Oxidative Phosphorylation Inhibitor

OXPHOS-IN-3 is a mitochondria-targeted dual OXPHOS/glycolysis inhibitor. OXPHOS-IN-3 exhibits potent antiproliferative activity against pancreatic cancer cells. OXPHOS-IN-3 induces mitochondrial dysfunction, ferroptosis, and immunogenic cell death (ICD). OXPHOS-IN-3 shows potent antitumor activity in pancreatic ductal adenocarcinoma (PDAC) models.

POLRMT-IN-4 is a photoactivated mitochondrial RNA polymerase (POLRMT) inhibitor. POLRMT-IN-4 can be liberated from the photoactivatable prodrug upon irradiation, enables spatiotemporally precise inhibition and localized tissue selectivity. POLRMT-IN-4 disrupts mitochondrial transcription, impairs oxidative phosphorylation, and suppresses cancer cell proliferation. POLRMT-IN-4 can be used in research on various cancers, such as pancreatic cancer.

ATP Synthesis-IN-4 is a mitochondria-targeted small-molecule ligand that inhibits ATP synthesis. ATP Synthesis-IN-4 binds to mtDNA G4s in melanoma cells, thereby inducing changes in mitochondrial metabolism and inhibiting cell proliferation. ATP Synthesis-IN-4 suppresses the translation of key mitochondrial respiratory chain proteins (CYTB, ATP8, COX1, COX3, ND2) in melanoma cells, downregulates the expression of OXPHOS complexes, activates the phosphorylation of AMPK, and induces metabolic reprogramming to upregulate glycolysis. ATP Synthesis-IN-4 is applicable to relevant research on melanoma.

GT19630 is an orally active c-Myc PROTAC targeted degrader based on the cereblon E3 ubiquitin ligase, with an IC₅₀ of 1.5 nM against human c-Myc. GT19630 mediates the degradation of MYC, GSPT1, GSPT2, CK1 alpha, N-Myc, B7-H3 and XIAP, and disrupts the MYC-GSPT1 synergistic regulatory feedback loop. GT19630 inhibits cell proliferation, blocks S-phase progression of the cell cycle, promotes cell apoptosis, reduces cell migration capacity, induces integrated stress response, and blocks oxidative phosphorylation by inhibiting the TCA cycle. GT19630 can be used in the research of Myc-driven hematological cancers, small cell lung cancer, breast cancer, TP53-mutant cancers, and venetoclax-resistant cancers.

Ureidopropionic acid (3-Ureidopropionic acid) is a selective mitochondrial respiratory chain complex V inhibitor. Ureidopropionic acid induces the production of reactive oxygen species, delayed elevation of intracellular calcium concentration, secondary energy-dependent excitotoxicity and neurodegeneration in neurons. Ureidopropionic acid promotes neuropathological changes by impairing mitochondrial energy metabolism, oxidative stress and excitotoxicity pathways. Ureidopropionic acid can be used in studies related to 3-ureidopropionase deficiency and severe propionic aciduria.

BDE 47 targets mitochondria, inhibits mitochondrial oxidative phosphorylation (OXPHOS), decreases mitochondrial membrane potential (MMP) and induces apoptosis in embryonic cell. BDE 47 induces the generation of ROS, and activates the JNK signaling pathway. BDE 47 exhibits embryonic developmental toxicity in zebrafish.

MS-L6 is a OXPHOS inhibitor and antimalarial agent. MS-L6 inhibits NADH oxidation and electron transport. MS-L6 induces OXPHOS uncoupling, dissipates mitochondrial membrane potential, increases non-ATP-coupled oxygen consumption, and reduces ATP synthesis. MS-L6 triggers the production of ROS. MS-L6 exhibits anti-amoebic activity. MS-L6 exerts antitumor activity in mouse lymphoma xenograft models. MS-L6 can be used in research related to B-cell lymphoma, T-cell lymphoma, and non-Hodgkin B-cell lymphoma.

Diafenthiuron is a thiourea compound commonly used a broad-spectrum insecticide and acaricide. Diafenthiuron disturbs the insect respiratory system by inhibiting the oxidative phosphorylation and mitochondrial ATP synthesis.

Benzarone is an oral inhibitor of human urate transporter 1 (hURAT1) with an IC₅₀ value of 2.8 μM, and it also acts as an uncoupler of oxidative phosphorylation. Benzarone can cause liver damage and promote cell apoptosis and necrosis. Benzarone can be used to lower serum uric acid levels and for research in vascular diseases.

Moringa Extract is the extract of Moringa with antioxidative and antibacterial activity. Moringa Extract increases Nrf2 and NQO1 expression, scavenges radicals, reduces oxidative stress, inhibits growth of Staphylococcus aureus and Escherichia coli. Moringa Extract can be used for the research of dietary supplements, cosmetics, and natural water purification.

