Catalog No.
Product Name
Application
Product Information
Citations
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Mitochondrial F0F1-ATPase Inhibitor
Isoapoptolidin is an inhibitor of the mitochondrial F0F1-ATPase, exhibiting a Ki greater than 100 μM and selective action towards mitochondrial complex V. This compound is valuable for investigating mitochondrial energy metabolism-related disorders, including cancer and neurodegenerative diseases. Its inhibitory properties facilitate studies on the role of ATP synthase in cellular energy regulation. -
Ca2+-ATPase Inhibitor
IPrAuCl is a gold compound that functions as a selective inhibitor of sarcoplasmic reticulum Ca2+-ATPase, demonstrating an IC50 value of 16.3 µM. Its primary mechanism involves hindering calcium ion transport, making it a valuable tool for researching calcium homeostasis and muscle contraction dynamics. IPrAuCl may also be useful in studies investigating the role of Ca2+-ATPase in various cellular processes and diseases. -
Ca2+- ATPase Activator
Rp-8-Br-cGMPS sodium is a potent activator of Ca2+-ATPase, facilitating the reduction of cytosolic Ca2+ levels. This compound acts as an agonist of the rod cyclic nucleotide-gated (CNG) channel while also inhibiting protein kinase G (PKG). Its key biological activities make it valuable for research applications involving calcium signaling and cellular calcium homeostasis. -
ATPase
Creatine phosphokinase, Rabbit muscle (CPK) is an enzyme that catalyzes the reversible conversion of creatine and ATP into phosphocreatine and ADP. By facilitating the maintenance of an optimal ATP/ADP ratio, CPK plays a critical role in energy metabolism, particularly during periods of high energy demand. This enzyme is widely used in biochemical research to study cellular energy dynamics and various metabolic disorders. -
Ca2+‑ATPase Inhibitor
rel-(E)-6,7-Transdihydroxyligustilide is a potent inhibitor of Ca2+-ATPase, specifically in calmodulin-deficient human erythrocyte membranes. This compound, derived from the dried tuberous roots of Polygonum multiflorum, plays a significant role in the regulation of calcium homeostasis. It is particularly valuable in research related to hyperlipidemia and related metabolic disorders. -
SERCA Inhibitor
4,4'-Methylenebis(2,6-di-tert-butylphenol) is a selective inhibitor of sarco/endoplasmic reticulum calcium ATPase (SERCA), with an IC50 value of 17 μM. This compound plays a critical role in modulating calcium homeostasis and is valuable for research into cellular processes and disorders linked to calcium dysregulation. Its application extends to studying various diseases where altered calcium signaling is implicated. -
SERCA Blocker
JTV-519 fumarate is a Ca2+-dependent blocker of the sarcoplasmic reticulum Ca2+-stimulated ATPase (SERCA), functioning as a partial agonist for ryanodine receptors in striated muscle. This compound exhibits cardioprotective properties and demonstrates significant antiarrhythmic activity, making it valuable for research on cardiac function and arrhythmias. Its unique mechanism highlights its potential in studying calcium handling and related cardiac pathologies. -
Ca2+- ATPase Activator
Rp-8-Br-cGMPS (Rp-8-bromo-Cyclic GMP sodium salt) is an effective activator of Ca2+-ATPase, promoting the reduction of cytosolic Ca2+ levels by enhancing the efflux of Ca2+ from cells. Additionally, it acts as an agonist of the rod cyclic nucleotide-gated (CNG) channel and functions as an inhibitor of protein kinase G (PKG). This compound is valuable for studies involving calcium signaling, cellular response mechanisms, and cardiovascular research. -
RyR2 Stabilizer
RyR2 stabilizer-1 is a potent stabilizer of the ryanodine receptor 2 (RyR2) and an activator of the sarco/endoplasmic reticulum Ca2+ ATPase 2a (SERCA2a), exhibiting EC50 values of 2.7 μM for RyR2 and 383 nM for SERCA2a. This compound effectively inhibits calcium leakage from the sarcoplasmic reticulum through RyR2 while enhancing the reuptake of calcium by SERCA2a. As a result, RyR2 stabilizer-1 shows promise in preventing cardiac arrhythmias by maintaining calcium homeostasis in cardiac cells. -
Biochemical Assay Reagent
