3-Bromopyruvic acid is a hexokinase inhibitor that has been shown to abolish ATP production and cause severe depletion of cellular ATP. It displays potent cytotoxic activity against cancer cells with mitochondrial respiratory defects and cells in a hypoxic environment.

A plant and fungal toxin, 3-nitropropionic acid acts as an irreversible inactivator of succinate dehydrogenase. Selectively inhibits succinic dehydrogenase complex (Complex II) in the mitochondrial electron transport chain. Also shown to cause brain lesions similar to those of Huntington′s disease.

3,3′,5’-Triiodo-L-thyronine (Reverse T3), is a thyroid hormone generated by the deiodination of the prohormone thyroxine. It is about 1,000-fold less active at the thyroid hormone receptors TRα and TRβ than 3,3′,5-triiodo-L-thyronine.  Reverse T3 positively regulates the hepatic FGF21 expression and stimulates the metabolic breakdown of glucose, fats, and proteins by enhancing the levels of numerous […]

A Roscovitine-related purine derivative that selectively and potently increases the production of extracellular Aβ42 and decreases the production of extracellular Aβ38 in cultured cells.

Roscovitine-related purine with no activity on CDKS. Selectively and potently increases the production of extracellular Aβ42 and decreases the production of extracellular Aβ38 in cultured cells.

A non-selective ion channel blocker with broad fungicidal activity. Amiodarone induces an immediate influx of Ca2+ in Saccharomyces cerevisiae, followed by mitochondrial fragmentation and cell death. Also acts as an autophagy inducer.

Antimycin A, isolated from Streptomyces sp., is a mixture of Antimycins A1, A2, A3 and A4. Inhibits mitochondrial electron transport, specifically between cytochromes b and c1. Induces apoptosis, which is not prevented by the presence of Bcl-2.

Artesunate is a semisynthetic derivative of artemisinin. It acts on the electron transport chain, generates local reactive oxygen species, and causes the depolarization of the mitochondrial membrane. It inhibits TNFα-induced production of proinflammatory cytokines via inhibition of NF-κB and PI3 kinase/Akt signal pathway in human rheumatoid arthritis fibroblast-like synoviocytes.

AT-101 is the R-(-) enantiomer of Gossypol that acts as an inhibitor of the antiapoptotic Bcl proteins (Bcl-2, Bcl-XL, Bcl-W, and Mcl-1) and an inducer of the pro-apoptotic proteins noxa and puma. It induces apoptosis in drug-resistant multiple myeloma cell lines. Apoptosis is activated by the mitochondrial pathway.

Atovaquone is a broad-spectrum antiprotozoal agent that is active against Plasmodium, Toxoplasma, and Babesia, among other protozoa. It inhibits complex III activity on dihydroorotate in isolated P. falciparum and P. yoelii mitochondria more potently than in rat liver mitochondria and depolarizes the mitochondrial membrane in P. yoelii-infected mouse erythrocytes. Atovaquone also inhibits transport mediated by […]

Synthetic. Originally isolated from Penicillium sp. strain. An antibiotic and antifungal agent. Potent and specific mitochondrial complex II (succinate-ubiquinone oxidoreductase) inhibitor and mitochondrial ATP-sensitive potassium (mK(ATP)) channel activator. Modulates mitochondrial ROS generation during cardioprotection.

Atractyloside is an extremely toxic glycoside isolated from thistles. It blocks mitochondrial ATP synthesis by inhibiting ADP/ATP translocases, which are responsible for the exchange of adenine di- and triphosphates across the inner mitochondrial membrane.

