mitochondrial electron transport

Antimalarial agent 14 (NSC-102533) is a bioactive chemical.

Rotenone is a natural plant-derived insecticide that acts as an inhibitor of mitochondrial electron transport chain complex I. It promotes the generation of mitochondrial reactive oxygen species, induces apoptosis, and is commonly used to establish Parkinson's disease models.

Fenpyroximate is an acaricide and insecticide. It blocking the mitochondrial electron transport in complex I.

Ammonium formate (Formic acid ammonium salt) is the simplest carboxylic acid. Formate is an intermediate in normal metabolism. It is responsible for both metabolic acidosis and disrupting mitochondrial electron transport and energy production by inhibiting cytochrome oxidase activity, the terminal electron acceptor of the electron transport chain. Cell death from cytochrome oxidase inhibition by formate is believed to result partly from depletion of ATP, reducing energy concentrations so that essential cell functions cannot be maintained. Furthermore, inhibition of cytochrome oxidase by formate may also cause cell death by increased production of cytotoxic reactive oxygen species (ROS) secondary to the blockade of the electron transport chain.

DX3-234 is a potent oxidative phosphorylation (OXPHOS) inhibitor that acts by inhibiting complex I in the mitochondrial electron transport chain (ETC), leading to intracellular ATP depletion and cell death, and can be used for the treatment of specific cancers dependent on aerobic metabolism, such as pancreatic cancer.

Inz-5 is a small-molecule inhibitor of the mitochondrial electron transport chain that selectively targets mitochondrial complex III (cytochrome bc1 complex), disrupting the process of oxidative phosphorylation and reducing ATP production. It is commonly used in studies of mitochondrial energy metabolism, fungal respiration, and mechanisms related to the electron transport chain. Inz-5 exhibits antifungal activity against a variety of fungal pathogens, demonstrating particularly strong inhibitory effects against Candida species associated with candidiasis; in some studies, its minimum inhibitory concentration (MIC) against Candida albicans reached the sub-micromolar range (approximately 0.5 μM). Furthermore, as an inhibitor of mitochondrial oxidative phosphorylation, Inz-5 is also used to study mechanisms related to tumor cell metabolism and mitochondrial function.

MS-L6 is an inhibitor of the mitochondrial respiratory complex I (ETC-I) with uncoupling properties. This product blocks oxidative phosphorylation (OXPHOS) by inhibiting NADH oxidation and exerting uncoupling effects. MS-L6 reduces mitochondrial membrane potential, inhibits ATP production, and induces mitochondrial dysfunction and apoptosis in tumor cells.

SHO1122147 (Compound 7m) disrupts the mitochondrial electron transport chain, demonstrating mitochondrial uncoupling activity (EC50=3.6 μM). It increases the cellular oxygen consumption rate (OCR=69%) and enhances cellular respiration. Additionally, SHO1122147 is orally active and can be utilized in research related to obesity and metabolic dysfunction-associated steatohepatitis (MASH).

Antitrypanosomal agent 26 (Compound 1) is an allosteric inhibitor of trypanosome alternative oxidase (TAO). It exhibits potent activity against African trypanosomes, such as Trypanosoma brucei, with an IC50 value of 1.3 nM for recombinant TAO. The compound disrupts the mitochondrial electron transport chain of trypanosomes and inhibits glucose-dependent respiration. Antitrypanosomal agent 26 shows potential for research in treating African animal trypanosomiasis, including bovine trypanosomiasis.

(E/Z)-MitoTam (iodide, hydriodide) is a mixture of E/Z isomers of MitoTam iodide, hydriodide. This compound, a derivative of tamoxifen, acts as an electron transport chain (ETC) inhibitor, preventing changes in mitochondrial membrane potential and affecting mitochondrial morphology in aging cells. It is an effective anticancer agent, impeding the formation of respiratory complex I (CI- respiration) and supercomplexes (SCs) in breast cancer cells, and can induce apoptosis (apoptosis).

Antileishmanial agent-35 (Compound 6) is an antileishmanial compound with an IC50 of 0.29 μM against the promastigotes of Leishmania amazonensis. It acts by disrupting the electron transport chain (where ubiquinone plays a role), markedly reducing mitochondrial membrane potential and ATP levels, and increasing reactive oxygen species (ROS) production. Antileishmanial agent-35 is applicable in the study of cutaneous leishmaniasis.

MS6076 is a mitochondrial protease ClpP activator. It specifically triggers the activation of ClpP protease within the mitochondrial matrix, significantly disrupting the mitochondrial electron transport chain (ETC) by accelerating the degradation of unfolded proteins. MS6076 exhibits strong cytotoxicity against various breast cancer cell lines, including triple-negative breast cancer cells (MDA-MB-468, MDA-MB-231), as well as other subtypes (SK-BR-3, MCF-7, BT-474). This compound is applicable in breast cancer research.

Oligomycin is a macrolide antibiotic produced by Streptomyces. Oligomycin is commonly used to study mitochondrial function and cellular energy metabolism and has antifungal and antitumor activities.

