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(12beta,20R)-12-hydroxy-20,25-epoxydammarane-3,6-dione
-
(1R,2R,3aS,5aS,6aR,7aS,9R,11R,11aS,12aR,13aR,15aR)-2,3a,11,11a-tetrahydroxy-9,15a-dimethyl-1-(5-oxo-2,5-dihydrofuran-3-yl)icosahydro-7aH,13aH-cyclopenta[7,8]phenanthro[2,3-b]pyrano[3,2-e][1,4]dioxine-13a-carbaldehyde
-
-
(1R,2R,3aS,5aS,6aR,7aS,9S,11R,11aS,12aR,13aR,15aR)-3a,11,11a-trihydroxy-9-(hydroxymethyl)-15a-methyl-1-(5-oxo-2,5-dihydrofuran-3-yl)-2-(2-oxopropanoyl)icosahydro-7aH,13aH-cyclopenta[7,8]phenanthro[2,3-b]pyrano[3,2-e][1,4]dioxine-13a-carbaldehyde
-
-
(1R,3aS,5aS,6aR,7aS,9R,11R,11aS,12aR,13aR,15aR)-13a-formyl-3a,11a-dihydroxy-9,15a-dimethyl-1-(5-oxo-2,5-dihydrofuran-3-yl)icosahydro-1H,7aH-cyclopenta[7,8]phenanthro[2,3-b]pyrano[3,2-e][1,4]dioxin-11-yl beta-D-glucopyranoside
-
-
(1R,3aS,5aS,6aR,7aS,9R,11R,11aS,12aR,13aR,15aR)-3a,11,11a-trihydroxy-9,15a-dimethyl-1-(5-oxo-2,5-dihydrofuran-3-yl)icosahydro-7aH,13aH-cyclopenta[7,8]phenanthro[2,3-b]pyrano[3,2-e][1,4]dioxine-13a-carbaldehyde
-
-
(1R,3aS,5aS,6aR,7aS,9S,11R,11aS,12aR,13aR,15aR)-3a,11,11a-trihydroxy-9-(hydroxymethyl)-15a-methyl-1-(5-oxo-2,5-dihydrofuran-3-yl)icosahydro-7aH,13aH-cyclopenta[7,8]phenanthro[2,3-b]pyrano[3,2-e][1,4]dioxine-13a-carbaldehyde
-
-
(1S,3aR,3bR,12aR,14R)-10-fluoro-14-hydroxy-3a,3b,6,6,12a-pentamethyl-1-[(2R)-2,6,6-trimethyloxan-2-yl]-2,3,3a,3b,4,5a,6,7,12,12a,12b,13,14,14a-tetradecahydrocyclopenta[5,6]naphtho[2,1-b]carbazol-5(1H)-one
-
(1S,3aR,3bR,12aR,14R)-14-hydroxy-3a,3b,6,6,12a-pentamethyl-1-[(2R)-2,6,6-trimethyloxan-2-yl]-2,3,3a,3b,4,5a,6,7,12,12a,12b,13,14,14a-tetradecahydrocyclopenta[5,6]naphtho[2,1-b]carbazol-5(1H)-one
-
(1S,3aR,3bR,12aR,14R)-14-hydroxy-3a,3b,6,6,12a-pentamethyl-10-(trifluoromethoxy)-1-[(2R)-2,6,6-trimethyloxan-2-yl]-2,3,3a,3b,4,5a,6,7,12,12a,12b,13,14,14a-tetradecahydrocyclopenta[5,6]naphtho[2,1-b]carbazol-5(1H)-one
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(20R)-20,25-epoxydammarane-3,6,12-trione
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(3beta,12beta,20R)-12-hydroxy-3-phenoxy-20,25-epoxydammaran-6-one
-
(3beta,12beta,20R)-12-hydroxy-3-[(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)oxy]-20,25-epoxydammaran-6-one
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(3beta,12beta,20R)-12-hydroxy-3-[4-(trifluoromethoxy)phenoxy]-20,25-epoxydammaran-6-one
-
(3beta,12beta,20R)-3-(ethenyloxy)-12-hydroxy-20,25-epoxydammaran-6-one
-
(3beta,12beta,20R)-3-ethoxy-12-hydroxy-20,25-epoxydammaran-6-one
-
(3E,5beta,15beta,16beta)-16-(acetyloxy)-3-(hydroxyimino)-8-methyl-14,15-epoxybufa-20,22-dienolide
-
-
(3E,5beta,15beta,16beta)-16-(acetyloxy)-3-(methoxyimino)-8-methyl-14,15-epoxybufa-20,22-dienolide
-
-
(3E,5beta,15beta,16beta)-16-(acetyloxy)-3-[(2-aminoethoxy)imino]-8-methyl-14,15-epoxybufa-20,22-dienolide
-
most potent inhibitor
(5aR,7R,8S,10aR,10bR)-7-hydroxy-1,1,5a,10a,10b-pentamethyl-8-[(2R)-2,6,6-trimethyloxan-2-yl]hexadecahydrocyclopenta[5,6]naphtho[2,1-c]azepine-3,12-dione
-
(5aR,8S,10aR,10bR,12R)-12-hydroxy-1,1,5a,10a,10b-pentamethyl-8-[(2R)-2,6,6-trimethyloxan-2-yl]tetradecahydro-1H-cyclopenta[5,6]naphtho[2,1-c]oxepine-3,7-dione
-
(5aR,8S,10aR,10bR,12S)-12-hydroxy-1,1,5a,10a,10b-pentamethyl-8-[(2R)-2,6,6-trimethyloxan-2-yl]tetradecahydro-1H-cyclopenta[5,6]naphtho[2,1-c]oxepine-3,7-dione
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(6alpha,12beta,20R)-12-hydroxy-6-[(prop-2-en-1-yl)oxy]-20,25-epoxydammaran-3-one
-
(6alpha,12beta,20R)-6,12-bis(benzyloxy)-20,25-epoxydammaran-3-one
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(6alpha,12beta,20R)-6,12-bis[(prop-2-en-1-yl)oxy]-20,25-epoxydammaran-3-one
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(6alpha,12beta,20R)-6-(benzyloxy)-12-hydroxy-20,25-epoxydammaran-3-one
