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(-)-epicatechin-3-O-gallate
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IC50: 0.072 mM
(-)-epigallocatechin
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IC50: 0.073 mM
(-)-epigallocatechin-3-O-gallate
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IC50: 0.046 mM
(4,4',5,5',6,6'-hexahydroxybiphenyl-2,2'-diyl)bis[(2R,3R)-5,7-dihydroxy-3,4-dihydro-2H-chromene-2,3-diyl] bis(3,4,5-trihydroxybenzoate)
-
-
1,2,3,4,6-pentagalloyl-beta-D-glucose
-
IC50: 0.026 mM
1,4-diacetoxy-2-methoxy-5-methyl-3-tetradecanoyloxybenzene
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1-acyl-sn-glycero-3-phosphate
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competitive inhibition for 1-alkyl-sn-glycero-3-phosphate
1-methoxyphaseolidin
-
IC50: 0.048 mM
1-methoxyphaseolin
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IC50: 0.057 mM
1-O-alkyl-2-acetyl-sn-glycero-3-phosphocholine
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irreversible inhibition dependent of both 1-O-alkyl-2-acetyl-sn-glycero-3-phosphocholine and enzyme concentration
1-O-alkyl-sn-glycero-3-phosphocholine
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inhibition at high concentrations due to its detergent effect
2-methoxy-1,3,4-trihydroxy-5-methylbenzene
i.e. 2-methoxy-1,3,4-trihydroxy-5-methylbenzene, isolated from Penicillium sp. strain F33
2-methoxy-5-methyl-1,3,4-triacetoxybenzene
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2-methoxy-5-methyl-3-octadecanoyloxy-1,4-benzoquinone
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2-methoxy-5-methyl-3-tetradecanoyloxy-1,4-benzoquinone
3,4-dichloro-1-(4,5-dichloro-2-methoxyphenyl)-1H-pyrrole-2,5-dione
3,4-dihydroxy-1,2-dimethoxy-5-methylbenzene
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3-acetoxy-2-methoxy-5-methyl-1,4-benzoquinone
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3-chloro-1-(3-chloro-4-methoxyphenyl)-4-(2-methoxyphenoxy)-1H-pyrrole-2,5-dione
3-chloro-1-(4,5-dichloro-2-methoxyphenyl)-4-(2-hydroxyanilino)-1H-pyrrole-2,5-dione
3-chloro-4-(morpholin-4-yl)-1-(4-phenoxyphenyl)-1H-pyrrole-2,5-dione
3-decanoyloxy-2-methoxy-5-methyl-1,4-benzoquinone
3-hexanoyloxy-2-methoxy-5-methyl-1,4-benzoquinone
-
3-hydroxy-2-methoxy-5-methyl-1,4-benzoquinone
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4-(1-Naphthylvinyl)pyridine
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IC50: 0.043 mM
6,8-diprenylgenistein
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IC50: 0.019 mM
6-hydroxy-2,5,7,8-tetramethylchroman-2-carboxylic acid
i.e. Trolox, reduces production of platelet-activating factor (PAF) in H2O2-treated HUVEC cells
ascorbic acid
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18.3% inhibition at 1 mM
butyl 4-(3,4-dichloro-2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)benzoate
chiyusaponin
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IC50: 0.2 mM
dexamethasone
-
2 mg/kg for 3 days in liver and spleen
dihydrofumigatin
i.e. 2-methoxy-1,3,4-trihydroxy-5-methylbenzene, isolated from Penicillium sp. strain F33
diisopropylfluorophosphate
ebselen
-
suppresses alkyl-2-acetyl-sn-glycero-3-phosphocholine synthesis by 7.7% and 26.6% in presence of glutathione
farnesyl gallate
-
IC50: 0.066 mM
gallic acid
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5.3% inhibition at 0.1 mM
geranyl gallate
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IC50: 0.089 mM
glutathione
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suppresses alkyl-2-acetyl-sn-glycero-3-phosphocholine synthesis by 18.9%
H2O2
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8% inhibition at 1 mM
licoricidin
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IC50: 0.0077 mM
lopinavir-r
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remaining activity in human mesangial cells: 76%. By contrast no effect on activity is observed in blood of naiive patients treated with the drug
luteolin
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IC50: 0.045 mM