Digitoxigenin is a biochemical assay reagent primarily used for the study of cardiac glycosides. This compound exhibits significant biological activity, particularly in inhibiting Na+/K+ ATPase, which is crucial for cell membrane potential and ion transport. It is applied in research focusing on cardiac function, cellular signaling, and related pathways in various biological systems. -
Natural Products
Thevetin A is a cardiac glycoside derived from the plant Cascabela thevetioides. It exhibits potent biological activity by inhibiting Na+/K+ ATPase, leading to increased intracellular calcium levels and enhanced contractility of cardiac muscle. This compound is primarily utilized in cardiovascular research to study its effects on cardiac function and potential therapeutic applications in heart disease. -
PM Ca2+-ATPase Inhibitor
Caloxin 2A1 is a selective inhibitor of the plasma membrane Ca2+-ATPase (PMCA), functioning at the extracellular level. This peptide demonstrates a targeted inhibition of PMCA activity without influencing basal Mg2+-ATPase or Na+-K+-ATPase activity. It serves as a valuable tool in studies investigating calcium homeostasis and its implications in cellular signaling and physiology. -
v-ATPase Inhibitor
Verucopeptin is a selective v-ATPase inhibitor that targets the ATP6V1G subunit, effectively reducing v-ATPase activity. This compound has a notable impact on HIF-1 signaling, decreasing the expression of HIF-1α and its target genes. Additionally, Verucopeptin demonstrates antitumor properties against multidrug resistant (MDR) cancers, making it a valuable tool for cancer research. Its specific mechanism and biological activity position it as a significant reagent for studies focused on tumor biology and therapy resistance. -
H+/K+-ATPase Inhibitor
(R)-Tegoprazan is a potent H+/K+-ATPase inhibitor characterized by its benzimidazole structure. It demonstrates an IC50 of 98 nM against canine kidney Na+/K+-ATPase, highlighting its efficacy in modulating ion transport. This compound is prominently applied in research related to gastrointestinal diseases, offering valuable insights into therapeutic interventions. -
PM H+-ATPase Inhibitor
Protonstatin-1 is a selective inhibitor of the plasma membrane H+-ATPase, exhibiting an IC50 of 3.9 μM. By interacting with the central loop of the enzyme, Protonstatin-1 disrupts the functions of the N- and P-domains, ultimately inhibiting pump activity and auxin transport. This reagent is valuable for research in plant physiology and studies involving cellular ion homeostasis. -
V-ATPase Inhibitor
V-ATPase-IN-1 is a selective inhibitor of Vacuolar-type H+-ATPases (V-ATPase), demonstrating an IC50 value of 194.80 μM and a binding affinity for the V-ATPase subunit A with a Kd of 0.803 μM. This compound exhibits notable insecticidal activity against M. separata, with an LC50 of 2.64 mM. V-ATPase-IN-1 is a valuable tool in research focused on the development of chemical insecticides and understanding the biological role of V-ATPase in various organisms. -
H+-K+-ATPase Inhibitor
(±)-Vasicine is a potent inhibitor of H+-K+-ATPase, with an observed IC50 of 73.47 μg/mL. This compound exhibits notable anti-ulcer properties, demonstrating significant anti-secretory, antioxidant, and cytoprotective effects. As such, (±)-Vasicine serves as a valuable reagent for research applications focused on gastrointestinal protection and related mechanisms in cellular physiology. -
H(+), K(+)-ATPase Inhibitor
Lansoprazole sulfone is a selective inhibitor of H+, K+-ATPase, primarily targeting gastric acid secretion. By inhibiting this enzyme, lansoprazole sulfone may significantly stimulate gastric acid secretion, making it a valuable tool in research related to gastric physiology. Its potential applications extend to the study of conditions such as duodenal ulcers, gastric ulcers, gastroesophageal reflux disease, and Zollinger-Ellison syndrome. -
RUVBL1/2 ATPase Inhibitor
TIP48/49-IN-1 is a selective inhibitor of the RUVBL1/2 ATPase, demonstrating an IC50 of 59 nM against purified RUVBL1/2. By disrupting the DNA replication process, TIP48/49-IN-1 induces S-phase arrest and apoptosis in cancer cells. This compound has been shown to inhibit tumor growth and enhance radiosensitivity in non-small cell lung cancer (NSCLC) models, making it a valuable tool for cancer research. -
H+, K+-ATPase Inhibitor