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(6alpha,20R)-6-hydroxy-20,25-epoxydammarane-3,12-dione
-
1,8,9-trihydroxy-3-methoxy-6H-[1]benzofuro[3,2-c]chromen-6-one
-
i.e. wedelolactone, inhibitor of kidney Na+K+-ATPase and ligand for the central benzodiazepine receptor
1-chloro-2,4-dinitrobenzene
-
inhibition of the transport activity of the Na-K pump
12,20-dihydroxydammar-24-en-3-yl 2-O-D-glucopyranosyl-D-glucopyranoside
-
-
12,20-dihydroxydammar-24-en-3-yl D-glucopyranoside
-
-
19-hydroxy-2''-oxovoruscharin
-
i.e. UNBS1450, a trans-trans-cis cardiotonic steroid
1H-[1,2,4]oxadiazole[4,3-a]quinoxalin-1-one
-
ODQ, inhibition of SNP-induced pump stimulation
2,3-dihydroxy-6H-[1,3]dioxolo[5,6][1]benzofuro[3,2-c]chromen-6-one
-
inhibitor of kidney Na+K+-ATPase and ligand for the central benzodiazepine receptor
2,8,9-trihydroxy-3-methoxy-6H-[1]benzofuro[3,2-c]chromen-6-one
-
inhibitor of kidney Na+K+-ATPase and ligand for the central benzodiazepine receptor
2,9-dihydroxy-3,8-dimethoxy-6H-[1]benzofuro[3,2-c]chromen-6-one
-
inhibitor of kidney Na+K+-ATPase and ligand for the central benzodiazepine receptor
2-aminoethyl-methanethiosulfonate
-
inhibition of mutants F323C, P333C, E334C, G335C, I322C, G326C and A330C
3,8,9-trihydroxy-2-methoxy-6H-[1]benzofuro[3,2-c]chromen-6-one
-
inhibitor of kidney Na+K+-ATPase and ligand for the central benzodiazepine receptor
3-[(2-O-D-glucopyranosyl-D-glucopyranosyl)oxy]-12-hydroxydammar-24-en-20-yl D-glucopyranoside
-
-
3-[(3S,3aS,4R,5aR,6S,9aR,9bS)-4-hydroxy-6,9a,9b-trimethyl-8-oxo-3-[(2R)-2,6,6-trimethyloxan-2-yl]dodecahydro-1H-cyclopenta[a]naphthalen-6-yl]propanoic acid
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4,7-diacetoxy-14-hydroxydolast-1(15),8-diene
-
-
4-acetoxy-9,14-dihydroxydolast-1(15),7-diene
-
-
4-[(1R,3aS,5aS,6aR,7aS,9R,11R,11aS,12aR,13aR,15R,15aS)-3a,11,11a,15-tetrahydroxy-13a-(hydroxymethyl)-9,15a-dimethylicosahydro-1H,7aH-cyclopenta[7,8]phenanthro[2,3-b]pyrano[3,2-e][1,4]dioxin-1-yl]furan-2(5H)-one
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-
4-[(1R,3aS,5aS,6aR,7aS,9S,11R,11aS,12aR,13aR,15aR)-3a,11,11a-trihydroxy-9,13a-bis(hydroxymethyl)-15a-methylicosahydro-1H,7aH-cyclopenta[7,8]phenanthro[2,3-b]pyrano[3,2-e][1,4]dioxin-1-yl]furan-2(5H)-one
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4-[(1R,3aS,5aS,6aR,7aS,9S,11R,11aS,12aR,13aR,15R,15aS)-3a,11,11a,15-tetrahydroxy-9,13a-bis(hydroxymethyl)-15a-methylicosahydro-1H,7aH-cyclopenta[7,8]phenanthro[2,3-b]pyrano[3,2-e][1,4]dioxin-1-yl]furan-2(5H)-one
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-
5-hydroxydecanoate
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presence of 5 mM ATP, inhibitory above 1 mM. Presence of 0.05 mM ATP, inhibitory above 0.25 mM. No effect on ouabain-sensitiviy of the enzyme
8-methoxycoumestrol
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inhibits the isozyme alpha1beta1 Na,K-ATPase, mechanism, overview
A-769662
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inhibits the Na+-K+-ATPase transport activity and cell surface abundance in L6 cells, which is independent of AMP kinase activation, overview
alpha2-adrenergic agonists
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negative modulator
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astragaloside III
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from dried roots of Astragalus membraneceus or var. mongholicus
ATP
-
competitive inhibitor of K+-phosphatase activity
benzyltriethylammonium chloride
-
inhibition of pump current is dependent on membrane potential
bradykinin
-
negative modulator
cholic acid
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from dried bile of Ursus arctos or Selenarctos thibetanus
