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Mitochondrial metabolism compounds act on the respiratory chain, energy coupling and redox balance of mitochondria. In 1961 Mitchell proposed that phosphorylation is coupled to electron transfer through a chemiosmotic mechanism. In this model a proton gradient across the inner membrane drives adenosine triphosphate (ATP) synthase in oxidative phosphorylation (OXPHOS). Rotenone inhibits complex I of the electron transport chain, and oligomycin A blocks ATP synthase. Gboxin, reported in 2019, is an OXPHOS inhibitor that suppresses the growth of glioblastoma cells. Mito-TEMPO is a mitochondria-targeted antioxidant that scavenges superoxide in the matrix. Meldonium inhibits carnitine biosynthesis and so limits fatty acid transport into mitochondria. The set is mixed and also lists compounds with secondary mitochondrial links, such as the fluoroquinolone ciprofloxacin.
PDK4-IN-1 is a potent inhibitor of pyruvate dehydrogenase kinase 4 (PDK4), demonstrating an IC50 value of 84 nM. This anthraquinone derivative effectively represses cellular transformation and proliferation while inducing apoptosis. PDK4-IN-1 holds promising applications in the fields of cancer research, diabetes treatment, and allergy modulation.
Drpitor1a is a selective inhibitor of Dynamin-related protein 1 (Drp1). This compound effectively reduces mitochondrial reactive oxygen species (ROS) production and prevents mitochondrial fission, contributing to improved right ventricular diastolic dysfunction during ischemia-reperfusion injury. Drpitor1a holds potential for research applications in lung cancer, facilitating studies on mitochondrial dynamics and their role in cancer pathophysiology.
DRP1 Allosteric-IN-3 is an allosteric inhibitor targeting DRP1, with an IC50 value of 11 μM for the DRP1:MiD49 protein-protein interaction. This compound provides valuable insights into mitochondrial division processes and related disorders. Its application in research can facilitate the understanding of diseases associated with mitochondrial dysfunction.
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DRP1i27 is a selective inhibitor of human dynamin-related protein 1 (Drp1). By binding to the GTPase site and forming critical hydrogen bonds with Gln34 and Asp218, DRP1i27 effectively modulates Drp1-mediated mitochondrial fission. This compound has demonstrated protective effects against simulated ischemia-reperfusion injury in cell line models, making it valuable for research into mitochondrial dynamics and neuroprotection.
Drp1-IN-1 is a selective inhibitor of dynamin-related protein 1 (Drp1), exhibiting an IC50 of 0.91 μM. This compound interferes with Drp1's regulatory role in mitochondrial dynamics, promoting mitochondrial fusion and potentially mitigating cellular stress responses. Drp1-IN-1 is useful in research focused on mitochondrial function, neurodegenerative diseases, and other conditions where oxidative stress plays a critical role.
MB-0223 is a selective partial inhibitor targeting the dynamin-related GTPase Drp1, with an IC50 of 1.3 μM, demonstrating high potency and specificity over other dynamin family members, such as Opa1 and dynamin-1 (IC50 > 100 μM). This compound is useful in studies investigating mitochondrial dynamics, apoptosis, and cellular energy metabolism, making it an important tool for research on neurodegenerative diseases and cancer biology.
DRP1 Allosteric-IN-2 is a potent allosteric inhibitor of Dynamin-related protein 1 (DRP1). It demonstrates an IC50 value of 4.3 μM for inhibiting the DRP1:MiD49 protein-protein interaction. This compound is valuable for investigating diseases associated with mitochondrial division disorders, providing insights into cellular dynamics and potential therapeutic strategies.
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DRP1 Allosteric-IN-1 is an allosteric inhibitor of dynamin-related protein 1 (DRP1), demonstrating an IC50 of 3.6 μM for disrupting the DRP1:MiD49 protein-protein interaction. This compound serves as a valuable tool for investigating mitochondrial division disorders and associated pathologies. Its application in biochemical research can enhance the understanding of the role of mitochondrial dynamics in diverse diseases.
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Synonyms: Malonyl coenzyme A tetralithium
Malonyl CoA tetralithium is a potent inhibitor of carnitine palmitoyltransferase 1 (CPT1), a key enzyme in fatty acid oxidation. By inhibiting CPT1, Malonyl CoA tetralithium effectively modulates fatty acid metabolism, serving as a crucial substrate in fatty acid biosynthesis. This compound is valuable for research applications focused on metabolic processes and the regulation of lipid pathways.