lysophosphatidylcholine
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inhibition at high concentrations due to its detergent effect
medroxyprogesterone
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50 mg/kg in liver
methyl 4-(3,4-dichloro-2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)benzoate
methyl 4-[3-chloro-2,5-dioxo-4-(4-sulfamoylanilino)-2,5-dihydro-1H-pyrrol-1-yl]benzoate
MgATP2-
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32% and 54% inhibition at 0.125 and 1 mM respectively in neuronal nuclear fraction
myricetin
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suppresses alkyl-2-acetyl-sn-glycero-3-phosphocholine synthesis by 17%
N-acetylcysteine
reduces production of platelet-activating factor (PAF) in H2O2-treated HUVEC cells
n-dodecyl gallate
-
IC50: 0.091 mM
nordihydroguaiaretic acid
oleic acid
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1-acyl lysolipids less inhibited than the 1-alkyl species
p-chloromercuribenzoate
-
-
palmitoyllyso-glycero-3-phosphocholine
phenylmethylsulfonyl fluoride
-
30% inhibition at 50 mM
procyanidin B-2,3,3'-di-O-gallate
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IC50: 0.031 mM
procyanidin B-5,3,3'-di-O-gallate
-
IC50: 0.024 mM
propan-2-yl 4-(3,4-dichloro-2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)benzoate
propan-2-yl 4-(3-chloro-2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)benzoate
propan-2-yl 4-[3-chloro-4-(2-hydroxyanilino)-2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl]benzoate
propan-2-yl 4-[3-chloro-4-(morpholin-4-yl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl]benzoate
propyl 4-(3,4-dichloro-2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)benzoate
pyrrolidinecarbodithioic acid
i.e. PDTC, reduces production of platelet-activating factor (PAF) in H2O2-treated HUVEC cells
resveratrol
-
0.157 microM, results in 50% inhibition in interleukin 1beta effect on catalytic activity
serine/threonine phosphatase
-
diminishes rates of acetylation for 1-alkyl-sn-glycero-3-phosphocholine and 1-acyl-sn-glycero-3-phosphocholine
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sodium dodecylsulfate
-
inactivation at 0.1%
tenofovir-DF
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remaining activity in human mesangial cells: 32%. By contrast no effect on activity is observed in blood of naiive patients treated with the drug
theaflavin
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IC50: 0.032 mM
theaflavin-3'-O-gallate
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IC50: 0.039 mM
theaflavin-3,3'-di-O-gallate
-
IC50: 0.028 mM
theaflavin-3-O-gallate
-
IC50: 0.058 mM
theasinensin A
-
IC50: 0.029 mM
Triton X-100
-
75 and 95% inhibition at 0.2 and 0.6 mM respectively due to detergent
tyrosol
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0.048 microM, results in 50% inhibition in interleukin 1beta effect on catalytic activity
Urea
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inactivation at 8 mM
2-methoxy-5-methyl-3-tetradecanoyloxy-1,4-benzoquinone
derivative of a metabolite from Penicillium sp. F33 , strong inhibition. Compound also significantly suppresses the gene expression of lyso-PAF acetyltransferase/LPCAT2 in mouse bone marrow-derived macrophages stimulated by lipopolysaccharide
2-methoxy-5-methyl-3-tetradecanoyloxy-1,4-benzoquinone
-
derivative of a metabolite from Penicillium sp. F33 , strong inhibition. Compound also significantly suppresses the gene expression of lyso-PAF acetyltransferase/LPCAT2 in mouse bone marrow-derived macrophages stimulated by lipopolysaccharide
3,4-dichloro-1-(4,5-dichloro-2-methoxyphenyl)-1H-pyrrole-2,5-dione
-
3,4-dichloro-1-(4,5-dichloro-2-methoxyphenyl)-1H-pyrrole-2,5-dione
-
3-chloro-1-(3-chloro-4-methoxyphenyl)-4-(2-methoxyphenoxy)-1H-pyrrole-2,5-dione
-
3-chloro-1-(3-chloro-4-methoxyphenyl)-4-(2-methoxyphenoxy)-1H-pyrrole-2,5-dione
-
3-chloro-1-(4,5-dichloro-2-methoxyphenyl)-4-(2-hydroxyanilino)-1H-pyrrole-2,5-dione
-
3-chloro-1-(4,5-dichloro-2-methoxyphenyl)-4-(2-hydroxyanilino)-1H-pyrrole-2,5-dione
