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2,2'-dithiodipyridine
-
9 mM, 90% inhibition of Mg2+-dependent enzyme, 16% inhibition of Mg2+-independent enzyme
4,4'-dithiodipyridine
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9.0 mM, 96% inhibition of Mg2+-dependent enzyme, 20% inhibition of Mg2+-independent enzyme
4-chlormercuriphenylsulfonic acid
-
-
5,5'-dithiobis(2-nitrobenzoic acid)
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0.2 mM, 80% inhibition of Mg2+-dependent enzyme, no inhibition of Mg2+-independent enzyme
cystamine dihydrochloride
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1 mM, 25% inhibition of Mg2+-dependent enzyme, 8% inhibition of Mg2+-independent enzyme
diacylglycerol diphosphate
DMSO
-
addition to the reaction mixture results in a dose-dependent inhibition of PAP1 activity, 25% loss of PAP1 activity at a 1% concentration
epinephrine
promotes dephosphorylation of lipin, but has no effect on PAP activity, markedly decreases amounts of lipin and PAP activity in the soluble fraction
ethanol
-
inhibition of PAP-1
lysophosphatidic acid
-
-
lysophosphatidylethanolamine
-
-
lysophosphatidylglycerol
-
-
N,N'-p-phenylenedimaleimide
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0.4 mM, 44% inhibition of Mg2+-dependent enzyme, 7% inhibition of Mg2+-independent enzyme
Na3VO4
-
2 mM, about 90% inhibition
oleate
-
reversed by phosphatidic acid and albumin
oleic acid
promotes dephosphorylation of lipin, but has no effect on PAP activity, markedly decreases amounts of lipin and PAP activity in the soluble fraction
p-chloromercuriphenylsulfonic acid
p-nitrophenyl phosphate
-
inhibits hydrolysis of phosphatidic acid
palmitate
-
1 mM, 30% inhibition
phosphatidate
-
conpetitive versus diacylglycerol diphosphate
phosphatidylcholine
-
slight inhibition of cytosolic activity
phosphatidylglycerol
-
0.7 mg/ml, 75% inhibition
RNAi2
reduces expression levels of LPR1 by ca. 60% in SK-OV-3 cells
-
SDS
1%, strong inhibition
shRNA
-
lipin 2 shRNA treatment significantly reduces hepatocyte PAP-1 activity in both wild-type and fld hepatocytes
-
spermidine trihydrochloride
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7% inhibition at equimolar concentration of substrate, PAP-2
sphingomyelin
-
72% inhibition at equimolar concentration with pure phosphatidic acid. No effect with equimolar concentrations of phosphatidic acid mixed with phosphatidylcholine
sphingosine 1-phosphate
-
-
thimerosal
-
0.5 mM, 85% inhibition of Mg2+-dependent enzyme, 12% inhibition of Mg2+-independent enzyme
vanadate
10 mM, strong inhibition
Zwitterionic phospholipids
-
slight inhibition
-
1,2-diacylglycerol
-
-
ATP
-
half-maximal inhibition at 0.2 mM
ATP
-
complex inhibition of the 104-kDa enzyme form, inhibition of the 45-kDa enzyme form, inhibition by nucleotides involves the chelation of Mg2+ ions
ATP
-
the mechanism of inhibition by ATP is complex, affecting both the Vmax and Km for phosphatidic acid, competitive to Mg2+ and involving the chelation of the cofactor
bromoenol lactone
-
bromoenol lactone-induced apoptosis is accompanied by a very strong inhibition of PAP-1-regulated events, such as incorporation of choline into phospholipids and de novo incorporation of arachidonic acid into triacylglycerol
bromoenol lactone
-
inhibition of PAP-1
bromoenol lactone
-
i.e. BEL OR U-73122
bromoenol lactone
-
selective inhibition of PAP1
Ca2+
-
1 mM, 10% inhibition
Ca2+
-
activity with aqueously dispersed phosphatidic acid
Ca2+
-
inhibition at optimal concentrations of Mg2+
Ca2+
-
10 mM, 60% inhibition of PAP-2
Ca2+
-
IC50: 15 mM, reaction with phosphatidic acid. IC50: 7.1 mM, reaction with diacylglycerol diphosphate. IC50: 8.2 mM, reaction with lysophosphatidic acid
chlorpromazine
-
-
chlorpromazine
