F0211 | Transport

Compound Dose Time Species Model Method Action Result Positive criterion Reference
MCU-i11 10 μM Skeletal Muscle Fibers measured mitochondrial Ca2+ uptake in flexor digitorum brevis (FDB) myofibers freshly isolated from adult mice and previously transfected in vivo with the mitochondria-targeted Ca2+ probe 4mt-GCaMP6f decrease Positive 301
DS16570511 7 μM HEK293A cells HEK293A cell lines expressing the mitochondria-targeted Ca2+ indicator protein aequorin decrease Positive IC50 302
neomycin 400 μM zebrafish zebrafish lateral line hair measrueing cytoplasmic oxidation (HyPer) and mitochondrial Ca2+ uptake (mitoRGECO) increase Positive 315
lovastatin C2C12 myoblasts affect Positive 180
Simvastatin C2C12 myoblasts affect Positive 180
Perhexiline decrease Positive 16
Perhexiline decrease Positive 16
Diazoxide EC50= 40mmol/L, saturation by 100mmol/L Primary Culture of Neonatal Rat Cardiac Ventricular Myocytes flow cytometry and quantitative image analysis of cells stained with fluorescent DC indicators. affect Positive 188
Pinacidil affect Positive 188
thiazolidinediones decrease Positive 35
5-Hydroxydecanoate 500mmol/L Primary Culture of Neonatal Rat Cardiac Ventricular Myocytes flow cytometry and quantitative image analysis of cells stained with fluorescent DC indicators. affect Positive 188
Glibenclamide affect Positive 188
Glibenclamide K1/2 values 1-6 microM heart and liver mitochondria from rat affect Positive 190
promethazine increase Positive 22
clomipramine increase Positive 22
imipramine increase Positive 22
Chlorpromazine increase Positive 22
2,4-dinitrophenol increase Positive 24
2,4-dinitrophenol increase Positive 24
thiazolidinediones decrease Positive 34
1h-benzimidazol-5-amine-2-4-aminophenyl ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
2-(Dimethylamino)-1,3-benzothiazol-6-ol ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
4-[(7-Nitro-2,1,3-benzoxadiazol-4-yl)amino]phenol ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
7,8-Dihydroxy-4-methylcoumarin ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
4-Amino-2-(5-ethyl-benzooxazol-2-yl)-phenol ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
(4-Methoxyphenyl)-[2-(p-anisidino)ethyl]amine ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
3,3'-Diamino-4,4'-dihydroxydiphenyl Sulfone ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
2-(4-Hydroxy-1H-indol-3-yl)acetamide ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
2,5-Bis(2-phenylacetamido)terephthalic acid ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
2,6-Dimethyl-5,12-dihydroindolo[3,2-d][1,3]benzodiazepine;hydrochloride ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
N-(4-{[(4,6-Dimethyl-2-pyrimidinyl)amino]sulfonyl}phenyl)-2,4-dimethoxybenzamide ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
N'-(4-Methoxybenzyl)-N,N-dimethylbenzene-1,3-diamine ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
4-(1,2,3,4-Tetrahydro-benzo[a]phenanthridin-5-yl)-benzene-1,2-diol ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
N-Benzyl-4-methoxyaniline ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
Methyl 2-amino-4-ethyl-5-methylthiophene-3-carboxylate ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
N-(4-(4-Methyl-1-piperazinyl)phenyl)-9-acridinamine ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
4-Chloro-N-(2-hydroxyphenyl)benzenesulfonamide ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
N-(4-Hydroxyphenyl)furan-2-carboxamide ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
(Z)-2-Cyano-3-(3-ethoxy-4-hydroxyphenyl)prop-2-enamide ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
(3-Bromo-4-hydroxyphenyl)[(4-chlorophenyl)sulfonyl]amine ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
2-Chloro-6-methylindolo[1,2-c]quinazolin-12-amine ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
