mitochondrial metabolism

Imeglimin hydrochloride (EMD 387008 hydrochloride） is an oral hypoglycemic agent. Imeglimin improves insulin sensitivity, inhibits the production of reactive oxygen species, increases mitochondrial DNA, and improves mitochondrial function.

BRD6897 is a mitochondrial content inducer that increases the cellular content of mitochondria and induces a significant increase in the electron density of existing mitochondria.

Nerol (Neryl alcohol) is a monoterpene found in many essential oils, such as lemon balm and hop.Nerol can lessened the severity of ouabain-triggered arrhythmias in mammalian heart.

Tricarballylic acid (Carballylic acid) is an inhibitor of aconitase.

L-Histidine (L-(-)-Histidine) is a semi-essential amino acid (children should obtain it from food) needed in humans for growth and tissue repair, L-Histidine is important for maintenance of myelin sheaths that protect nerve cells and is metabolized to the neurotransmitter histamine. Histamines play many roles in immunity, gastric secretion, and sexual functions. L-Histidine is also required for blood cell manufacture and protects tissues against damage caused by radiation and heavy metals.

Glibenclamide (Glyburide) is an antidiabetic sulfonylurea derivative with actions similar to those of chlorpropamide.

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

Tempo (2,2,6,6-Tetramethylpiperidinooxy) has a wide range of applications including use as a free radical scavenger, a reagent in organic synthesis and as a structural probe in electron spin resonance spectroscopy.

D-Histidine is an enantiomer of L-histidine. L-Histidine is an inhibitor of mitochondrial glutamine transport and also an essential amino acid for infants.

Lipoic acid (R-(+)-Thioctic acid) is an organosulfur compound derived from octanoic acid. It is made in animals normally, and is essential for aerobic metabolism.

Idebenone (CV-2619) is a synthetic analogue of ubiquinone (Coenzyme Q10), a vital cell antioxidant and essential component of the Electron Transport Chain (ETC).

Rotenone (Rotocide) is a natural product and a botanical insecticide. Rotenone is a mitochondrial electron transport complex I inhibitor that promotes the production of reactive oxygen species in mitochondria and induces apoptosis.

Thiabendazole (2-(4-Thiazolyl)benzimidazole) is a benzimidazole derivative with anthelminthic property.

Daidzin (Daidzoside) is an isoflavone isolated from soya bean with anti-oxidant, anti-carcinogenic, and anti-atherosclerotic activities.

Imeglimin (EMD 387008) is an orally available antidiabetic compound that enhances mitochondrial function, enhances insulin secretion, promotes β-cell proliferation and improves pancreatic β-cell survival in mice.

(-)-Epigallocatechin Gallate (EGCG) is a phenolic antioxidant polyphenol flavonoid found in plants such as green and black tea, which inhibits telomerase and DNA methyltransferase, blocks the activation of EGF receptors and HER-2 receptors, inhibits cellular oxidation, and prevents free radical damage to cells.

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

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)

α-Lipoic Acid (Alphalipoic acid) inhibits NF-κB-dependent HIV-1 LTR activation. α-Lipoic Acid induces endoplasmic reticulum (ER) stress-mediated apoptosis in hepatoma cells.α-Lipoic Acid is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes.

TT01001 (Ethyl 4-(3-(3,5-dichlorophenyl)thioureido)piperidine-1-carboxylate) is a selective agonist of mitoNEET and reduces oxidative stress injury and neuronal apoptosis by improving mitochondrial dysfunction. TT01001 can be used in studies about the treatment of type II diabetes.

4-methyl-6-phenyl-2H-pyranone is derived from Scutellaria baicalensis Georgi and improves mitochondrial functionality to protect astrocytes against hydrogen peroxide-induced toxicity.

ND-011992 is a reversible and selective quinazoline inhibitor targeting quinone reductases and quinol oxidases.ND-011992 inhibits E. coli BL21*Δcyo respiratory complex I. ND-011992 inhibits bo3 oxidase, bd-I oxidases and bd-II oxidases, ND-011992 inhibits E. coli BL21*Δcyo respiratory complex I, bo3 oxidase, bd-I oxidases, and bd-II oxidases with IC50s of 0.12, 2.47, 0.63, and 1.3 μM, respectively.ND-011992 can be used in the study of tuberculosis.

VK-28 is a brain permeable iron chelator with neuroprotection. VK-28 inhibits basal as well as iron-induced mitochondrial lipid peroxidation.

McN3716 is a carnitine palmitoyltransferase I (CPT-1) inhibitor used for researching metabolic diseases.

(S)-Coriolic acid (13(S)-HODE) is an important intracellular signaling agent generated by the reaction of linoleic acid with plant and mammalian lipoxygenases. It is involved in cell proliferation and differentiation in various biological systems and inhibits the adhesion of tumor cells to the vascular endothelium, while down-regulating IRGpIIb IIIa receptor expression at around 1 μM. Additionally, (S)-Coriolic acid is a metabolite of 15-lipoxygenase (15-LOX) and often acts as an endogenous ligand to activate PPARγ. It induces mitochondrial dysfunction and airway epithelial damage.