-
3-chloro-4-(morpholin-4-yl)-1-(4-phenoxyphenyl)-1H-pyrrole-2,5-dione
-
3-chloro-4-(morpholin-4-yl)-1-(4-phenoxyphenyl)-1H-pyrrole-2,5-dione
-
3-decanoyloxy-2-methoxy-5-methyl-1,4-benzoquinone
derivative of a metabolite from Penicillium sp. F33 , strong inhibition. Compound also significantly suppresses the gene expression of lyso-PAF acetyltransferase/LPCAT2 in mouse bone marrow-derived macrophages stimulated by lipopolysaccharide; not active against lipoxygenase and cyclooxygenases
3-decanoyloxy-2-methoxy-5-methyl-1,4-benzoquinone
-
derivative of a metabolite from Penicillium sp. F33 , strong inhibition. Compound also significantly suppresses the gene expression of lyso-PAF acetyltransferase/LPCAT2 in mouse bone marrow-derived macrophages stimulated by lipopolysaccharide
acetyl-salicylic acid
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IC50: 1.52 mM
acetyl-salicylic acid
-
weak inhibition
baicalein
-
concentration dependent inhibition, IC50: 0.105 mM
baicalein
-
IC50: 0.148 mM
butyl 4-(3,4-dichloro-2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)benzoate
80.4% inhibition at 0.02 mM
butyl 4-(3,4-dichloro-2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)benzoate
83.0% inhibition at 0.02 mM
CaCl2
-
10 mM, 46% inhibition
diisopropylfluorophosphate
-
-
diisopropylfluorophosphate
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98% inhibition at 10 mM
EDTA
-
67.9 and 72.7% inhibition at 0.5 and 1 mM respectively
EDTA
-
1 mM, 47% inhibition
EGTA
-
-
Fe2+
-
31% inhibition at 0.01 mM
honokiol
-
IC50: 0.06 mM, reversible inhibition
indomethacin
-
IC50: 0.26 mM
indomethacin
-
weak inhibition at 1 mM
magnolol
-
IC50: 0.07 mM, reversible inhibition
methyl 4-(3,4-dichloro-2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)benzoate
-
methyl 4-(3,4-dichloro-2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)benzoate
-
methyl 4-[3-chloro-2,5-dioxo-4-(4-sulfamoylanilino)-2,5-dihydro-1H-pyrrol-1-yl]benzoate
-
methyl 4-[3-chloro-2,5-dioxo-4-(4-sulfamoylanilino)-2,5-dihydro-1H-pyrrol-1-yl]benzoate
-
MgCl2
-
-
MnCl2
-
-
nordihydroguaiaretic acid
-
concentration dependent inhibition, IC50: 0.075 mM
nordihydroguaiaretic acid
-
IC50: 0.06 mM
nordihydroguaiaretic acid
-
IC50: 0.29 mM
oleoyl-CoA
-
45-55% inhibition
oleoyl-CoA
-
16% and 36% inhibition at 0.002 and 0.01 mM respectively in neuronal nuclear fraction
p-bromophenacyl bromide
-
-
p-bromophenacyl bromide
-
90% inhibition at 0.1 mM
palmitoyl-CoA
-
-
palmitoyl-CoA
-
85% inhibition at 10 uM due to detergent effect
palmitoyllyso-glycero-3-phosphocholine
-
-
palmitoyllyso-glycero-3-phosphocholine
-
competitive inhibitor for alkyl-sn-glycero-3-phosphocholine
propan-2-yl 4-(3,4-dichloro-2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)benzoate
95.2% inhibition at 0.02 mM
propan-2-yl 4-(3,4-dichloro-2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)benzoate
95.5% inhibition at 0.02 mM
propan-2-yl 4-(3-chloro-2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)benzoate
competitively inhibits the lyso-PAFAT activity with acetyl-CoA
propan-2-yl 4-(3-chloro-2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)benzoate
compound competes with acetyl-CoA for the inhibition of isoform LPCAT2 lyso-PAFAT activity and suppresses platelet-activating factor biosynthesis in mouse peritoneal macrophages stimulated with a calcium ionophore. The compound has low inhibitory effects on isoform LPCAT1 activity
propan-2-yl 4-[3-chloro-4-(2-hydroxyanilino)-2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl]benzoate
83.1% inhibition at 0.02 mM
propan-2-yl 4-[3-chloro-4-(2-hydroxyanilino)-2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl]benzoate
82.4% inhibition at 0.02 mM
propan-2-yl 4-[3-chloro-4-(morpholin-4-yl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl]benzoate
-
propan-2-yl 4-[3-chloro-4-(morpholin-4-yl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl]benzoate
-
propyl 4-(3,4-dichloro-2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)benzoate
85.4% inhibition at 0.02 mM