4-(2,3-Dihydro-1H-benzo[f]cyclopenta[c]quinolin-4-yl)benzene-1,2-diol ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
(5E)-5-(4-Hydroxybenzylidene)-2-mercapto-1,3-thiazol-4(5H)-one ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
8-Chloro-2,2-dimethyl-2,3-dihydro-1H-phenothiazin-4(10H)-one ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
2-[(3,4-Dimethylphenyl)sulfonyl]benzene-1,4-diol ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
4-([4-(1H-Benzimidazol-2-yl)phenyl]amino)-4-oxobutanoic acid ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
Ethyl 2-ethoxy-5-hydroxy-1H-indole-3-carboxylate ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
4-(1,2,3,4-Tetrahydrobenzo[a]phenanthridin-5-yl)benzene-1,3-diol ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
N-(Cyclohexylmethyl)-4-methoxyaniline ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
N-(Furan-2-ylmethyl)-1,3-benzodioxol-5-amine ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
5-Nitro-2-phenyl-1H-indole ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
8-Chloro-2,3-dihydro-1H-phenothiazin-4(10H)-one ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
N-(4-Bromophenyl)-4,5,6,7-tetrahydro-1,3-benzothiazol-2-amine ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
2-[2-(2-Aminophenyl)vinyl]-5,7-dimethylquinolin-8-ol ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
4,6-Dimethyl-2-phenyl-2H-pyrazolo[3,4-b]pyridin-3-ol ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
4-Methoxy-2-[(4-piperidylpiperidyl)methyl]phenol ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
N-(5-Isopropyl-1,3,4-thiadiazol-2-yl)-3-nitrobenzamide ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
2-Amino-6-ethyl-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxamide ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
(NE)-N-[[3-[[3-[(E)-hydroxyiminomethyl]-2,4,6-trimethylphenyl]methyl]-2,4,6-trimethylphenyl]methylidene]hydroxylamine ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
N-(3-Fluorophenyl)-2,4,6-tri(propan-2-yl)benzenesulfonamide ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
2-(4-Hydroxy-3-methoxybenzylidene)-1H-indene-1,3(2H)-dione ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
2-[2-(5-Hydroxy-1H-indol-3-yl)ethyl]-1H-isoindole-1,3(2H)-dione ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
2-Furancarboxamide, N-[[(4-methoxyphenyl)amino]thioxomethyl]- ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
2-Amino-N-quinolin-8-yl-benzenesulfonamide ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
(5Z)-5-[(4-Fluorophenyl)methylidene]-1-methyl-3-phenyl-1,3-diazinane-2,4,6-trione ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
2-[4-(1-Adamantyl)phenoxy]-N,N-diethylethanamine;hydrochloride ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
(2Z)-2-(Acetylamino)-N-(4-hydroxyphenyl)-3-phenylprop-2-enamide ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
(5E)-5-[(3-Bromo-4-methoxyphenyl)methylidene]-1-phenyl-2-sulfanylidene-1,3-diazinane-4,6-dione ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
[(3-{[(4-Bromophenyl)amino]carbonyl}phenyl)thio]acetic acid ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
2-[(4-Chlorobenzyl)thio]-6,7-dihydro-5H-pyrrolo[1,2-a]imidazole ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
1-(5-Hydroxy-2-methyl-1-phenyl-1H-indol-3-yl)ethanone ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
2-[(4-Ethylpiperazin-1-yl)methyl]-4-methoxyphenol ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
4-(4-Fluorophenyl)-1,3,5-trimethyl-2,6-diphenylpiperidin-4-ol ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
N-[(E)-1-[5-(4-Bromophenyl)furan-2-yl]-3-[3-(dimethylamino)propylamino]-3-oxoprop-1-en-2-yl]-4-methylbenzamide ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
(2Z)-3-{N-[4-(4-Chlorophenyl)phenyl]carbamoyl}prop-2-enoic acid ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