cinobufotalin
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27.5% inhibition at 0.01 mM
cyclosporin A
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diminishs induction of alpha1 protein in activated lymphocytes
dammar-24-ene-3,12,20-triol
-
-
dammar-24-ene-3,6,12,20-tetrol
-
-
dansylcysteinyl-mercuric chloride
-
-
diphenyl diselenide
-
activity is restored by DTT
dopamine
-
negative modulator
endothelin
-
negative modulator
-
epicatechin-3-gallate
-
solubilization of the Na+,K+-ATPase with a nonionic detergent reduces sensitivity to epigallocatechin-3-gallate
epigallocatechin-3-gallate
-
noncompetitive with respect to ATP, reduces the affinity for vanadate, shifts the equilibrium of E1P and E2P toward E1P, and reduces the rate of the E1P to E2P transition
epinephrine
-
0.5 mM epinephrine added for 20 min, decreases the activity of the enzyme by around 50%. Treatment with Rp-cAMP, indomethacin, PP2, SB202190, and PD98059 completely abrogate the effect of epinephrine
ethylester of glutathione
-
inhibition of the transport activity of the Na-K pump
ethylmercurithiosalicylate
-
-
fenoldopam
-
induces inhibition of Na+ ?K+-ATPase activity in HK-2 cells. Ouabain protects against the cyclic adenosine monophosphate accumulation and Na+ ?K+-ATPase inhibition induced by the D1 receptor agonist fenoldopam in HK-2 cells. Chronic ouabain treatment decreases the protein and mRNA expression levels of the D1 receptor and increases the basal phosphorylation of the D1 receptor in HK-2 cells
genistein
-
tyrosine kinase inhibitor, block phosphorylation of alpha-subunit of the Na+,K+-ATPase
ginsenoside Rh2
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from dried roots of Panax ginseng or Panax notoginseng
glyburide
-
presence of 5 mM ATP, slightly stimulating up to 1 mM, inhibitory above. Presence of 0.05 mM ATP, stimulating at least up to 3 mM
glycyrrhizin
-
from roots of Glycyrrhiza uralensis , Glycyrrhiza inflata, or Glycyrrhiza glabra
herbimycin A
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tyrosine kinase inhibitor, block phosphorylation of alpha-subunit of the Na+,K+-ATPase
isovaleric acid
-
isovaleric acid injection significantly inhibits Na+,K+-ATPase activity by 25% in cerebral cortex of rats 2 or 24 h after administration, while pre-treatment of rats with creatine completely prevents the inhibitory effects of isovaleric acid on Na+,K+-ATPase
jujuboside B
-
from mature seeds of Ziziphus jujube var. spinosa
L-homocysteine
-
inhibitory effect is reversed by alanine
lauric acid
-
presence of 5 mM ATP, inhibitory above 0.25 mM. Presence of 0.05 mM ATP, stimulating up to 0.3 mM, inhibitory above
lavendustin A
-
tyrosine kinase inhibitor, block phosphorylation of alpha-subunit of the Na+,K+-ATPase
Lyn kinase
-
Lyn kinase directly binds to the Na+,K+-ATPase alpha3 subunit for regulation of activity
-
m-trifluoromethyl-diphenyl diselenide
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i.e. (m-CF3C6H4Se)2, activity is restored by DTT
methyl 3-[(3S,3aS,4R,5aR,6R,7R,9aR,9bS)-4-hydroxy-7-(2-hydroxypropan-2-yl)-6,9a,9b-trimethyl-8-oxo-3-[(2R)-2,6,6-trimethyloxan-2-yl]dodecahydro-1H-cyclopenta[a]naphthalen-6-yl]propanoate
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methyl 3-[(3S,3aS,4R,5aR,6R,7S,9aR,9bS)-4-hydroxy-6,9a,9b-trimethyl-8-oxo-7-(prop-2-en-1-yl)-3-[(2R)-2,6,6-trimethyloxan-2-yl]dodecahydro-1H-cyclopenta[a]naphthalen-6-yl]propanoate
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methyl 3-[(3S,3aS,4R,5aR,6S,9aR,9bS)-4-hydroxy-6,9a,9b-trimethyl-8-oxo-3-[(2R)-2,6,6-trimethyloxan-2-yl]dodecahydro-1H-cyclopenta[a]naphthalen-6-yl]propanoate
-
monosodium glutamate
-
selenofuranoside therapy is able to prevent the inhibition of the enzyme activity in the hippocampus but not in the brain cortex
