CBR-470-1 is an Inhibitor of the glycolytic enzyme PGK1 that induces Nrf2 activity. PGK1 inhibition results in acculumation of methylglyoxalyl (MGO), a toxic, reactive metabolite removed by other enzymes. The accumulated MGO then irreversibly reacts with Keap1 forming inactive Keap1 dimers, resulting in accumulation of Nrf2.
Inhibitor of the glycolytic enzyme PGK1 inducing Nrf2 activity
Lagerklassenschlüssel
11 - Combustible Solids
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WGK 3
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Not applicable
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The transcription factor NRF2 controls resistance to oxidative insult and is thus a key therapeutic target for treating a number of disease states associated with oxidative stress and aging. We previously reported CBR-470-1, a bis-sulfone which activates NRF2 by increasing
The neurotoxin MPP+ (1-methyl-4-phenylpyridinium ion) disrupts mitochondrial function leading to oxidative stress and neuronal death. Here we examine whether activation of the Keap1-Nrf2 cascade can protect SH-SY5Y neuroblastoma cells from MPP+-induced cytotoxicity. Treatment of SH-SY5Y cells with CBR-470-1, an inhibitor
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