Schaftoside (APIGENIN-6-GLUCOSIDE-8-ARABINOSIDE) has antioxidant and anticancer activity.

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

FCCP (Trifluoromethoxy carbonylcyanide phenylhydrazone) is an oxidative phosphorylation (OXPHOS) inhibitor and mitochondrial proton carrier uncoupler. FCCP is often used as an apoptosis inducer.

Mito-TEMPO, a mitochondria-targeted superoxide dismutase mimetic, scavenges superoxide and alkyl radicals, preventing mitochondrial oxidation, necrosis, and apoptosis.

CCCP (Carbonyl Cyanide m-Chlorophenylhydrazone) is an oxidative phosphorylation (OXPHOS) inhibitor and mitochondrial proton carrier uncoupler. CCCP inhibits the activation of STING and its downstream signaling molecules TBK1 and IRF3.

MSDC 0160 (CAY10415) is a prototype mTOT-modulating insulin sensitizer being used in trials studying the treatment of Type 2 Diabetes and Alzheimer's Disease.

THP104c is an inhibitor of mitochondrial fission.

GW604714X (2,4-Thiazolidinedione, 5-[[5-[6-(4-acetyl-1-piperazinyl)-3-nitro-2-pyridinyl]-2-fluorophenyl]methylene]-) were found to be potent inhibitors of mitochondrial respiration supported by pyruvate

L-2-Hydroxyglutaric acid disodium ((S)-2-Hydroxyglutaric acid disodium) is an epigenetic modifier and putative oncometabolite in renal cancer. L-2-Hydroxyglutaric acid inhibits mitochondrial creatine kinase (Mi-CK) activity(Km and Ki of 2.52 mM and 11.13 mM, respectively).

CCI-006, a selective inhibitor and chemosensitizer for MLL-rearranged leukemia cells, disrupts mitochondrial respiration. This action leads to irreversible mitochondrial depolarization and triggers a pro-apoptotic unfolded protein response in specific MLL-r leukemia cells.

BI-6C9 is an inhibitor of tBid (Kd = 20 µM).BI-6c9 prevented MOMP and mitochondrial fission, and protected the cells from cell death.

VLX600 is an iron-chelating oxidative phosphorylation (OXPHOS) inhibitor, is a cell-permeable anticancer agent. It acts by reducing mitochondrial oxidative phosphorylation in tumor cells.

Mito-LND (Mito-Loidamine) is an orally active and mitochondria-targeted inhibitor of oxidative phosphorylation.

Azemiglitazone (MSDC 0602) is an insulin sensitizer potentially for the treatment of diabetes.

Olesoxime (TRO 19622) (TRO19622), A Mitochondrial-Targeted Neuroprotective Compound,is an experimental neuroprotective drug.

Adjudin (AF-2364) is a small molecule compound known to possess antispermatogenic function, attenuates microglia activation by suppression of the NF-κB pathway.

FGIN-1-43 is a potent and specific ligand for the mitochondrial DBI receptor.

Mitochondrial fusion promoter M1, a modulator of mitochondrial dynamics, enhances mitochondrial function and cellular respiration, and has shown efficacy in reducing brain and cardiac damage in rats suffering from cardiac ischemia/reperfusion injury.

Speract, a peptide from sea urchin eggs, regulates sperm motility and stimulates sperm mitochondrial metabolism.

α-Lipoic Acid (DL-α-Lipoic acid) an octanoic acid bridged with two sulfurs so that it is sometimes also called a pentanoic acid in some naming schemes. It is biosynthesized by cleavage of LINOLEIC ACID and is a coenzyme of oxoglutarate dehydrogenase (KETOGLUTARATE DEHYDROGENASE COMPLEX). It is used in DIETARY SUPPLEMENTS.

CTPI-2 is an inhibitor of mitochondrial citrate carrier SLC25A1 with(KD : 3.5 μM). CTPI-2 inhibits glycolysis, PPARγ, and its downstream target the glucose transporter GLUT4. CTPI-2 exhibits anti-tumor activity.CTPI-2 halts salient alterations of NASH reverting steatosis, preventing the evolution to steatohepatitis, reducing inflammatory macrophage infiltration in the liver and adipose tissue, and starkly mitigating obesity induced by a high-fat diet.

Glutamate dehydrogenase NAD(P) (GLDH), a mitochondrial enzyme found in hepatocytes, renal tissue, brain, muscle, and intestinal cells, catalyzes the reversible oxidative deamination of glutamate to α-ketoglutarate (α-KG), playing a critical role in the urea cycle [1], and is frequently utilized in biochemical research.

ER-000444793 is a potent mitochondrial permeability transition pore (mPTP) opening inhibitor and it also inhibits mPTP (IC50: 2.8 μM).