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competitive inhibition at optimal concentrations of Mg2+
chlorpromazine
-
55% inhibition at equimolar concentration of substrate, PAP-2
Co2+
-
IC50: 0.029 mM, reaction with phosphatidic acid. IC50: 1.1 mM, reaction with diacylglycerol diphosphate. IC50: 1.2 mM, reaction with lysophosphatidic acid
CTP
-
-
CTP
-
complex inhibition of the 104-kDa enzyme form, inhibition of the 45-kDa enzyme form, inhibition by nucleotides involves the chelation of Mg2+ ions
CTP
-
the mechanism of inhibition by CTP is complex, affecting both the Vmax and Km for phosphatidic acid, competitive to Mg2+ and involving the chelation of the cofactor
diacylglycerol
-
-
diacylglycerol
-
DPP1-encoded PAP2 enzyme is inhibited by CDP-DAG
diacylglycerol diphosphate
-
competitive with respect to phosphatidic acid
diacylglycerol diphosphate
-
conpetitive versus phosphatidate
diacylglycerol diphosphate
-
-
EDTA
-
50 mM, 70% inhibition
EDTA
-
inhibition of hydrolysis of phosphatidate bound to microsomal membrane or phosphatidate in sonicated dispersion of organic solvent-disrupted microsomes, no effect on hydrolysis of phosphatidate dispersed in sonicated microsomal lipid
EDTA
-
inhibits activity with membrane-bound phosphatidic acid in the cytosol by 65%, the activity with aqueously dispersed phosphatidic acid is inhibited 10%
EDTA
-
1.0-2.0 mM, complete loss of cytosolic activity, reduced microsomal activity
EDTA
-
complete inhibition at 2 mM
F-
-
50 mM, 80% inhibition
F-
-
activity with aqueously dispersed phosphatidic acid
F-
-
50 mM, 90% inhibition
Insulin
markedly decreases the amounts of lipin and PAP activity in microsomes, effects of insulin are attenuated by rapamycin or by inhibiting PI 3 kinase
-
Insulin
-
phosphorylation inhibits activity, lipin 1 is phosphorylated in response to insulin treatment in adipocytes in an mTOR-dependent manner
-
Mg2+
about 75% inhibition at 20 mM, isozyme LPPgamma; about 95% inhibition at 20 mM, isozyme LPPepsilon1
Mg2+
-
2.5 mM, slight inhibition
Mg2+
-
at high concentrations, activity with aqueously dispersed phosphatidic acid
Mg2+
-
15 mM MgCl2, 10-20% inhibition of PAP-2
Mg2+
-
inhibition of reaction with diacylglycerol diphosphate. Little effect on reaction with lysophosphatidic acid and phosphatidic acid
Mn2+
-
above 0.1 mM, when assayed in presence of 5 mM MgCl2
Mn2+
-
activity with aqueously dispersed phosphatidic acid
Mn2+
-
IC50: 0.066 mM, reaction with phosphatidic acid. IC50: 0.01 mM, reaction with diacylglycerol diphosphate. IC50: 0.091 mM, reaction with lysophosphatidic acid
N-ethylmaleimide
-
-
N-ethylmaleimide
-
inhibition of the 45-kDa and 104-kDa enzyme forms
N-ethylmaleimide
-
potent inhibitor
NaF
-
-
NaF
-
5 mM, 21% inhibition of reaction with phosphatidic acid, 30% inhibition of reaction with diacylglycerol diphosphate and 44% inhibition of the reaction with lysophosphatidic acid
NEM
-
inhibition of cytosolic and light membrane activity
NEM
-
the enzyme from plasma membrane is insensitive to inhibition, the enzyme from cytosol and microsomes is sensitive to NEM
NEM
inhibition of isozyme DPPL1; inhibition of isozyme DPPL2
NEM
-
inhibition of PAP-1
NEM
-
the Mg2+-dependent enzyme is inhibited, the Mg2+-independent enzyme is unaffected
NEM
-
1 mM, 80% inhibition of Mg2+-dependent enzyme, 10% inhibition of Mg2+-independent enzyme
NEM
-
the Mg2+-dependent enzyme form is inhibited, the Mg2+-independent enzyme form is not inhibited
NEM
-
2 mM, complete inhibition of PAP-1. NEM, up to 8 mM has little effect on PAP-2
NEM
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isozyme PAP1 is sensitive to NEM, while isozyme PAP2 is not
NEM
-
70% inhibition of isozyme PAP-1; 70% inhibition of isozyme PAP-1, 30% inhibition of isozyme PAP-2
NEM
