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 |