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Merck
CN

SML4176

MCU-i4

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≥98% (HPLC), powder, mitochondrial calcium uniporter blocker

Synonym(s):

4-[[4-(Diethylamino)phenyl]amino]-6-methyl-3-quinolinecarboxylic acid ethyl ester, Ethyl 4-[[4-(diethylamino)phenyl]amino]-6-methyl-3-quinolinecarboxylate, MCU i4, MCUi4

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About This Item

Empirical Formula (Hill Notation):
C23H27N3O2
CAS Number:
371924-24-2
Molecular Weight:
377.48
MDL number:
MFCD02730422

Key Documents

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Quality Level

100

Assay

≥98% (HPLC)

form

powder

color

faint green to dark yellow

solubility

DMSO: 2 mg/mL, clear (warmed)

storage temp.

-10 to -25°C

SMILES string

O=C(C1=CN=C2C=CC(C)=CC2=C1NC3=CC=C(N(CC)CC)C=C3)OCC

General description

MCU-i4 is a mitochondrial calcium uniporter (MCU) inhibitor that selectivelysuppresses MCU complex-mediated mitochondrial Ca2+ uptake via directinteraction 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.

Application

MCU-i4 may be used asa mitochondrial calcium uniporter (MCU) inhibitor to study its effects on cellviability, apoptosis, cytosolic Ca²⁺levels, mitochondrial Ca²⁺and membrane potential, glycolytic rate, ATP production, and reactive oxygenspecies generation in breast cancer cells.

Biochem/physiol Actions

Selective mitochondrial calcium uniporter (MCU) blocker that inhibits Ca2+-induced mitochondria Ca2+ uptake in whole cells.

Regulatory Information

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Certificates of Analysis (COA)

Lot/Batch Number
0000470081
0000470085
0000470081
0000470085
0000449819

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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
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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