-
45000 Da enzyme form, at 1 mM
NEM
-
IC50: 0.23 mM, reaction with phosphatidic acid. IC50: 0.12 mM, reaction with diacylglycerol diphosphate. IC50: 0.17 mM, reaction with lysophosphatidic acid
NEM
-
potent inhibition of LPP1
NEM
-
the yeast DPP1-encoded PAP2 activity is insensitive to NEM, whereas LPP1-encoded PAP2 activity is sensitive to NEM
p-chloromercuriphenylsulfonic acid
-
45000 Da enzyme form, at 1 mM
p-chloromercuriphenylsulfonic acid
-
-
PCMB
-
-
PCMB
-
0.05 mM, 90% inhibition
Phenylglyoxal
-
inhibition of the 45-kDa and 104-kDa enzyme forms
Phenylglyoxal
-
inhibition of the 45000 Da enzyme form and the 104000 Da enzyme form
Phenylglyoxal
-
IC50: 7 mM, reaction with phosphatidic acid. IC50: 3.4 mM, reaction with diacylglycerol diphosphate. IC50: 2.5 mM, reaction with lysophosphatidic acid
Phenylglyoxal
-
is an arginine reactive compound, inhibits PAP1 activity in dose-dependent manner
phosphatidic acid
-
competitive inhibition
phosphatidic acid
-
competitive with respect to diacylglycerol diphosphate
phosphatidic acid
-
substrate inhibition
phytosphingosine
-
-
phytosphingosine
-
inhibition of PAH1
propanolol
-
slight stimulation
propanolol
-
effective inhibitor of type 1 phosphatidic acid phosphatase, modest inhibitor of phosphatidic acid phosphatase PAP-2a, PAP-2b and PAP-2c
propanolol
-
inhibition of the 45000 Da enzyme form and the 104000 Da enzyme form
propranolol
-
inhibition of PAP-1
propranolol
-
moderately effective inhibitor of LPP activity
propranolol
-
inhibition of the 45-kDa and 104-kDa enzyme forms
propranolol
-
IC50: 2.51 mM, reaction with phosphatidic acid. IC50: 1.68 mM, reaction with diacylglycerol diphosphate. IC50: 7.17 mM, reaction with lysophosphatidic acid
propranolol
-
interacts with the Mg2+-binding site of the enzyme, inhibits PAP1 activity in dose-dependent manner
siRNA
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rat2 fibroblasts treated with siRNA for LPP2 show a ca. 60% decrease in mRNA for the targeted LPP
-
siRNA
-
rat2 fibroblasts treated with siRNA for LPP1 show about a 60% decrease in mRNA for the targeted LPP
-
siRNA
-
decrease of LPP1 mRNA by ca. 90%, knockdown of endogenous LPP1 activity by about 50% and increase of lyso-phosphatidic acid-induced migration
-
spermine
-
above 1 mM
spermine
-
55% inhibition at equimolar concentration of substrate, PAP-2
sphinganine
-
-
sphinganine
-
inhibition of PAH1
sphingosine
-
-
sphingosine
-
93% inhibition at equimolar concentration with pure phosphatidic acid. 29% inhibition with equimolar concentrations of phosphatidic acid mixed with phosphatidylcholine
sphingosine
-
inhibition of PAH1
Triton X-100
-
-
Triton X-100
-
slight depression of activity with aqueously dispersed phosphatidic acid
Tween 20
-
hydrolysis of phosphatidate bound to microsomal membrane in presence of optimal concentration of 8 mM
Zn2+
-
-
Zn2+
-
above 0.1 mM, when assayed in presence of 5 mM MgCl2
Zn2+
-
zinc depletion increases the enzyme activity in vivo, stress condition of zinc depletion induces DPP1 expression
Zn2+
-
PAP2 activity is also inhibited by Zn2+ ions in a mechanism that involves the formation of DGPP-Zn2+ complexes
additional information
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light inhibition of PAP2 in ROS is a transducin-mediated mechanism
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additional information
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light regulation of the lipid phosphate phosphatases, overview
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additional information
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no inhibition by NEM
-
additional information
the enzyme is insensitive to N-ethylmaleimide; the enzyme is insensitive to N-ethylmaleimide; the enzyme is insensitive to N-ethylmaleimide
