oxphos

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

DX3-213B is a potent, orally active inhibitor of oxidative phosphorylation (OXPHOS) complex I with an IC50 of 3.6 nM. DX3-213B blocks ATP production (IC50: 11 nM) and inhibits the growth of MIA PaCa-2 cells (GI50: 11 nM). DX3-213B can be used to study pancreatic cancer.

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.

IMT1 (Propanamide, N,N-dimethyl-2-[[4-(2-methylphenyl)-2-oxo-2H-1-benzopyran-7-yl]oxy]-) has anticancer activity.

OXPHOS-IN-1 (compound 2) is an inhibitor of oxidative phosphorylation (OXPHOS) that inhibits the growth of MIA PaCa-2 cells (IC50: 2.34 μM) and BxPC-3 cells (IC50: 13.82 μM).

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.

IM-156 acetate, an activator of NADH dehydrogenase (IC50=2.2 μM) and AMP-activated protein kinase alpha (AMPKα), is an orally available and bioavailable inhibitor of mitochondrial oxidative phosphorylation (OxPhos).IM-156 acetate increases AMPKα activity and inhibits chlorhexadiene-induced peritoneal fibrosis and inhibit tumor growth in rats .

OXPHOS-IN-2 is an orally active inhibitor of OXPHOS, demonstrating potent inhibitory effects in PC9 cells (IC50= 12.3 nM) and Bxpc-3 cells (IC50= 250 nM in glucose medium, IC50= 17.5 nM in galactose medium). It modulates the NADH/NAD+ ratio and decreases ATP levels. OXPHOS-IN-2 induces apoptosis in tumor cells by activating reactive oxygen species (ROS) and downregulating Nrf2 levels. This compound is applicable for research in cancers such as non-small cell lung cancer and pancreatic cancer.

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.

Nicotinamide N-oxide (Nicotinamide 1-oxide) is recognized as an in vivo metabolite of nicotinamide which is a precurser of nicotinamide-adenine dinucleotide (NAD+) in animals. The enzyme that catalyzes the reduction of nicotinamide N-oxide to nicotinamide in the liver is xanthine oxidase.

Oxyclozanide (Oxyclozanid) is a salicylanilide anthelmintic used in grazing animals for fasciola and cestode infestations.

Phenoxyethanol (NSC-1864) is germicidal. It often used together with quaternary ammonium compounds.

Benzarone (Benzarona) is a potent inhibitor of human uric acid transporter 1 (URAT1, IC50 = 2.8 μM in oocyte). Benzarone lowers the level of uric acid serum.

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

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.

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.

NMac1 (Nm23 activator 1) is a natural compound, cassumunene, derived from Zingiber cassumunar Roxb. and traditionally used as an anti-inflammatory agent in East Asia. NMac1 exhibits anti-metastatic potential by directly interacting with the C-terminal of Nm23-H1, activating its NDP kinase (NDPK) enzymatic activity in vitro. NMac1 inhibits breast cancer metastasis in vivo.

(E)-NMac1 is a compound extracted from Java ginger, useful in cardiovascular disease and neurodegenerative disease research.

HL271 hydrochloride is a chemical derivative of metformin and a potent AMPK activator that enhances AMPK phosphorylation levels. In animal models, HL271 hydrochloride alleviates age-related cognitive impairment. As an effective inhibitor of oxidative phosphorylation (OXPHOS), HL271 can be used in solid tumor research.

BAM 15 is an uncoupler of mitochondrial protonophore.

ATP Synthesis-IN-4 is a mitochondrial-targeting small molecule ligand that inhibits ATP synthesis. This compound binds with mtDNA G4s in melanoma cells, leading to alterations in mitochondrial metabolism and suppression of cell proliferation. It inhibits the translation of essential mitochondrial respiratory chain proteins (CYTB, ATP8, COX1, COX3, ND2) in these cancer cells and downregulates the expression of OXPHOS complexes. Additionally, it activates AMPK phosphorylation, inducing metabolic reprogramming to upregulate glycolysis. ATP Synthesis-IN-4 is a valuable tool for research related to melanoma.

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.