An anti-arthritic drug that inhibits various leukocyte activation pathways at multiple sites. Inhibits release of inflammatory mediators from human basophils, pulmonary mast cells, and macrophages. Also inhibits human neutrophil 5-lipoxygenase. Inhibits IκB kinase (IKK) by modifying Cys179 of the IKKß subunit. Efficient inducer of mitochondrial membrane permeability transition via the inhibition of mitochondrial thioredoxin reductase […]

Acts as an inhibitor of protein tyrosine phosphatase 1B (PTB1B (IC₅₀ = 20.8±1.9 µM). Antioxidant and an inhibitor of mitochondrial lipid peroxidation. Also inhibits inducible nitric oxide synthase (iNOS; NOS II) expression. DNA polymerase inhibitor. Shows antimicrobial and cytotoxic activity.

BAY 87-2243 is a highly potent and selective inhibitor of hypoxia-induced gene activation. It inhibits HIF-1α and HIF-2α protein accumulation under hypoxic conditions in non-small cell lung cancer (NSCLC) cell line H460 but had no effect on HIF-1α protein levels induced by the hypoxia mimetics desferrioxamine or cobalt chloride. In addition, BAY 87-2243 is also […]

Cell-permeable. A small-molecule pan–Bcl-2 antagonist that mimics BH3-only proteins by binding to multiple antiapoptotic Bcl-2 members. GX15-070 has been shown to overcome Bcl-2–, Bcl-xl–, Bcl-w–, and Mcl-1–mediated resistance to Bax or Bak. It potently interferes with the direct interaction between Mcl-1 and Bak in the intact outer mitochondrial membrane and inhibits the association between Mcl-1 […]

A neuroprotective agent and mitochondrial gene regulator. Also acts as a ROS (reactive oxygen species) scavenger and apoptosis inhibitor. In addition, Bilabolide activates the phosphatidylinositol 3-kinase (PI3K) dependent pathway.

Brusatol is a quassinoid isolated from the Brucea javanica plant that has recently been shown to inhibit Nrf2 signaling, reduce tumor burden, and ameliorate chemoresistance in both in vitro and in vivo cancer models. Brusatol also inhibits c-Myc expression and showed that overexpression of c-Myc prevented brusatol-induced degradation of HIF-1α and cancer cell death by […]

Carboxyatractyloside is a plant-derived natural heteroglucoside that prevents mitochondrial ATP synthesis by inhibiting ADP/ATP translocases, which are responsible for the exchange of adenine di- and triphosphates across the inner mitochondrial membrane.

Cardiolipin probe is an excellent fluorescent probe for the detection and quantification of cardiolipin (CL). This probe displays improved sensitivity and excellent selectivity for CL over other major mitochondrial membrane lipids.

Cell-permeable. A selective protein kinase C (PKC) inhibitor. Chelerythrine is at least 100-fold more selective for PKCs than for other kinases. It induces apoptotic cell death in polymorphonuclear leukocytes through activation of caspase-3.

A naturally occurring quinone found throughout the body in cell membranes, primarily in mitochondrial membranes. It is an endogenous cellular antioxidant and an essential component of the electron transfer chain. CoQ10 takes part in aerobic cellular respiration and generation of energy in the form of ATP.

CPI-613 is a non-redox active lipoate derivative that acts as a selective inhibitor mitochondrial enzymes pyruvate dehydrogenase (PDH) and α-ketoglutarate dehydrogenase. In vitro, CPI-613 dose-dependently and efficiently kills H460 human lung cancer cells and Saos-2 human sarcoma cells. In vitro, CPI-613 treatment potently disrupts H460 cancer cell mitochondrial metabolism including inhibition of PDH complex activity. CPI-613 treatment […]

Cytochrome c is an electron-carrying mitochondrial protein. It is a small heme protein containing a single polypeptide chain and a single heme group, which is covalently attached to the polypeptide. The ready fluctuation of cytochrome c within the cell between ferrous and ferric states makes it an efficient biological electron-transporter and it plays a vital […]

Potent anti-cancer agent whose potential target site may be mitochondrial cytochrome c oxidase. Inhibits RNA and DNA synthesis. Also inhibits eukaryotic topoisomerase I & II. Induces DNA single-strand breaks and apoptosis in HeLaS3 tumor cells.

