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 |