oxidative phosphorylation

IMT1B (LDC203974) is an orally administered, specific noncompetitive allosteric inhibitor of mitochondrial RNA polymerase (POLRMT), effectively suppressing mitochondrial DNA (mtDNA) expression and conferring anti-tumor properties.

Usnic Acid (Usniacin) is an antimicrobial, antitumor and enzyme inhibiting agent shown to uncouple oxidative phosphorylation in mouse-liver mitochondria. Usnic acid induces necrosis in certain cells.

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.

Rafoxanide as a dual CDK4 6 inhibitor for the treatment of skin cancer. Rafoxanide is a salicylanilide used as an anthelmintic. It is used to treat fluke, hookworm and other infestations.

4'-Hydroxychalcone (2-Benzal-4-Hydroxyacetophenone) is a chalcone metabolite with hepatoprotective activity

PZL-A, an activator of mtDNA synthesis, restored the function and activity of the most common POLγ mutant variant and activated mtDNA synthesis in the cells of pediatric patients with fatal diseases, thereby enhancing the oxidative phosphorylation mechanism and the biogenesis of cellular respiration, and can be used to treat progressive diseases associated with mtDNA depletion.

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.

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

Oligomycin A (MCH 32) is an inhibitor of ATP synthase, inhibits oxidative phosphorylation and all the ATP-dependent processes occurring on the coupling membrane of mitochondria.

IM156 (HL156A; HL271 acetate) is a chemical derivative of Metformin. IM156 is a potent and orally active AMPK activator that increases AMPK phosphorylation. IM156 attenuates aging-associated cognitive impairment in animal model [1] [2]. IM156 is a potent oxidative phosphorylation (OXPHOS) inhibitor which is able to be used for the research of solid tumors [3].

Calcimycin (A-23187) is an ionophorous, polyether carboxylic antibiotic from Streptomyces chartreusensis. It binds and transports calcium and other divalent cations across membranes, uncouples oxidative phosphorylation, and inhibits ATPase of rat liver mitochondria. The substance is primarily used as a biochemical tool to study the role of divalent cations in various biological systems.

BAM 15 is an uncoupler of mitochondrial protonophore.

Choerospondin, a dietary flavonoid glycoside isolated from the bark of the southern date palm (Ziziphus jujuba L.), is a potential α-glucosidase inhibitor with antiproliferative, antioxidant, antitumor, and anti-inflammatory activities that enhances the resistance to oxidative stress, and significantly inhibits inflammatory responses by attenuating mitogen-activated protein kinase phosphorylation and nuclear factor-κ B activation.

Gboxin is an inhibitor of oxidative phosphorylation that targets glioblastoma,inhibits the activity of F0F1 ATP synthase, with antitumour activity.

PDHK1-IN-1 (compound 17) is a selective inhibitor of PDHK1 with an IC50 value of 1.5 μM, demonstrating anticancer properties. PDHK1 negatively regulates the pyruvate dehydrogenase complex (PDC), thereby restricting the tricarboxylic acid (TCA) cycle and oxidative phosphorylation. Overexpression of PDHK1 leads to increased reliance on glycolysis (Warburg effect). PDHK1-IN-1 inhibits phosphorylation at the PDHK1 recognition site PDC E1α Ser232 and also suppresses phosphorylation of Ser293.

Calcium 2-hydroxypropanoate (pentahydrate) acts as an activator of the hydroxyl-carboxylic acid receptor 1 (HCAR1) and serves as an epigenetic regulator that induces lysine residue lactylation. This compound, a glycolysis end product, bridges the gap between glycolysis and oxidative phosphorylation and functions as a tumor metabolite with immunoprotective effects of lactate in antitumor immunity.

Oligomycin is an antifungal antibiotic that is an inhibitor of H+-ATP synthetase. The Oligomycin blocks oxidative phosphorylation and the electron transport chain. Oligomycin inhibited HIF-1alpha expression in hypoxic tumor cells.

13-Hydroxystevane shows an inhibitory action on oxidative phosphorylation.

Clidanac, a potent anti-inflammatory drug, has been found to uncouple oxidative phosphorylation.

IACS-010759 hydrochloride is an orally potent and selective OXPHOS inhibitor that inhibits proliferation and induces apoptosis in OXPHOS-dependent brain cancer and acute myeloid leukaemia models for the study of relapsed refractory AML and advanced solid tumours.

Rutamycin is a macrolide antibiotic of the oligomycin group obtained from Streptomyces rutgersensis. It inhibits various ATPases and uncouples oxidative phosphorylation from electron transport.

Bromethalin works by uncoupling mitochondrial oxidative phosphorylation.

KH-176 is an effective intracellular REDOX regulator that targets reactive oxygen species, which are important in the pathogenesis of mitochondrial oxidative phosphorylation disorders and may be used to treat mitochondrial diseases.