propyl 4-(3,4-dichloro-2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)benzoate
86.7% inhibition at 0.02 mM
quercetin
-
suppresses alkyl-2-acetyl-sn-glycero-3-phosphocholine synthesis by 8.8%
quercetin
-
IC50: 0.08 mM
additional information
500 ml/day of low-fat milk fortified with phytosterols, linoleic and alpha linolenic acids, vitamin C, vitamin E, vitamin A, vitamin B6, vitamin B12, folic acid, magnesium and selenium has no effect on the enzyme activity in vivo
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additional information
identification of LPCAT2-specific inhibitors in order to ameliorate platelet-activating factor-related inflammatory diseases: N-phenylmaleimide derivatives are selected from a 174000-compound library using fluorescence-based high-throughput screening followed by the evaluation of the effects on LPCAT1 and LPCAT2 activities, cell viability, and cellular platelet-activating factor production. The selected compounds have low inhibitory effects on enzyme LPCAT1 activity which is mostly expressed in the lungs where it produces platelet-activating factor, indicating that adverse effects on respiratory functions may be avoided. Structure-activity relationship, overview
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additional information
-
inhibition of lipopolysaccharide-induced platelet activating factor production and gene expression of lysophosphatidylcholine acyltransferase (LPCAT2)/lyso-PAF acetyltransferase by synthetic fumigatin derivatives, compound stability and inhibitory potencies, synthesis and evaluation, overview. Dihydrofumigatin is isolated and identified from Penicillium sp. strain F33. In addition to the efficacy to inhibit the function of lyso/PAF acetyltransferase/LPCAT2, 3-hexanoyloxy-2-methoxy-5-methyl-1,4-benzoquinone, 3-decanoyloxy-2-methoxy-5-methyl-1,4-benzoquinone, and 2-methoxy-5-methyl-3-tetradecanoyloxy-1,4-benzoquinone also inhibit the expression of LPCAT2 mRNA
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additional information
inhibition of lipopolysaccharide-induced platelet activating factor production and gene expression of lysophosphatidylcholine acyltransferase (LPCAT2)/lyso-PAF acetyltransferase by synthetic fumigatin derivatives, compound stability and inhibitory potencies, synthesis and evaluation, overview. Dihydrofumigatin is isolated and identified from Penicillium sp. strain F33. In addition to the efficacy to inhibit the function of lyso/PAF acetyltransferase/LPCAT2, 3-hexanoyloxy-2-methoxy-5-methyl-1,4-benzoquinone, 3-decanoyloxy-2-methoxy-5-methyl-1,4-benzoquinone, and 2-methoxy-5-methyl-3-tetradecanoyloxy-1,4-benzoquinone also inhibit the expression of LPCAT2 mRNA
-
additional information
identification of LPCAT2-specific inhibitors in order to ameliorate platelet-activating factor-related infl ammatory diseases: N-phenylmaleimide derivatives are selected from a 174000-compound library using fluorescence-based high-throughput screening followed by the evaluation of the effects on LPCAT1 and LPCAT2 activities, cell viability, and cellular platelet-activating factor production. The selected compounds have low inhibitory effects on enzyme LPCAT1 activity which is mostly expressed in the lungs where it produces platelet-activating factor, indicating that adverse effects on respiratory functions may be avoided. Structure-activity relationship, overview
-
additional information
-
identification of LPCAT2-specific inhibitors in order to ameliorate platelet-activating factor-related infl ammatory diseases: N-phenylmaleimide derivatives are selected from a 174000-compound library using fluorescence-based high-throughput screening followed by the evaluation of the effects on LPCAT1 and LPCAT2 activities, cell viability, and cellular platelet-activating factor production. The selected compounds have low inhibitory effects on enzyme LPCAT1 activity which is mostly expressed in the lungs where it produces platelet-activating factor, indicating that adverse effects on respiratory functions may be avoided. Structure-activity relationship, overview
-