SMILES string
O=C(C1=CN=C2C=CC(C)=CC2=C1NC3=CC=C(N(CC)CC)C=C3)OCC
assay
≥98% (HPLC)
form
powder
color
faint green to dark yellow
solubility
DMSO: 2 mg/mL, clear (warmed)
storage temp.
-10 to -25°C
Quality Level
Application
MCU-i4 may be used as a mitochondrial calcium uniporter (MCU) inhibitor to study its effects on cell viability, apoptosis, cytosolic Ca²⁺ levels, mitochondrial Ca²⁺ and membrane potential, glycolytic rate, ATP production, and reactive oxygen species generation in breast cancer cells.
Biochem/physiol Actions
MCU-i4 is a mitochondrial calcium uniporter (MCU) inhibitor that selectively suppresses MCU complex-mediated mitochondrial Ca2+ uptake via direct interaction with MICU1. MCU-i4 (10 μM) effectively inhibits agonist-induced mitochondria Ca2+ uptake in intact cells (agonist = 100 μM histamine when using HeLa, 100 μM ATP when using MEF, MDA-MB-231, and HEK293A), exhibiting no effect in cells expressing MICU1 mutant construct (Q302A, Q306A, L443A) that does not bind MCU-i4 or in MICU1-, but not MICU2-, silenced cells.
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Edmund Cheung So et al.
Oncology research, 33(2), 397-406 (2025-01-27)
Mitochondrial Ca2+ uniporter (MCU) provides a Ca2+ influx pathway from the cytosol into the mitochondrial matrix and a moderate mitochondrial Ca2+ rise stimulates ATP production and cell growth. MCU is highly expressed in various cancer cells including breast cancer cells
Negative modulation of mitochondrial calcium uniporter complex protects neurons against ferroptosis.
Alejandro Marmolejo-Garza et al.
Cell death & disease, 14(11), 772-772 (2023-11-26)
Ferroptosis is an iron- and reactive oxygen species (ROS)-dependent form of regulated cell death, that has been implicated in Alzheimer's disease and Parkinson's disease. Inhibition of cystine/glutamate antiporter could lead to mitochondrial fragmentation, mitochondrial calcium ([Ca2+]m) overload, increased mitochondrial ROS
Tianyang Lan et al.
International journal of molecular sciences, 23(15) (2022-08-13)
Oocyte vitrification has been widely used in the treatment of infertility and fertility preservation. However, vitrification-induced mitochondrial damage adversely affects oocyte development. Several studies have reported that mitochondrial calcium uptake protein 1 (MICU1) regulates the uptake of mitochondrial calcium by
Giulia Di Marco et al.
Cell reports, 30(7), 2321-2331 (2020-02-23)
Mitochondrial Ca2+ uptake depends on the mitochondrial calcium uniporter (MCU) complex, a highly selective channel of the inner mitochondrial membrane (IMM). Here, we screen a library of 44,000 non-proprietary compounds for their ability to modulate mitochondrial Ca2+ uptake. Two of
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