4-[(E)-3-(4-Ethylpiperazin-1-yl)prop-1-enyl]-N,N-dimethylaniline ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
1,5-Dihydro-4,5-diphenyl-2H-imidazol-2-one ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
2-[(E)-2-(4-Chlorophenyl)ethenyl]-1-methyl-1H-benzimidazole ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
4-[1-Azabicyclo[2.2.2]octan-3-ylidene-[4-(dimethylamino)phenyl]methyl]-N,N-dimethylaniline;hydrochloride ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
4-Oxo-4-((4-(styryl)phenyl)amino)but-2-enoic acid ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
2,5-Dianilinoterephthalic acid ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
4-Methoxy-N-[4-(thiazol-2-ylsulfinamoyl)-phenyl]-benzamide ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
3-[(3,4-Dimethylphenyl)sulfonyl]propanenitrile ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
4-[4-(1,3-Benzoxazol-2-yl)anilino]-4-oxobutanoic acid ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
1-(3-Chlorophenyl)-2,3,4,5,6,7,8,8a-octahydro-1H-isoquinolin-4a-ol;hydrochloride ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
6-Methyl-2-(1,2,2,2-tetrafluoroethyl)-1H-benzimidazole ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
Ethyl 6-amino-5-cyano-2-methyl-4-(2-nitrophenyl)-4H-pyran-3-carboxylate ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
N-(2,1,3-Benzoxadiazol-4-yl)-2,2,2-trifluoroacetamide ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
4-Tert-butyl-N-(4-methylphenyl)benzamide ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
2-Methoxy-4-(morpholin-4-ylmethyl)phenol ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
Bis((1E)-2-phenylvinyl)phosphinic acid ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
1-[2-(Allyloxy)benzyl]-4-benzylpiperidine ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
2,5-Diaminoterephthalic acid ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
N-(1-Adamantylcarbonyl)-N'-(3-cyano-4,5,6,7-tetrahydro-1-benzothien-2-yl)thiourea ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
2-(Isobutylthio)succinic acid ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
N-{4-[Acetyl(methyl)amino]phenyl}-4-biphenylcarboxamide ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
4-[(E)-3-(2-Ethylpiperidin-1-yl)prop-1-enyl]-N,N-dimethylaniline ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
3-(2-Chloro-phenyl)-2-(4-(2-oxo-2H-chromen-3-YL)-thiazol-2-YL)-acrylonitrile ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
Ethyl (7Z)-2-amino-7-(hydroxyimino)-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxylate ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
2-Amino-4-(3,4-dichlorophenyl)thiazole ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
5-(2-Nitrobenzylidene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
3-(4-Bromo-2-thienyl)-2-cyano-2-propenethioamide ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
Benzyl [(6-amino-3,5-dicyano-4-ethylpyridin-2-yl)sulfanyl]acetate ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
N-{2-[(1,3-Diphenyl-1H-pyrazol-5-yl)amino]phenyl}benzamide ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
2-Butyl-5-methylisophthalic acid ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
2-Butylsulfanyl-6-methyl-9H-1,3,4,9-tetraaza-fluorene ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
2-Phenyldipyrrolo[1,2-a:2',1'-c]pyrazine ∼2.5 µM rat skeletal muscle mitochondria measurement of superoxide/H2O2 production affect Positive 162
SB202190 10 μM intact and in permeabilized HeLa cells (MM5 cells expressing mitmutAEQ ) mitochondrial Ca2+ uptake increase Positive 233
Diclofenac 50 μmol/L 2 minutes rat liver mitochondria Assessment of Mitochondrial Ca2+ Efflux; Energized with succinate decrease Positive not mentioned 6
kaempferol 1μM The HeLa cell clone MM5 expressing mitochondrially targeted mutated aequorin was used for [Ca2+]M measurements. [Ca2+]c measurements were carried out using HeLa cells transiently transfected with the plasmid for cytosolic aequorin. increase Positive 234
