not specific for GVIA PLA2 and actually functions through activation of the inhibitor by GVIA PLA2 followed by nonspecific covalent modification of cysteine residues in all proximally located enzymes
bromophenacyl bromide
specific sPLA2 inhibitor
CaCl2
-
1 mM, residual activity 82.1%
Calmodulin
-
GVIA PLA2 is regulated by calmodulin which negatively regulates GVIA PLA2 through direct binding on the residues 694-705 of GVIA-1 PLA2
catechin
-
reaches 50% inhibition at concentrations of 2.5 mM
Cdcas F3
-
a crotapotin
-
Cdcas F4
-
a crotapotin
-
Cdcoll F3
-
a crotapotin
-
Cdcoll F4
-
a crotapotin
-
Cdt F7
-
a crotapotin
-
chlorogenic acid
cholate
bile salt regulation of lipid metabolism via both activation and inhibition of PLA2, interaction and binding structure analysis, overview
chondroitin sulfate
-
plasmalogen-specific PLA2
citrate
-
plasmalogen-specific PLA2
Co2+
-
can replace Ca2+, decreased activity
Cowper's gland mucin
-
plasmalogen-specific PLA2
-
crotapotin
-
curcumin
cyanidin
-
mixed competitive and noncompetitive inhibition, partial hyperbolic type of inhibition
cyproheptadine
-
at a dose of 5 mg inhibits 82% promutoxin elicited microvascular leakage
dantrolene
-
-
darapladib
delphinidin
-
mixed competitive and noncompetitive inhibition, complete inhibition
deoxycholate
-
substrate: phosphatidylcholine
dexamethasone
Dicetyl phosphate
diethyl 4-nitrophenyl phosphate
Diethyl p-nitrophenyl phosphate
diisopropyl fluorophosphate
dithiothreitol
DNA containing thymine glycol
-
i.e. MAFP, a specific PLA2 inhibitor
-
ethyl (2E,4S)-4-[(2-oxohexadecanoyl)amino]oct-2-enoate
-
reduces the cellular release of arachidonic acid by 16%
ethyl 2-(2-oxohexadecanamido)acetate
-
-
ethyl 3-(2-oxohexadecanamido)propanoate
-
-
ethyl 4-(2-oxohexadecanamido)benzoate
-
-
ethyl 4-[(2-oxohexadecanoyl)amino]butanoate
-
-
ethyl 5-(2-oxohexadecanamido)pentanoate
-
-
factor Xa
-
-
-
Fe3+
-
plasmalogen-specific PLA2
fetuin
-
plasmalogen-specific PLA2
-
FPL67047XX
used as a prototype structure with a binding energy of -18.96 kJ/mol
gallic acid
inhibitory in micromolar concentrations
ganglioside GM1
-
plasmalogen-specific PLA2
ganglioside GM3
-
plasmalogen-specific PLA2
genistein
-
inhibits sPLA(2) enzymes of inflammatory exudates in a concentration dependent manner. Increasing the Ca2+ concentration from 2.5 to 15 mM and substrate concentration up to 0.000120 mM does not alter the level of inhibition
ginkgolide B
-
ginkgolide B at a dose of 5 mg inhibits 31% microvascular leakage induced by promutoxin when they are coinjected
giripladib
i.e. Wyeth-2, the inhibition of phospholipase A2alpha reduces platelet adhesion and accumulation on collagen, it inhibits cPLA2alpha-mediated release of arachidonic acid from glycerophospholipid sources; inhibitor, reduces platelet adhesion and accumulation on collagen. Giripladib differentially affects P-selectin expression and GPIIbIIIa activation depending on the agonist employed. The levels of PAR4- and GPVI-mediated platelet activation are significantly reduced
glycochenodeoxycholate
bile salt regulation of lipid metabolism via both activation and inhibition of PLA2, interaction and binding structure analysis, overview
glycocholate
bile salt regulation of lipid metabolism via both activation and inhibition of PLA2, interaction and binding structure analysis, overview
gracilin A
Guanidine HCl
-
-
heparan sulfate
-
plasmalogen-specific PLA2
heparin
hexadecyl-3-trifluorethylglycero-sn-2-phospho-methanol
hyaluronic acid
-
plasmalogen-specific PLA2
indole-5-carboxamide
-
inhibits isozyme cPLA2alpha
indole-5-carboxylic acid
-
inhibits isozyme cPLA2alpha
indoxam
iodoacetamide
iodoacetate
-
plasmalogen-specific PLA2
koninginin E
koninginin F
luffariellin B
LY 329722
LY311727
LY315920
lysophosphatidylcholines
-
inhibitory plasma compounds, profile determination by mass spectroscopy, overview