SDH-IN-45 is a targeted inhibitor of succinate dehydrogenase (BcSDH) and a mycelial growth inhibitor for Botrytis cinerea, with an IC50 of 5.97 μg/mL. It disrupts the mitochondrial electron transport chain component succinate dehydrogenase through a unique binding mode, thus regulating fungal energy metabolism. SDH-IN-45 induces morphological damage to Botrytis cinerea mycelia, causing structural collapse and shrinkage. This compound shows in vitro fungicidal activity against Botrytis cinerea and can be used in studies related to cucumber gray mold.

GW844520 is a potent and selective inhibitor of the cytochrome bc1 complex of mitochondrial electron transport in P. falciparum.

Vatiquinone, also known as EPI 743, is an orally bioavailable para-benzoquinone being developed for inherited mitochondrial diseases. The mechanism of action of EPI-743 involves augmenting the synthesis of glutathione, optimizing metabolic control, enhanc

Antimycin A2 is a principal constituent and the biologically active component of the antibiotic complex known as Antimycin A, which exerts its inhibitory activity against a range of fungal species and certain insects through a primary mechanism of action involving the potent inhibition of cellular respiration by blocking the reoxidation of cytochrome b within the mitochondrial electron transport chain.

Antimycin A4 is an active component of the antimycin A antibiotic complex that is more polar than antimycin A1 , antimycin A2 , and antimycin A3 . Antimycin A4 inhibits ATP-citrate lyase with a Ki value of 64.8 μM. The antimycin A complex is a mixture of antimycins A1, A2, A3, and A4 that demonstrates antifungal, insecticidal, nematocidal, and piscicidal properties. It blocks mitochondrial respiration and can deplete cellular levels of ATP via inhibition of complex III of the mitochondrial electron transport chain (ETC). Antimycin A prevents the transfer of electrons between the b-cytochromes and ubiquinone at the Q(inner) site of complex III. This results in the stabilization of the ubisemiquinone radical at the Q(outer) site of complex III, leading to increased production of superoxide. Antimycin A is widely used in research to shunt electron flow through the ETC to study the chemical details of oxygen respiration. Additionally, antimycin A has been shown to inhibit Bcl-2 and Bcl-xL proteins, inducing apoptosis.

Piericidin B is a bacterial metabolite that has been found inS. mobaraensisand has insecticidal and antimicrobial activities.1,2,3It inhibits NADH oxidase activity in isolated bovine heart mitochondria and inhibits respiration in isolated rat liver mitochondria and isolated cockroach (P. americana) muscle mitochondria.2,3Topical application of piericidin B (4 μg/insect) induces mortality in 87.5% of houseflies (M. domestica).1It induces 93.3, 100, and 100% mortality in rice stem borer (C. simples), silkworm (B. mori), and green caterpillar (P. rapae) larvae, respectively, when applied at respective concentrations of 60, 4.8, and 96 μg/larva. Piericidin B is active against the fungiT. asteroides,T. rubrum,M. gypseum, andC. neoforms(MICs = 20, 10, 20, and 2 μg/ml, respectively), as well as the bacteriaM. luteusandP. vulgaris(MICs = 50 and 100 μg/ml, respectively). 1.Takahashi, N., Suzuki, A., Kimura, Y., et al.Isolation, structure and physiological activities of piericidin B, natural Insecticide produced by a StreptomycesAgr. Biol. Chem.32(9)1115-1122(1968) 2.Jeng, M., Hall, C., Crane, F.L., et al.Inhibition of mitochondrial electron transport by piericidin A and related compoundsBiochemistry7(4)1311-1322(1968) 3.Mitsui, T., Fukami, J.-I., Fukunaga, K., et al.Studies on piericidin. I. : Effects of piericidin A and B on mitochondrial electron transport in insect muscle comparing with rotenoneSci. Insect Control34(3)126-134(1969)

Pyridaben is a METI acaricide that inhibits mitochondrial electron transport at complex I (METI; Ki = 0.36 nmol/mg protein in rat brain mitochondria).

IACS-010759 is an orally bioavailable inhibitor of complex I of oxidative phosphorylation of the mitochondrial electron transport chain.

Compound 5C, referred to as Pkm2-in-4, is a selective PKM2 inhibitor (IC50 = 0.35 µM) that modulates pyruvate-dependent respiration and promotes mitochondrial H2O2 production rate and electron transport system coupling [1].

HQNO is a natural product isolated from P. aeruginosa,and is a potent inhibitor of electron transport chain(Kd of 64 nM for complex III). It also is a potent mitochondrial NDH-2 inhibitorin many species.

2,6-Dichlorophenolindophenol sodium hydrate (DCPIP) is a blue-colored redox dye commonly employed as an indicator for the determination of vitamin C (ascorbic acid) content. DCPIP undergoes a reduction reaction with vitamin C, during which it changes from a blue-colored oxidized state to a colorless reduced form, providing a simple visual assay for ascorbic acid. Beyond vitamin C determination, DCPIP is utilized in diverse research applications, including the evaluation of enzymatic activity of gold nanoparticles, the development of UVB-specific dosimeters, its role as an electron acceptor in histochemical staining techniques, and investigations of mitochondrial electron transport chain activity.