A synthetic substrate of cytochrome and mitochondrial permeability transition pore (MPTP) inhibitor.

Destruxin B is a cyclic hexadepsipeptide metabolite from the fungus Metarhizium anisopliae. It shows insecticidal and anti-cancer properties. It induces a concentration-dependent antiproliferative effect on lung adenocarcinoma A549 cells, with an IC₅₀ value of 4.9 μM. It induces apoptosis in the human non-small cell lung cancer cells A549 and H1299 cells via a Bcl-2 family-dependent mitochondrial […]

Dexpramipexole dihydrochloride is a neuroprotectant that may slow the progression of ALS by keeping the power on in deteriorating motor nerves. Dexpramipexole maintains mitochondrial function in people with ALS by increasing the efficiency of ATP production.

Cell-permeable. A pan-specific ubiquitin isopeptidase inhibitor. NSC-632839 does not affect proteasome proteolytic activity. Induces apoptosis via a Bcl-2-dependent but apoptosome-independent mitochondrial pathway.

Cell-permeable. A reversible, noncompetitive inhibitor of dynamin that interferes in vitro with the GTPase activity of dynamin1, dynamin2, and Drp1, the mitochondrial dynamin, but not of other small GTPases.

Erastin is a selective antitumor agent that displays greater lethality in human tumor cells harboring mutations in the oncogenes HRAS, KRAS, or BRAF. It binds to mitochondrial voltage-dependent anion channels (VDAC) proteins, more specifically on VDAC2, and alters its gating. Erastin rapidly induces oxidative, non-apoptotic cell death in several human tumors harboring activating mutations in the RAS-RAF-MEK signaling.

F16 is a cell-permeable, fluorogenic, cationic, lipophilic mitochondrial toxin. Induces apoptosis as well as necrosis in tumor cells. Displays antitumor properties.

FCCP is a potent and reversible inhibitor of mitochondrial oxidative phosphorylation. It depolarizes mitochondrial membrane potential and induces apoptosis.

Fucoxanthin is a natural pigment found in microalgae, especially diatoms and Chrysophyta. Recently, it has been shown to have antioxidant, anti-inflammatory, anti-tumor, and anti-obesity activity in humans. Fucoxanthin increases the amount of mitochondrial uncoupling protein 1 (UCP1), a fatty acid-stimulated protein involved in respiration and thermogenesis in WAT of mice and rats.

GDC-0917 (CUDC-427) is a second mitochondrial activator of caspases (Smac) mimetic, a small molecule inhibitor, that mimics Smac, an endogenous antagonist of IAP proteins. GDC-0917 binds to the Smac binding groove on IAPs, including the direct caspase inhibitor X chromosome-linked IAP (XIAP) and the cellular IAPs 1 and 2.

GW-7647 is a potent, selective agonist of human and murine PPARα. It activates human PPARα, PPARγ, and PPARδ with EC₅₀ values of 0.006, 1.1, and 6.2 µM, respectively, in a GAL4-PPAR binding assay. Similar EC₅₀ values of 0.001, 1.3, and 2.9 were observed with the murine receptors. Modulates oleate metabolism and mitochondrial enzyme gene expression in mature myotubules in vitro. […]

IACS-010759 is a potent and selective Oxidative Phosphorylation Inhibitor (IC₅₀ < 10 nM) with potential antineoplastic activity. IACS-010759 robustly inhibits proliferation and induces apoptosis in models of brain cancer and acute myeloid leukemia (AML) reliant on OXPHOS, likely owing to a combination of energy depletion and reduced aspartate production that leads to impaired nucleotide biosynthesis.

A benzoquinone analog of coenzyme Q10 that serves as a cofactor in the electron transport chain in mitochondria. Idebenone acts as a potent lipid antioxidant that prevents the generation of free radicals. Idebenone targets mitochondria preserve mitochondrial function and confers cytoprotection.