Maleic anhydride
-
-
malvidin
-
partial competitive inhibition
manoalogue
Me-Indoxam
methyl 2-(2-oxo-8-phenyloctanamido)acetate
-
-
methyl 2-(2-oxohexadecanamido)acetate
-
-
methyl 2-(7-phenylheptanamido)acetate
-
-
methyl 3-(2-oxohexadecanamido)propanoate
-
-
methyl 5-(2-oxohexadecanamido)pentanoate
-
-
methyl 9H-fluorene-4-carboxylate
-
inhibition of phospholipase A2 activity of cytotoxin ExoU
methyl arachidonyl fluorophosphate
-
i.e. MAFP, an inhibitor of cysteine-dependent phospholipases
methyl arachidonyl fluorophosphonate
methyl arachidonyl-fluorophosphonate
-
-
methyl N-(2-oxohexadecanoyl)glycinate
-
reduces the cellular release of arachidonic acid by 30%
methyl [1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]carbamate
-
-
methyl-4-nitrophenyl-octylphosphonate
-
inactivates at 100fold molar excess
methyl-arachidonyl fluorophosphonate
an irreversible inhibitor
methyl-arachidonylfluorophosphonate
-
irreversible inhibitor of cPLA2 and iPLA2. Ser214 site in microtubule-associated protein Tau is hyperphosphorylated upon inhibitor treatment
methylarachidonyl fluorophosphonate
-
inhibits release of [3H]arachidonic acid by a 0.01 mM concentration
MgCl2
-
1 mM, residual activity 71.6%
minocycline
interferes with the conformation of the active-site Ca2+-binding loop, preventing Ca2+ binding, and shields the active site from substrate entrance, resulting in inhibition of the enzyme. Dissociation constant for PLA2 is Kd = 0.00018 M
MJ33
i.e. 1-hexadecyl-3-(trifluoroethyl)-rac-glycero-2-phosphomethanol, an active-site-directed tetrahedral mimic
mucin
-
plasmalogen-specific PLA2
-
N,N-dimethyl-1-[3-(4-octylphenoxy)-2-oxopropyl]indole-5-carboxamide
-
inhibits isozyme cPLA2alpha
N,N-dimethyl-1-[3-(4-octylphenoxy)-2-oxopropyl]indole-5-sulfonamide
-
inhibits isozyme cPLA2alpha
N,N-dimethyl-9H-fluorene-4-carboxamide
-
inhibition of phospholipase A2 activity of cytotoxin ExoU
N-(2-oxododecanoyl)-L-norleucine
-
reduces the cellular release of arachidonic acid by 21%
N-(4-amylcinnamoyl) anthranilic acid
-
i.e. 12-hydroperoxy-5Z,8Z,10E,14Zeicosatetraenoic acid
N-(4-ethoxybutyl)-2-oxohexadecanamide
-
-
N-(4-[3-(1-(4-fluorophenyl)3-oxo-1,3-dihydroisobenzofuran-1-yl)-2,5-dimethylpyrrol-1-yl]phenyl)acetamide
-
35% inhibition at 0.033 mM
N-(cyclopent-1-en-1-yl)pyrrolidine
ccPLA2-alpha inhibitor, causes almost complete suppression of arachidonic acid release induced by various stimuli. Reduces by 70% the generation of platelet activating factor from macrophages
N-9H-fluoren-2-ylformamide
-
inhibition of phospholipase A2 activity of cytotoxin ExoU
N-9H-fluoren-4-ylacetamide
-
inhibition of phospholipase A2 activity of cytotoxin ExoU
N-acetylneuraminic acid
-
plasmalogen-specific PLA2
N-alpha-p-tosyl-L-lysine chloromethyl ketone
-
-
N-bromosuccinimide
-
-
N-cyclohexyl-N'-[1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]urea
-
-
N-dodecyl-N,N-dimethyl-3-aminopropanesulfonate
-
-
N-ethyl-N'-[1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]urea
-
-
N-ethylmaleimide
N-methyl-1-[3-(4-octylphenoxy)-2-oxopropyl]indole-5-carboxamide
-
inhibits isozyme cPLA2alpha
N-methyl-1-[3-(4-octylphenoxy)-2-oxopropyl]indole-5-sulfonamide
-
inhibits isozyme cPLA2alpha
N-phenyl-9H-fluorene-4-carboxamide
-
inhibition of phospholipase A2 activity of cytotoxin ExoU
N-tetradecyl-N,N-dimethyl-3-aminopropanesulfonate
-
-
N-tosyl-L-phenylalanyl chloromethyl ketone
-
-
N-[1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]acetamide
-
-
N-[[(2S,4R)-1-([2-[(2,4-difluorophenyl)carbonyl]phenyl]carbonyl)-4-(tritylsulfanyl)pyrrolidin-2-yl]methyl]-4-[(Z)-(2,4-dioxo-1,3-thiazolidin-5-ylidene)methyl]benzamide
-
-
naringin
-
the enzymatic activity of native secretory phospholipase A2 is virtually abolished by treatment with naringin
nifedipine
-
-
Nonidet-P40
-
-
nordihydroguaiaretic acid
-
-
o-nitrophenylsulfonyl chloride
Bothrops spp.
