Elesclomol

Elesclomol is an inducer of apoptosis and a copper ionophore.¹ It induces the production of reactive oxygen species (ROS) and increases oxidative stress response gene expression in Ramos (RA 1) B cell lymphoma cells when used at a concentration of 500 nM. Elesclomol (100 nM) disrupts the mitochondrial membrane potential and induces apoptosis in Ramos (RA 1) cells. It induces ferroptosis by selectively transporting copper into the inner mitochondrial membrane in MDA-MB-435 breast cancer cells.² Elesclomol preloaded with copper (3.6 mg/kg) increases brain mitochondrial copper and mitochondrial complex IV, also known as cytochrome c oxidase, levels, as well as increases survival time, body weight, and brain weight and prevents changes in neuronal morphology in a mottled-brindled mouse model of Menkes disease, a fatal, X-linked condition characterized by copper-transporting ATPase (ATP7A) gene mutation, which produces altered catecholamine and copper levels, hypopigmentation, and severe neurodegeneration.³

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1. Kirshner, J.R., He, S., Balasubramanyam, V., et al. Elesclomol induces cancer cell apoptosis through oxidative stress. Mol. Cancer Ther. 7(8), 2319-2327 (2008).

2. Nagai, M., Vo, N.H., Shin Ogawa, L., et al. The oncology drug elesclomol selectively transports copper to the mitochondria to induce oxidative stress in cancer cells. Free Radic. Biol. Med. 52(10), 2142-2150 (2012).

3. Guthrie, L.M., Soma, S., Yuan, S., et al. Elesclomol alleviates Menkes pathology and mortality by escorting Cu to cuproenzymes in mice. Science 368(6491), 620-625 (2020).