MTSET
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[2-(trimethylammonium)ethyl]methanethiosulphonate bromide, inhibits mutants G803C, V805C
Na+
-
25% inhibition at 80 mmol/l
Na/K ATPase-alpha1-specific siRNA A1
-
Na/K ATPase-alpha1-specific siRNA A2
-
Na/K ATPase-alpha1-specific siRNA A3
-
Na/K ATPase-alpha1-specific siRNA A4
-
O-[(3beta,12beta,20R)-12-hydroxy-6-oxo-20,25-epoxydammaran-3-yl] O-methyl 2-imidothiodicarbonate
-
odoroside A
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i.e. 3beta-O-(beta-D-diginosyl)-14-hydroxy-5beta,14beta-card-20(22)-enolide, isolated from the stems and twigs of Nerum oleander, inhibits the enzyme's ATPase activity
Omeprazole
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inhibit mutants G803C, T804C, V805C
p-chloro-diphenyl diselenide
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i.e. (p-ClC6H4Se)2, activity is restored by DTT
p-methoxyl-diphenyl diselenide
-
i.e. (p-CH3OC6H4Se)2, activity is restored by DTT
Pb2+
-
inhibitory effect of Pb2+ on the transport cycle of the Na+,K+-ATPase, overview. Pb2+ inhibits cycling of the enzyme, but it does not affect cytoplasmic Na+ binding and release of Na+ ions at the extracellular side at concentrations below 0.010 mM
polygalacic acid
-
from dried roots of Platycodon grandiflorum
PP1
-
Src kinase inhibitor
Prostaglandins
-
negative modulator
-
reduced glutathione
-
extracellular and, or intracellular, inhibition of the transport activity of the Na-K pump
saikosaponin A
-
from dried roots of Bupleurum chinense or Bupleurum scorzonerifolium
sarsasapogenin
-
from dried roots of Anemarrhena asphodeloides
suramin
-
potent inhibitor, acts on the inside surface of the sodium pump
tetraethylammonium chloride
-
inhibition of pump current is independent on membrane potential
Tumor necrosis factor alpha
-
TNF-alpha, TNF-alpha affects the Na+-K+ pump via PGE2-dependent pathways
-
ursolic acid
-
from whole plant of Prunella vulgaris with dried flowers
Yes kinase
-
regulator of the Na+,K+-ATPase activity
-
[Au(2,2'-bipyridine)Cl2]+
-
-
[Au(dimethylsulfoxide)2Cl2]+
-
-
[PdCl(dien)]+
-
noncompetitive, affinity for binding in decreasing order: [PdCl4]2-, [PdCl(dien)]+, [PdCl(Me4dien)]+. Addition of L-cysteine or glutathoione before exposure to Pd(II) complexes prevents inhibition
[PdCl(Me4dien)]+
-
noncompetitive, affinity for binding in decreasing order: [PdCl4]2-, [PdCl(dien)]+, [PdCl(Me4dien)]+. Addition of L-cysteine or glutathoione before exposure to Pd(II) complexes prevents inhibition
-
[PdCl4]2-
-
noncompetitive, affinity for binding in decreasing order: [PdCl4]2-, [PdCl(dien)]+, [PdCl(Me4dien)]+. Addition of L-cysteine or glutathoione before exposure to Pd(II) complexes prevents inhibition
BAY-K8644
-
a calcium channel agonist, the effect is blocked by a phosphatidylinositol-3 kinase inhibitor wortmannin
BAY-K8644
-
a calcium channel agonist, the effect is blocked by a phosphatidylinositol-3 kinase inhibitor wortmannin
bufalin
-
inhibition of the enzyme, enhancement of the acidification of the late endosome, alteration in membrane traffic
bufalin
-
from dried venom of Bufo gargarizans or Bufo bufo melanostictus
Ca2+
-
CaCl2 up to 300 microM does not affect Na+/K+-ATPase activity, but CaCl2 above 1 mM inhibits the activity
Ca2+
-
enzyme from anterior intestine is 5-fold more sensitive than enzymes from pyloric caeca and posterior intestine
digitoxigenin
-
-
digoxin
-
-
Ethacrynic acid
-
-
ethanol
-
-
ethanol
-
inhibits the enzyme in Golgi membranes of cerebellar neurons leading to potentiation of GABAergic transmission at Golgi cell-to-granule cell synapses throughan increase in Golgi cell excitability
Mg2+
-