Imisopasem manganese is a manganese-based non-peptidyl mimetic of the human mitochondrial manganese superoxide dismutase (MnSOD), with potential antioxidant and chemo/radioprotective activities. Imisopasem manganese mimics the activity of MnSOD and scavenges reactive oxygen species (ROS), such as superoxide anion, which prevents oxygen free radical damage to macromolecules such as DNA.

A cell-permeable indole derivative that acts as an antioxidant and mitochondrial metabolism modifier. IPAM binds to the rate-limiting component of oxidative phosphorylation in complex I of the respiratory chain and acts as a stabilizer of energy metabolism, thereby reducing the production of reactive oxygen species.

JC-1 is a mitochondrial dye that stains mitochondria in Living cells in a membrane potential-dependent fashion. JC-1 monomer is in equilibrium with so-called J-aggregates, which are favored at higher mitochondrial membrane potential. The monomer JC-1 has green fluorescence (lem = 527 nm), while the J-aggregates have red fluorescence (lem = 590 nm). Therefore, it has […]

A naturally occurring polyphenol antioxidant that displays a wide range of pharmacological activities, including antioxidant, anti-inflammatory, antimicrobial, anticancer, cardioprotective, neuroprotective, antidiabetic, anti-osteoporotic, estrogenic/antiestrogenic, anxiolytic, analgesic, and antiallergic activities. It reduces cell cycle progression in HT-29 cells. Kaempferol increases chromatin condensation, DNA fragmentation, and the number of early apoptotic cells in HT-29 cells in a dose-dependent […]

L-DON is a glutamine antagonist produced naturally by Streptomyces; it inhibits several glutamine-dependent enzyme pathways as well as acts as an inhibitor of the mitochondrial enzyme, glutaminase (GLS), the primary producer of neuronal glutamate.

Lanatoside C is a cardiac glycoside, used in the treatment of congestive heart failure and cardiac arrhythmia. Lanatoside C suppresses colorectal cancer cell growth by inducing mitochondrial dysfunction and increased radiation sensitivity by impairing DNA damage repair. Also activates IL-1β through activation of the inflammasome.

Lonidamine is a derivative of indazole-3-carboxylic acid that inhibits glycolysis by the inactivation of hexokinase, an enzyme that catalyzes glucose as the first step in glycolysis. Also blocks CFTR Cl- channels in vitro. Acts as an anticancer and antispermatogenic agent in vitro and in vivo.

Cell-permeable. A selective inhibitor of Dnm1 GTPase (IC₅₀ =1-10 µM). Inhibits mitochondrial outer membrane permeabilization. Inhibits mitochondrial division and apoptosis.

Mito-TEMPO is a mitochondria-targeted superoxide dismutase mimetic that possesses superoxide and alkyl radical scavenging properties. Mitochondrial targeting of superoxide scavenging using mito-TEMPO has been examined for potential therapeutic benefit to a variety of mitochondrondrial dysfunctions arising from excessive reactive oxygen species.

MOTS-c is a mitochondria-derived peptide (MDP) that promotes biosynthesis of the endogenous AMP analog AICAR and consequently AMP-activated protein kinase (AMPK). Induces cellular and systemic glucose uptake and improves insulin sensitivity. Shown to prevent diet-induced obesity (DIO) in mice. Potential anti-obesity and anti-aging compounds.

MTT is a tetrazolium salt used for determining cell viability. MTT produces a yellowish solution that is converted to dark blue, water-insoluble MTT formazan by mitochondrial dehydrogenases of living cells. The formazan is then solubilized and its concentration is determined by optical density.

NS-1619 is a calcium-dependent activator of large-conductance Ca²⁺-activated K⁺ (BKCa) channels in vascular smooth muscle. Induces a concentration-dependent decrease in mitochondrial membrane potential (EC₅₀ = 3.6 μM).