S 1924 is a potent H+, K+-ATPase inhibitor, demonstrating IC50 values of 10.3 μM at pH 7.4 and 1.6 μM at pH 6.0. This compound effectively modulates gastric acid secretion, making it valuable in research related to gastrointestinal physiology and pharmacology. Its specificity for H+, K+-ATPase makes S 1924 a useful tool for investigating proton pump mechanisms and related therapeutic targets. -
V ATPase Inhibitor
FR-167356 is a selective inhibitor of vacuolar ATPase, exhibiting potent activity with IC50 values of 170 nM for osteoclast plasma membranes, 220 nM for macrophage microsomes, and higher values for renal brush border and liver lysosomal membranes. This compound inhibits bone resorption and effectively addresses ovariectomy-induced bone loss. It serves as a valuable tool for research into osteoporosis and related bone disorders. -
V-ATPase Inhibitor
Apicularen B is a potent V-ATPase inhibitor derived from the myxobacterium Archangium gephyra. This cytotoxic macrolide exhibits significant biological activity relevant to the study of V-ATPase-related disorders, including osteopetrosis. Researchers can utilize Apicularen B to investigate the mechanisms underlying these diseases and explore potential therapeutic applications. -
H+/K+-ATPase Inhibitor
KR-60436 is a reversible inhibitor of H+/K+-ATPase, effectively obstructing proton and potassium transport across cellular membranes. This compound has demonstrated potent inhibition of CYP1A2 substrate metabolism, making it a valuable tool for studying gastric proton pump activity and its implications in drug metabolism. Its utility extends to drug interaction studies and the investigation of gastrointestinal pharmacology. -
Active Small Molecule
17α-Hydroxydigitoxigenin is an active small molecule primarily known for its ability to inhibit Na+/K+-ATPase activity. This inhibition plays a crucial role in various physiological processes and has been linked to cardiac and neuroprotective effects. It is relevant for research applications involving ion transport, cellular signaling, and the study of cardiovascular diseases. -
Stable Isotope
Digitoxigenin-21,23,23-d3 is a deuterium-labeled derivative of Digitoxigenin, serving as a stable isotope for research applications. This compound is primarily important for the synthesis of cardiac glycosides used in the treatment of heart failure and arrhythmias. By inhibiting the sodium-potassium ATPase pump, Digitoxigenin enhances cardiac contraction efficiency and force, making it a critical component in cardiovascular research and drug development. -
Brassinosteroid
24-Epicastasterone is a bioactive brassinosteroid that functions as a ligand for the ABCB1 and ABCB19 transporters in Arabidopsis thaliana. Its primary mechanisms include stimulating ATPase activity in ABCB19 and promoting ATP hydrolysis in ABCB1, facilitating the efflux of compounds from plant cells. Additionally, 24-Epicastasterone enhances the activities of catalase and guaiacol peroxidase in wheat roots, thereby mitigating heat-induced lipid peroxidation and improving heat tolerance in common wheat seedlings. This compound is valuable for research into plant stress responses and hormonal signaling pathways. -
Stable Isotope
Pantoprazole-d4 is a deuterated derivative of Pantoprazole, a potent proton pump inhibitor that targets the H+/K+-ATPase enzyme with an IC50 of 6.8 μM. This stable isotope is utilized primarily in pharmacokinetic studies and metabolic research to enhance the accuracy of drug absorption and distribution analysis. Pantoprazole exhibits anti-secretory and anti-ulcer properties, while its combination with Doxorubicin has been shown to significantly increase tumor growth delay, underscoring its potential utility in cancer research. -
Isotope-Labeled Compounds
Digitoxin-d3 is a deuterated derivative of digitoxin, a cardiac glycoside that primarily targets the Na+/K+ ATPase enzyme, enhancing intracellular calcium levels and improving myocardial contractility. This isotope-labeled compound is utilized in pharmacokinetic studies, providing insights into the metabolism and distribution of digitoxin in biological systems. It serves as a valuable tool for researchers examining heart function and the therapeutic mechanisms of cardiac glycosides. -
H+, K+-ATPase Inhibitor
