Rotenone is a mitochondrial electron transport inhibitor, which specifically inhibits NAD-linked substrate oxidation of NADH dehydrogenase with an EC50=10 pmol/mg. It is known that this interference of the electron transport chain occurs from complex I to ubiquinone, similarly to amytal. Studies indicate that Rotenone inhibits mammalian cell proliferation, via suppressing microtubule assembly by binding to tubulin. Rotenone can inhibit the effects of N-methyl-4-phenylpyridinium on mitochondrial swelling and cytochrome c release. Rotenone is an inhibitor of NDUFS.
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