-
BthTX-I: myotoxic activity reduced to 65% and the cytotoxic activity reduced to 58%
ochnaflavone
slight inhibition
octylglucoside
-
plasmalogen-specific PLA2
omega-bromo-4-nitroacetophenone
ONO-RS-082
p-bromophenacyl bromide
p-bromophenacylbromide
p-hydroxymercuribenzoate
palmitoyl lysophosphatidylcholines
-
competitive product inhibition
-
palmitoyltrifluoromethyl ketone
-
-
Pb2+
-
-
pelargonidin
-
mixed competitive and noncompetitive inhibition, complete inhibition
peonidin
-
mixed competitive and noncompetitive inhibition, partial hyperbolic type of inhibition
Peptide inhibitor
-
purified from Habu serum, 100000 Da, heat stable, stable in neutral and basic medium
-
pertussis toxin
-
inhibits dramatically promutoxin-induced histamine release from colon mast cells, but has less effect on promutoxin-induced histamine release from lung cells
-
petrosaspongiolide M
an anti-inflammatory marine natural product, mechanism of sPLA2-IIA inactivation, overview
petunidin
-
mixed competitive and noncompetitive inhibition, partial hyperbolic type of inhibition
phenyl [1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]carbamate
-
-
phenylmethylsulfonyl fluoride
phosphate
-
plasmalogen-specific PLA2
prostaglandin PGE2
-
-
prostaglandin PGI2
-
-
protein p11
-
phosphorylation of Ser727 disrupts the inhibitory cPLA2alpha-annexin A2-p11 heterotetramer interaction as annexin A2 complex annexin A2-p11 heterotetramer
-
protocatechuic acid
pseudolipasin A
-
a specific inhibitor for phospholipase A2 activity of cytotoxin ExoU
pure phospholipid vesicles
-
exception: vesicles composed of phosphatidylcholine or phosphatidylinositol 4,5-bisphosphate
-
pyrrolidine-1
pyrrolidine-2
pyrrophenone
pyrroxyphene
-
significantly inhibits both the increase in levels of cPLA2 alpha and eicosanoids as well as the mRNA expression of matrix metalloproteinase-3, -8, -9, -13, and cyclooxygenase-2. Strongly inhibits the incidence of arthritis and bone destruction
quercetin
-
quercetin-3-beta-D-glucoside
-
rilapladib
-
-
Rose bengal
Bothrops spp.
-
BthTX-I: myotoxic activity reduced to 20% and the cytotoxic activity reduced to 0.5%
salicylic acid
SB-203580
-
-
SB222657
-
-
SB435495
SB480848
-
darapladib, completely inhibits lp-PLA2 enzyme activity in the whole culture media of THP-1 cells with 0.0001 mM
sodium 2-(1-benzyl-2-ethyl)-3-oxamoylindol-4-yl oxyacetate
-
varespladib sodium or LY315920, most potent sPLA2 inhibitor
sodium deoxycholate
Sodium dodecyl sulfate
sphingomyelin
stearoyl lysophosphatidylcholines
-
competitive product inhibition
-
stigmasterol
sulfate
-
plasmalogen-specific PLA2
suramin
the C-terminal region of the enzyme is crucial to the stabilization of the complex with suramin and consequently is a major structural determinant of the inhibitory action of suramin
surfactant protein A
-
syringic acid
inhibitory in micromolar concentrations
taurochenodeoxycholate
bile salt regulation of lipid metabolism via both activation and inhibition of PLA2, interaction and binding structure analysis, overview
taurocholate
tectoridin
terfenadine
-
at a dose of 5 mg inhibits 67% promutoxin elicited microvascular leakage
tert-butyl ([3-[amino(oxo)acetyl]-1-benzyl-2-(2-methylpropyl)-1H-indol-4-yl]oxy)acetate
tert-butyl 2-(2-oxohexadecanamido)acetate
-
-
tert-butyl 3-(2-oxo-8-phenyloctanamido)propanoate
-
-
tert-butyl 3-(2-oxohexadecanamido)propanoate
-
-
tert-butyl 3-(7-phenylheptanamido)propanoate
-
-
tert-butyl 5-(2-oxohexadecanamido)pentanoate
-
-
tert-butyl 5-[(2-oxohexadecanoyl)amino]pentanoate
-
reduces the cellular release of arachidonic acid by 11%
tetrahydro-3-(1-naphthalenyl)-2H-pyran-2-one
-
-
thioetheramide
-
-
thioetheramide phosphatidylcholine
-
exhibits complete competitive inhibition
tributyltin oxide
-
-
Tris/maleate buffer
-
-
Triton X-100
turmerin
-
inhibits the enzymatic activity and neutralises the pharmacological properties, such as cytotoxicity, oedema and myotoxicity of multitoxic phospholipase A2 of cobra venom in a dose-dependent manner, at a 1:2.5 molar ratio of PLA2:turmerin
vanillic acid
inhibitory in micromolar concentrations
Withania somnifera glycoprotein WSG
-
in molar ratio of 1:2, enzyme:WSG, complete inhibition of activity, but not neutralization of toxicity
-
ZnCl2
-
1 mM, no residual activity
additional information
-