considerable inhibition of enzyme activity is seen above 5 mM Mg2+
Mg2+
-
IC50: 0.0008 mM; IC50: 0.0012 mM; IC50: 0.012 mM
Na/K ATPase-alpha1-specific siRNA A1
-
0% decreases in expression of human alpha subunit in 293T cells
-
Na/K ATPase-alpha1-specific siRNA A1
-
-
-
Na/K ATPase-alpha1-specific siRNA A2
-
20% decreases in expression of human alpha subunit in 293T cells
-
Na/K ATPase-alpha1-specific siRNA A2
-
-
-
Na/K ATPase-alpha1-specific siRNA A3
-
20% decreases in expression of human alpha subunit in 293T cells
-
Na/K ATPase-alpha1-specific siRNA A3
-
-
-
Na/K ATPase-alpha1-specific siRNA A4
-
40% decreases in expression of human alpha subunit in 293T cells
-
Na/K ATPase-alpha1-specific siRNA A4
-
-
-
oleandrin
-
-
oleandrin
-
oleandrin treatment results in selective inhibition of human cancer cell growth but not rodent cell proliferation, which corresponds to the relative level of Na,K-ATPase alpha3 subunit protein expression. A correlation is observed between the ratio of alpha3 to alpha1 isoforms and the level of oleandrin uptake during inhibition of cell growth and initiation of cell death, the higher the alpha3 expression relative to alpha1 expression, the more sensitive the cell is to treatment with oleandrin
oleandrin
-
oleandrin treatment results in selective inhibition of human cancer cell growth but not rodent cell proliferation, which corresponds to the relative level of Na,K-ATPase alpha3 subunit protein expression. A correlation is observed between the ratio of alpha3 to alpha1 isoforms and the level of oleandrin uptake during inhibition of cell growth and initiation of cell death, the higher the alpha3 expression relative to alpha1 expression, the more sensitive the cell is to treatment with oleandrin
oleanolic acid
-
-
oleanolic acid
-
from whole plant of Prunella vulgaris with dried flowers
oligomycin
-
inhibits (Na+,K+)-ATPase reaction and Na+-ATPase reaction, has little effect on the K+-phosphatase reaction and can stimulate the ADP/ATP exchange reaction
oligomycin
-
not completely inhibits but decreases the rate of turnover of transport and of the hydrolysis reaction. Oligomycin affects the extracellular side of the system, Na+ on the cytoplasmic side of the system is necessary for the effect, oligomycin decreases the rate of transition from the Na+ form to the K+ form of the enzyme, but has no effect on the rate of the reverse reaction
orthovanadate
-
up to 87% inhibition
orthovanadate
-
increasing orthovanadate concentrations from 0.0001 mM to 1 mM inhibit total ATPase activity by around 75%
orthovanadate
-
up to 67% inhibition in absence of NH4+
orthovanadate
-
up to 75% inhibition at 0.05 mM
orthovanadate
-
about 44% inhibition at 3 mM
Ouabain
-
ouabain up to 1 mM decreases silkworm ATPase activity to 42% of the maximal ATPase activity in presence of 10 mM NaCl and 30 mM KCl
Ouabain
-
up to 87% inhibition
Ouabain
-
76.4% residual activity at 3 mM
Ouabain
-
up to 67% inhibition in absence of NH4+
Ouabain
-
about 70% inhibition at 3 mM
Ouabain
-
ouabain triggers an apoptotic cascade that involves NCX and CaMKII as a downstream effector. Ouabain simultaneously activates an antiapoptotic cascade involving PI3K/AKT which is however, insufficient to completely repress apoptosis. The NCX inhibitor KB-R7943 and by the CaMKII inhibitors, KN93 and AIP prevent ouabain-induced apoptosis without affecting inotropy. Ouabain produces in the cat at 25 nM a 43% decrease in cell viability due to apoptosis and necrosis
Ouabain
-
inhibition of enzyme, enhancement of the acidification of the late endosome
Ouabain
-
ouabain does not affect TNF-alpha-induced mRNA expression but inhibits TNF-alpha-induced protein expression
Ouabain
-
specific inhibitor
Ouabain
-
