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| 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 | ||
| SB202190 | 10 μM | intact and in permeabilized HeLa cells (MM5 cells expressing mitmutAEQ ) | mitochondrial Ca2+ uptake | increase | Positive | 233 | |||
| 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 | |||
| quercetin | 21 μM | mitochondrial Ca2+ uptake | increase | Positive | EC50 | 234 | |||
| genistein | 37μM | mitochondrial Ca2+ uptake | increase | Positive | EC50 | 234 | |||
| 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 | ||||
| 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 | ||||
| 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 | ||
| CGP37157 | 1 μmol/L | Positive | 241 | ||||||
| Ru360 | 2 μmol/L | Positive | 241 | ||||||
| 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 | ||
| 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 | ||
| neomycin | 400 μM | zebrafish | zebrafish lateral line hair | measrueing cytoplasmic oxidation (HyPer) and mitochondrial Ca2+ uptake (mitoRGECO) | increase | Positive | 315 | ||
| 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 | ||||||
| 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 | ||||||
| Trimetazidine | 10-100µM | rat | isolated cardiac mitochondria | increase | Positive | 274 | |||
| Diclofenac | 50 μmol/L | 2 minutes | rat | liver mitochondria | Assessment of Mitochondrial Ca2+ Efflux; Energized with succinate | decrease | Positive | not mentioned | 6 |
| 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 | |||