F02110301 | Transport of calcium

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