Database
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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 | |||
| Trimetazidine | 10-100µM | rat | isolated cardiac mitochondria | increase | Positive | 274 | |||
| 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 | |||