kaempferol 7μM The HeLa cell clone MM5 expressing mitochondrially targeted mutated aequorin was used for [Ca2+]M measurements. [Ca2+]c measurements were carried out using HeLa cells transiently transfected with the plasmid for cytosolic aequorin. increase Positive EC50 234
Troglitazone 50 μM male CD-1 mice isolated liver mitochondria Assessment of mitochondrial Ca2+ efflux with arsenazo III at 675/685 nm. decrease Positive 331
Ciglitazone 50 μM male CD-1 mice isolated liver mitochondria Assessment of mitochondrial Ca2+ efflux with arsenazo III at 675/685 nm. decrease Positive 331
quercetin 21 μM mitochondrial Ca2+ uptake increase Positive EC50 234
genistein 37μM mitochondrial Ca2+ uptake increase Positive EC50 234
Trimetazidine 10-100µM rat isolated cardiac mitochondria increase Positive 274
CGP37157 1 μmol/L periodically paced rat ventricular myocytes (VMs) under β-adrenergic stimulation mitochondrial Ca2+ monitored by mitochondrial-targeted Ca2+ biosensor mtRCamp1h. Positive 241
Valproic Acid 0.5–2 mM 3min rat inverted submitochondrial vesicles (ISMV) from rat liver isolated mitochondria The rate of the radiolabeled substrate [1-14C]-pyruvate uptake by ISMV was measured in the presence or absence of an inwardly directed proton gradient. inhibitor Positive 279
alpha-Cyano-4-hydroxycinnamate 1mM 3min rat inverted submitochondrial vesicles (ISMV) from rat liver isolated mitochondria The rate of the radiolabeled substrate [1-14C]-pyruvate uptake by ISMV was measured in the presence or absence of an inwardly directed proton gradient. inhibitor Positive 279
alpha-Cyano-4-hydroxycinnamate 0.05mM inhibitor Positive >90% inhibition 280
Alpha-Cyanocinnamate 0.05mM inhibitor Positive >90% inhibition 280
kaempferol 10 μmol/L periodically paced rat ventricular myocytes (VMs) under β-adrenergic stimulation mitochondrial Ca2+ monitored by mitochondrial-targeted Ca2+ biosensor mtRCamp1h. Positive 241
N-ethylmaleimide 20 nmoles/mg protein bovine heart mitochondria and submitochondrial particles. Determination of the energized accumulation of Pi and the binding of ADP; Assay of energized translocation of calcium and Pi affect Positive 228
CGP37157 1 μmol/L Positive 241
Ru360 2 μmol/L Positive 241
MCU-i4 5 μM HeLa cells transfected with mitochondria-targeted aequorin (mtAeq) after cellular stimulation with histamine Highigh-throughput screening assay based on aequorin. decrease Positive 301
MCU-i11 5 μM HeLa cells transfected with mitochondria-targeted aequorin (mtAeq) after cellular stimulation with histamine Highigh-throughput screening assay based on aequorin. decrease Positive 301
MCU-i4 10 μM mouse embryonic fibroblasts (MEFs), MDA-MB-231, and HEK293T cell lines Small-Scale Validation Assay (cytoplasmic- or mitochondria-targeted aequorin (cytAeq and mtAeq, respectively) decrease Positive 301
MCU-i11 10 μM mouse embryonic fibroblasts (MEFs), MDA-MB-231, and HEK293T cell lines Small-Scale Validation Assay (cytoplasmic- or mitochondria-targeted aequorin (cytAeq and mtAeq, respectively) decrease Positive 301
MCU-i4 8.4 μM(Micu1), 18 μM (Micu1-Micu2) Purified recombinant Micu1, Micu2 Purified recombinant Micu1, Micu2, and the dimeric Micu1-Micu2 proteins were immobilized on different channels of a SPR sensor chip surface. decrease Positive IC50 301
MCU-i11 2.9 μM(Micu1), 2.7 μM (Micu1-Micu2) Purified recombinant Micu1, Micu2 Purified recombinant Micu1, Micu2, and the dimeric Micu1-Micu2 proteins were immobilized on different channels of a SPR sensor chip surface. decrease Positive IC50 301
MCU-i4 10 μM Skeletal Muscle Fibers measured mitochondrial Ca2+ uptake in flexor digitorum brevis (FDB) myofibers freshly isolated from adult mice and previously transfected in vivo with the mitochondria-targeted Ca2+ probe 4mt-GCaMP6f decrease Positive 301