mitochondrial complex

Lonidamine (Diclondazolic Acid) is an indazole carboxylic acid derivative, principally inhibiting aerobic glycolytic activity, by its effect on mitochondrially-bound hexokinase (HK).

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.

AMPK activator 4 is a potent and selective AMPK activator that does not inhibit mitochondrial complex I. It selectively activates AMPK in muscle tissue, dose-dependently improves glucose tolerance in normal mice, significantly reduces fasting glucose levels, and improves insulin resistance in db db diabetic mice. [AMPK activator 4 has hypoglycemic effects.]

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

Boscalid is a broad-spectrum carboxamide fungicide that inhibits fungal respiration by binding to the ubiquinone site of mitochondrial complex II succinate dehydrogenase.1It suppresses mycelial growth ofS. minorby 87 to 100% and ofS. sclerotiorumby 77 to 100% when used at a concentration of 1 μg ml.2In field studies, boscalid applied at 5.6 μg cm2provides 55.5 and 30.4% disease control for lettuce drop caused byS. minorandS. sclerotiorum, respectively. It decreases cell viability of mouse primary cortical neurons following long-term exposure but is not cytotoxic (LC50= >100 μM for acute and continuous exposure). Formulations containing boscalid have been used in agriculture to prevent fungal growth on crops. 1.Wang, Y., Duan, Y., Wang, J., et al.A new point mutation in the iron-sulfur subunit of succinate dehydrogenase confers resistance to boscalid in Sclerotinia sclerotiorumMol. Plant Pathol.16(7)653-661(2015) 2.Matheron, M.E., and Porchas, M.Activity of boscalid, fenhexamid, fluazinam, fludioxonil, and vinclozolin on growth of Sclerotinia minor and S. sclerotiorum and development of lettuce dropPlant Dis.88(6)665-668(2004)

Tebufenpyrad (Comanche) (mitochondrial complex-1 inhibitors) is an agro-chemically important acaricide that functions like the known mitochondrial toxicant rotenone.

MPP+ iodide, the metabolite of a neurotoxin MPTP, causes symptom of Parkinson's disease (PD) in animal models by selectively destroying dopaminergic neurons in substantia nigra. MPP+ induces dopamine transporter (DAT) externalization in dopaminergic (DA) neurons, but internalization of serotonin transporter (SERT) in serotonergic (5-HT) neurons. MPP+ induces autophagic cell death in SH-SY5Y cells.

Pyraclostrobin is one of the most heavily used fungicides that inhibits mitochondrial complex III of fungal and mammalian cells.

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.

DX3-235 is an oxidative phosphorylation (OXPHOS) inhibitor with nanomolar-level inhibitory effects on mitochondrial complex I function in galactose-containing media, resulting in reduced ATP production, leading to impaired cellular energy metabolism and cancer cytotoxicity.

ATP synthase inhibitor 1 is an inhibitor of the c subunit of the F1 FO-ATP synthase complex. It inhibits mitochondrial permeability transition pore (mPTP) opening and does not affect ATP levels.

Annonacin is an acetogenin that promotes cytotoxicity by inhibiting the mitochondrial complex and acts as the active agent in Graviola leaf extract, inhibiting sodium potassium (NKA) and sarcoplasmic reticulum (SERCA) ATPase pumps[1].

Aumitin, a diaminopyrimidine-based autophagy inhibitor, dose-dependently inhibits starvation- and rapamycin-induced autophagy with IC50s of 0.12 μM and 0.24 μM, respectively [1], and also inhibits mitochondrial respiration by targeting complex I.

Bcl-2-IN-22 (compound 1), a gold (I) NHC complex, exhibits anticancer activity. It induces cell death (apoptosis) via the mitochondrial pathway with an IC50 value of 0.014 μM. Additionally, Bcl-2-IN-22 targets members of the BCL-2 family, promoting apoptosis and sensitization in multidrug-resistant leukemia cells overexpressing BCL-2.

Sitamaquine hydrochloride (WR 6026) is an orally active 8-aminoquinoline analog with antileishmanial activity. This compound inhibits mitochondrial complex II (succinate dehydrogenase) and is characterized by its lipophilic weak base properties. It rapidly accumulates in the acidic compartments of Leishmania parasites, predominantly localizing within the acidocalcisomes.

Dopaminechrome (DACHR) is an oxidation product of dopamine that promotes the generation of H2O2 at mitochondrial complex I in the brain in a concentration- and respiration-dependent manner. It possesses neurotoxic properties and can be utilized in Parkinson's disease research.

ROS-ERS inducer 2 (Complex 3f) promotes the generation of intracellular ROS, affects mitochondrial function, facilitates the release of damage-associated molecular patterns (DAMPs), induces immunogenic cell death (ICD), and activates endoplasmic reticulum stress (ERS). It plays a significant role in anti-hepatocellular carcinoma research.

SDH-IN-25 is an SDH inhibitor with an IC50 of 4.82 mg/L, demonstrating broad-spectrum and potent antifungal activity. By binding to SDH amino acid residues (TRP173, TYR58, and ARG43), it mimics the action mode of the commercial fungicide flutolanil. SDH-IN-25 induces changes in hyphal morphology, disrupts respiratory metabolism by binding to complex II, generates reactive oxygen species (ROS), and affects mitochondrial membrane potential (MMP) in hyphae. This compound is utilized in agricultural disease control research.

Mitochondrial-IN (C458) is a potent inhibitor of mitochondrial complex I. It offers significant protection against Aβ toxicity, exhibits favorable pharmacokinetic properties, and has minimal off-target effects.

AG311 is an inhibitor of complex I and hypoxia-induced HIF-1α stabilization. In vitro, AG311 induces rapid necrosis in numerous cancer cell lines. Within minutes, exposure to AG311 also results in mitochondrial depolarization, superoxide production, and i

Bim-BLK-A efficiently blocks Bim-induced apoptosis after Bax is activated on the mitochondria. The cellular target of Bim-BLK-A was identified to be the succinate dehydrogenase subunit B (SDHB) protein of complex II of the mitochondrial electron transfer

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

S1QEL1.1 (S1QEL) is a mitochondrial respiratory complex I site IQ electron leak suppressor that inhibits O2-induced ROS production and prevents O2-induced DA closure, and can be used in the study of cardiovascular diseases.

Ganglioside GD3 is synthesized by the addition of two sialic acid residues to lactosylceramide and can serve as a precursor to the formation of more complex gangliosides by the action of glycosyl- and sialyltransferases. It induces apoptosis in HuT-78 cutaneous T cell lymphoma cells in a concentration-dependent manner and disrupts the mitochondrial membrane potential when used at a concentration of 200 μM. Expression of ganglioside GD3 in GD3-negative SK-MEL-28-N1 malignant melanoma cells increases both cell proliferation and invasion in vitro. Ganglioside GD3-deficient adult mice exhibit progressive loss of the neural stem cell (NSC) pool and impaired neurogenesis. Ganglioside GD3 mixture contains ganglioside GD3 molecular species with C18:1 and C20:1 sphingoid backbones.