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Synonyms: Malonyl coenzyme A
Malonyl CoA is an inhibitor of carnitine palmitoyltransferase 1 (CPT1), targeting the regulation of fatty acid oxidation. This compound serves as a substrate in fatty acid biosynthesis, influencing metabolic pathways involved in energy production. Its key biological activity makes it a valuable reagent for research applications in studies related to metabolic disorders and cellular energy homeostasis.
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Synonyms: Malonyl coenzyme A lithium
Malonyl CoA lithium is a selective inhibitor of carnitine palmitoyl transferase 1 (CPT1), a key enzyme in fatty acid oxidation. At elevated concentrations, Malonyl CoA lithium effectively suppresses fatty acid oxidation, while at lower concentrations, it allows for enhanced fat oxidation. This compound is valuable in studies exploring metabolic regulation and the role of fatty acid metabolism in various physiological and pathological conditions.
GNX-865 is an inhibitor of the mitochondrial permeability transition pore (mPTP) that plays a crucial role in cellular protection against ischemia-reperfusion injury. This compound has demonstrated effectiveness in mitigating cell death and promoting cell survival in various in vivo models. Its applications extend to research focused on cardiovascular diseases and mitochondrial dysfunction, making it a valuable tool for studying therapeutic strategies in ischemic conditions.
NRG1271 is an orally active inhibitor of the mitochondrial permeability transition pore (mPTP) that effectively penetrates the blood-brain barrier. This compound demonstrates significant neuroprotective properties, making it a valuable tool for investigating various neurological diseases and disorders. Its ability to modulate mitochondrial function positions NRG1271 as a key reagent in research focused on neurodegeneration and related pathologies.
Ferulenol is a sesquiterpene prenylated coumarin derivative that specifically inhibits succinate ubiquinone reductase within the ubiquinone cycle. This compound exhibits significant antimycobacterial activity, making it a potential candidate for studying mycobacterial infections. Additionally, Ferulenol is noted for its haemorrhagic properties, contributing to its diverse applications in biological research related to mitochondrial metabolism and infectious disease mechanisms.
mPTP-IN-1 is a specific inhibitor of the mitochondrial permeability transition pore (mPTP). It functions by blocking calcium-induced mPTP opening through targeting the C subunit of ATP synthase. This compound is useful in research involving myocardial ischemia/reperfusion injury (IRI), providing insights into mitochondrial function and cell survival in pathological conditions.
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Synonyms: Methyl palmoxirate; NSC359682
McN3716 is an inhibitor of carnitine palmitoyltransferase I (CPT-1), a key enzyme involved in mitochondrial fatty acid metabolism. By specifically targeting CPT-1, McN3716 effectively modulates lipid oxidation and energy production pathways in the mitochondria. This compound is suitable for research applications focused on metabolic disorders, obesity, and conditions related to altered mitochondrial function.
Synonyms: (+)-C75
(+)-trans-C75 is a selective inhibitor of carnitine palmitoyltransferase 1 (CPT1). This compound demonstrates potential for modulating energy metabolism and exhibits anorectic properties, making it relevant for weight management research. While it is less potent than the racemic mixture or the (-) enantiomer in enhancing the cytotoxic effects of ionizing radiation in cancer treatment, its unique properties make it a valuable tool for studying metabolic regulation in various biological contexts.
M77976 is a selective ATP-competitive inhibitor of pyruvate dehydrogenase kinase isoform 4 (PDK4), exhibiting an IC50 of 648 μM. This compound plays a critical role in metabolic research, particularly in the study of obesity and diabetes, by modulating glucose metabolism and energy homeostasis. M77976 is valuable for exploring the therapeutic potential of targeting PDK4 in metabolic disorders.
Synonyms: 1,4-Dihydroxy-6-naphthoic acid
DHNA, a selective PDK4 inhibitor, exhibits an IC50 value of 18 μM. This compound is valuable for investigating the role of PDK4 in metabolic regulation, particularly in the context of heart failure. Its ability to modulate energy metabolism makes DHNA a relevant tool for research focused on cardiac function and related pathophysiological conditions.
PDK4-IN-2 is a selective inhibitor of pyruvate dehydrogenase kinase 4 (PDK4) with an IC50 of 46 µM. It has demonstrated the ability to enhance ejection fraction in failing hearts by modulating bioenergetics through the activation of the tricarboxylic acid cycle. This compound is valuable for research into cardiac metabolism and potential therapeutic strategies for heart failure.
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