73% inhibition at 3 mM
Ouabain
-
interaction is dependent on the conformation and phosphorylation state of the protein
Ouabain
-
ouabain triggers an apoptotic cascade that involves NCX and CaMKII as a downstream effector. Ouabain simultaneously activates an antiapoptotic cascade involving PI3K/AKT which is however, insufficient to completely repress apoptosis.The NCX inhibitor KB-R7943 and by the CaMKII inhibitors, KN93 and AIP prevent ouabain-induced apoptosis without affecting inotropy
Ouabain
-
complete inhibition at 0.001 mM
Ouabain
-
-
671274, 673231, 675717, 675725, 695469, 695856, 696017, 699696, 700430, 701003, 710811
Ouabain
-
ouabain triggers an apoptotic cascade that involves NCX and CaMKII as a downstream effector. Ouabain simultaneously activates an antiapoptotic cascade involving PI3K/AKT which is however, insufficient to completely repress apoptosis. The NCX inhibitor KB-R7943 and by the CaMKII inhibitors, KN93 and AIP prevent ouabain-induced apoptosis without affecting inotropy. Ouabain produces in the rat at 0.002 mM a 43% decrease in cell viability due to apoptosis and necrosis
Ouabain
-
55% inhibition at 0.02 mM
Ouabain
-
6.1% inhibition at 0.01 mM
Ouabain
-
about 30% inhibition at 2 mM
Ouabain
-
specific inhibitor
Ouabain
-
enzyme from anterior intestine is ten-fold more sensitive than enzymes from pyloric caeca and posterior intestine
Ouabain
a cardiac glycoside derived from Strophanthus gratus, ouabain is deeply inserted into the transmembrane domain with the lactone ring very close to the bound K+. Low-affinity ouabain-bound state due to antagonism between ouabain and K+. The closure of the binding cavity confers a high affinity, homology model for the high affinity state, structures, overview. Binding of sugar moiety and steroid core, overveiw
Ouabain
-
specific inhibitor
Ouabain
-
Na+/K+-ATPase specific inhibitor
Ouabain
-
about 50% inhibition at 3 mM, ouabain inhibition increases about 80% in the presence of NH4+ with a 3fold lower KI value
oubain
-
-
oubain
-
two apparently different oubain binding sites
oubain
-
the IC50 value is higher in neonates than in children
oubain
-
K+ completely abolishes oubain binding to alpha1-beta1 isoenzymes. Residual oubain binding is still observed at high K+ concentrations for alpha2-beta1 and alpha3-beta1 complexes
oubain
-
K+ protects against inhibition, probably due to phosphorylating effect
oubain
-
quantitative aspects of the interaction between oubain and the enzyme in vitro
oubain
-
half-maximal inhibition at 0.1 mM
palytoxin
-
-
palytoxin
-
mild, non-toxic, exposures to the Na+/K+-ATPase inhibitor palytoxin synergistically sensitizes the vulnerability of neurons to normally non-toxic concentrations of domoic acid, leaving NMDA receptor-mediated excitotoxic response unaltered. Palytoxin causes a voltage-sensitive Na+ channel-independent increase in intracellular Na+. Enhancement of the excitotoxic response to domoic acid by palytoxin is time-dependent and is not affected by gene expression inhibitors
perillyl alcohol
-
a monoterpene, inhibits Na/K-ATPase, non-competitive inhibition for Na+ and K+ and an uncompetitive inhibition for ATP in brain and kidney
perillyl alcohol
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a monoterpene, inhibits Na/K-ATPase showing a noncompetitive inhibition profile to Na+ and K+ and an uncompetitive inhibition towards ATP. The generated electrochemical gradient is essential for a number of other cellular functions
prostaglandin E2
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putrescine
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putrescine
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putrescine inhibits (Na+, K+)-ATPase phosphorylation and activity in juvenile and adult shrimp gill