Esomeprazole magnesium, a potent H+, K+-ATPase inhibitor, is utilized in research related to upper intestinal disorders and gastroesophageal reflux disease. Its primary mechanism involves the inhibition of proton pumps, leading to decreased gastric acid secretion. Additionally, Esomeprazole magnesium exhibits properties as an exosome inhibitor by blocking exosome release through the inhibition of vacuolar H+-ATPases, making it valuable for studies on cellular communication and disease progression. -
SERCA Inhibitor
2,5-Di-tert-butylhydroquinone is a potent inhibitor of Sarco/endoplasmic reticulum Ca2+ ATPase (SERCA), demonstrating an IC50 of 400 nM. This compound disrupts the gating function of Glu309, thereby preventing calcium ions from accessing their binding site. Additionally, 2,5-Di-tert-butylhydroquinone influences the activity of key enzymes such as 5-lipoxygenase and COX-2, with IC50 values of 1.8 μM and 14.1 μM, respectively. It is utilized in research focused on cellular calcium regulation and inflammatory processes. -
Proton Pump Inhibitor
Ilaprazole sodium is a potent proton pump inhibitor that irreversibly targets H+/K+-ATPase, demonstrating a dose-dependent inhibition with an IC50 of 6 μM in rabbit parietal cell assays. This compound is primarily utilized in research focused on gastric ulcers, providing insights into gastric acid secretion regulation. Additionally, Ilaprazole sodium acts as an effective inhibitor of TOPK (T-lymphokine-activated killer cell-originated protein kinase), facilitating studies related to immune responses and cancer therapeutics. -
Antidepressant
Depramine, a tricyclic antidepressant, primarily targets neurotransmitter reuptake mechanisms, elevating levels of norepinephrine and serotonin in the synaptic cleft. It exhibits significant biological activity through the inhibition of acetylcholinesterase, Mg2+-ATPase, and Na+/K+ ATPase. Depramine is utilized in research focused on depression and related mood disorders, facilitating studies on neurotransmitter dynamics and cellular signaling pathways involved in antidepressant efficacy. -
Stable Isotope
Cyclopiazonic acid-13C20 is a stable isotope-labeled derivative of Cyclopiazonic acid, a selective inhibitor of endoplasmic reticulum calcium ATPases (ECAs) and has demonstrated efficacy against human respiratory syncytial virus (RSV) with an EC50 value of 4.13 μM. This compound is shown to inhibit the antagonistic effects of serotonin receptors in rat thoracic aorta, induce p53-dependent apoptosis, and exhibit reproductive toxicity in mouse testes, as well as inhibit the biological activation of aflatoxin B. Cyclopiazonic acid-13C20 is valuable for research applications in calcium signaling, viral infections, and toxicology studies. -
Natural Product
Fusicoccin H is a natural product derived from the fungus Fusicoccum amygdali. It primarily functions as a plant growth regulator by promoting continuous activation of plasma membrane H+-ATPase, leading to enhanced cell elongation and growth. This compound is utilized in research to study plant physiological responses and signaling pathways associated with stress resistance and developmental processes. -
Proton Pump inhibitor
Azeloprazole is a proton pump inhibitor that targets the H+,K+-ATPase enzyme, effectively reducing gastric acid secretion. It has demonstrated significant efficacy in preclinical models, including a dog's gastric fistula, where it outperformed esomeprazole in terms of duration of action. This compound is useful in studying acid-related diseases and exploring mechanisms of gastric acid regulation. -
Cardiac Glycoside
Cuspidoside is a cardiac glycoside that primarily targets the sodium-potassium ATPase, leading to increased intracellular calcium levels. This compound exhibits positive inotropic effects, enhancing cardiac contractility and is relevant for the study of cardiovascular diseases, including heart failure. Its pharmacological properties make it a valuable tool for investigating therapeutic strategies in cardiac dysfunction. -
Cardiac Glycoside
Scillaren A is a cardiac glycoside that can be isolated from the bulbs of Dioscorea coromandeliana. It exhibits potent activity in inhibiting the sodium-potassium ATPase pump, leading to increased intracellular calcium concentrations. This compound is primarily utilized in cardiovascular research to study its effects on cardiac contractility and its potential therapeutic applications in heart failure and arrhythmias.