-
additional information
the enzyme is insensitive to N-ethylmaleimide; the enzyme is insensitive to N-ethylmaleimide; the enzyme is insensitive to N-ethylmaleimide
-
additional information
the enzyme is insensitive to N-ethylmaleimide; the enzyme is insensitive to N-ethylmaleimide; the enzyme is insensitive to N-ethylmaleimide
-
additional information
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the enzyme is insensitive to N-ethylmaleimide; the enzyme is insensitive to N-ethylmaleimide; the enzyme is insensitive to N-ethylmaleimide
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additional information
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caspase3/7 inhibitor N-acetyl-Asp-Glu-Val-Asp-CHO blocks cellular effects of lysophosphatidic acid and sphingosine 1-phosphate on p42/p44 MAPK pathway
-
additional information
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no inhibition by NEM
-
additional information
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CHAPS-insoluble LPP1 is resistant to the actin-disrupting drug cytochalasin D. CHAPS-resistant floating complexes containing LPP1 are sensitive to cholesterol depletion
-
additional information
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insensitive to inhibition by the alkylating agent N-ethyl maleimide
-
additional information
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the presqualene diphosphate phosphatase is a potent Mg2+-independent, NEM-insensitive type II PAP
-
additional information
mitotic phosphorylation of lipin 1 inhibits its phosphatidic acid phosphatase activity
-
additional information
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presence of EDTA or EGTA does not significantly affect enzyme activity
-
additional information
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no inhibition by NEM
-
additional information
epinephrine and oleic acid promote dephosphorylation of lipin 1, insulin and epinephrine control lipin primarily by changing localization rather than intrinsic PAP activity, overview
-
additional information
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PAP-1 chemical inhibition does not reduce the synergistic activation of group IVA phospholipase A2
-
additional information
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mitotic phosphorylation of lipin 2 inhibits its phosphatidic acid phosphatase activity
-
additional information
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phosphorylation inhibits activity, phosphorylation of lipin 1 on multiple sites correlates with a decrease of its microsomal-bound pool
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additional information
no inhibition by N-ethylmaleimide
-
additional information
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no inhibition by N-ethylmaleimide
-
additional information
-
no inhibition by NEM
-
additional information
-
insensitive to inhibition by the alkylating agent N-ethyl maleimide
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additional information
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no effect on the enzyme forms by choline
-
additional information
-
phosphorylation of Pah1p inhibits its PAP1 activity. Pah1p is phosphorylated in vivo on at least 12 sites, including seven Ser/Thr-Pro (S/T-P) motifs. Pah1p is phosphorylated in mitotic cells in a Cdk1/Cdc28p-dependent manner. Mutations in the Nem1p-Spo7p complex result in hyperphosphorylation of Pah1p
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additional information
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the isozymes are not affected by wounding or by treatment with jasmonic acid
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