spermidine
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spermidine
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spermidine inhibits (Na+, K+)-ATPase phosphorylation and activity in juvenile and adult shrimp gill
strophanthidin
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tyrosine kinase inhibitor, block phosphorylation of alpha-subunit of the Na+,K+-ATPase
strophanthidin
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29.6% inhibition at 0.01 mM
vanadate
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vanadate
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20fold less sensitive to vanadate than alpha1 and 3; 20 times more sensitive to vanadate than alpha2
vanadate
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epigallocatechin-3-gallate reduces the affinity for vanadate, shifts the equilibrium of E1P and E2P toward E1P, and reduces the rate of the E1P to E2P transition
additional information
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not inhibitory: NH4+. At elevated concentrations of NH4+, enzyme is fully active and K+ cannot displace NH4+ from its exclusive binding sites
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additional information
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odoroside A and ouabain potently reduce NF-kappaB-inducible de novo protein synthesis, largely due to its ability to block Na+-dependent transport of amino acids across the plasma membrane, but not to interfering with the translation machinery
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additional information
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ETB receptor inhibits Na+-K+ ATPase activity by facilitating extracellular Ca2+ entry and Ca2+ release from endoplasmic reticulum
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additional information
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inhibitory potencies of cardenolide glycosides, isolated from the roots of Pergularia tomentosa, on Na+,K+-ATPase activity
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additional information
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spermine has a negligible effect (less than 10%) on enzyme activity
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additional information
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enzyme activity is inhibited by excess ATP
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additional information
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decrease in extracellular pH inhibits Na+-K+ pump activity
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additional information
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physical training is effective against Na+,K+-ATPase enzyme activity inhibition, while fluid percussion injury induces a decrease in Na+,K+-ATPase activity in the ipsilateral cerebral cortex of sedentary animals
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additional information
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ETB receptor inhibits Na+-K+ ATPase activity by facilitating extracellular Ca2+ entry and Ca2+ release from endoplasmic reticulum
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additional information
cardiac glycosides are efficient inhibitors of the Na+,K+-ATPase
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additional information
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molecular docking and modelling, and inhibitory potencies of steroid-like compounds from Chinese medicinal products, used for promoting the blood circulation, with Na+,K+-ATPase, overview
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