IM176OUT05 (2-Me-Phen hydrochloride), a biguanide, is a mitochondrial OXPHOS inhibitor. IM176OUT0 inhibits mitochondrial electron transport chain (ETC) activity with an IC₅₀ of 3.2 μM. IM176OUT05 activates stem cell metabolism, promotes hair regrowth and increases stemness induction and maintenance during the pluripotent stem cell generation process.

Ureidopropionic acid (Standard) is the analytical standard of Ureidopropionic acid. This product is intended for research and analytical applications. Ureidopropionic acid (3-Ureidopropionic acid) is a selective mitochondrial respiratory chain complex V inhibitor. Ureidopropionic acid induces the production of reactive oxygen species, delayed elevation of intracellular calcium concentration, secondary energy-dependent excitotoxicity and neurodegeneration in neurons. Ureidopropionic acid promotes neuropathological changes by impairing mitochondrial energy metabolism, oxidative stress and excitotoxicity pathways. Ureidopropionic acid can be used in studies related to 3-ureidopropionase deficiency and severe propionic aciduria.

JWJ-01-306 is a CRBN-recruiting ZBTB11 Molecular Glues degrader. JWJ-01-306 degrades ZBTB11 and reprograms cellular metabolism, thereby reducing the level of Oxidative Phosphorylation and the activity of the tricarboxylic acid cycle. JWJ-01-306 enhances the response of organoids to K-Ras inhibition. JWJ-01-306 inhibits the proliferation of pancreatic ductal adenocarcinoma cells and melanoma cells. JWJ-01-306 can be used in studies related to pancreatic ductal adenocarcinoma and melanoma.

BD-AcAc2 (R,S-1,3-Butanediol acetoacetate diester) is an orally active, CNS-penetrant antiepileptic agent. BD-AcAc2 inhibits NF-κB, NLRP3 inflammasome, caspase-1/3, pyroptosis, apoptosis, and enhances autophagy. BD-AcAc2 exhibits antioxidant activity by modulating ROS, MDA, SOD, and GSH levels, and alleviates oxidative stress. BD-AcAc2 mitigates chronic colitis, counteracts Dextran Sodium Sulfate (DSS)-induced pathology, protects against central nervous system oxygen toxicity and acute lung injury, and exhibits anti-seizure efficacy. BD-AcAc2 can be used for the research of colitis, sarcopenia, acute lung injury, seizure, and obesity.

TPP-IOA is a cytochrome c peroxidase inhibitor. TPP-IOA inhibits apoptosis by preventing cardiolipin oxidation and cytochrome c release to the cytosol. TPP-IOA disrupts oxidative phosphorylation in isolated mitochondria. TPP-IOA inhibits cell death in SH-SY5Y cells grown in glucose, but not galactose. TPP-IOA causes mitochondrial depolarization and network fragmentation. TPP-lOA mitigates radiation induced death in mice.

R419 is a Complex I inhibitor. R419 has anti-cancer activity against liver cancer.

OXPHOS-IN-2 is an orally active OXPHOS inhibitor. OXPHOS-IN-2 exhibits potent inhibitory activity in PC9 (IC₅₀ = 12.3 nM) and Bxpc-3 cells (IC₅₀ = 250 nM in glucose medium, IC₅₀ = 17.5 nM in galactose medium). OXPHOS-IN-2 decreases the NADH/NAD⁺ ratio and reduces ATP levels. OXPHOS-IN-2 induces tumor cells apoptosis by activating reactive oxygen species (ROS) and downregulating the level of Nrf2. OXPHOS-IN-2 can be used for research on cancer such as non-small cell lung cancer and pancreatic cancer.

Phenoxyethanol-d₄ is the deuterium labeled Phenoxyethanol. Phenoxyethanol has a broad spectrum of antimicrobial agent. Phenoxyethanol is an uncouple agent in oxidative phosphorylation from respiration and competitively inhibits malate dehydrogenase. Phenoxyethanol is used as a preservative in cosmetic, vaccine, and textile, et al.

STAT3-IN-32 is an orally active, selective STAT3 SH2 domain inhibitor with a K_d of 21.3 nM, showing selectivity over STAT1/5. STAT3-IN-32 binds to the STAT3 SH2 domain, blocks Tyr705 and Ser727 phosphorylation, abrogates nuclear transcription and mitochondrial oxidative phosphorylation functions. STAT3-IN-32 inhibits tumor growth in mouse pancreatic cancer xenograft models. STAT3-IN-32 can be used for the research of pancreatic cancer.

LCB-2151 (Compound 2), a nucleoside analogue, is an anticancer agent. LCB-2151 disrupts the two primary sources of ATP production (glycolysis and mitochondrial oxidative phosphorylation), reducing the bioenergetic capacity of KRAS-mutated pancreatic cancer cells and inducing ROS formation. LCB-2151 effectively inhibits key enzymes (such as CACT and CPT2) in glycolysis, the TCA cycle and fatty acid β-oxidation. LCB-2151 has significant cytotoxicity and induces cells apoptosis. LCB-2151 can be used for radiation therapy of cancers research.