ATPase

Brefeldin A (Cyanein) belongs to the class of macrolide antibiotics and is an ATPase inhibitor (IC50=0.2 μM). Brefeldin A can induce tumor cell differentiation and apoptosis, and also possesses autophagy inhibitory activity.

Tirofiban(MK383) hydrochloride monohydrate is a non-peptide glycoprotein IIb IIIa antagonist.

Bufalin is an active ingredient and one of the glycosides in the traditional Chinese medicine ChanSu; it is also a bufadienolide toxin originally isolated from the venom of the Chinese toad Bufo gargarizans, with potential cardiotonic and antineoplastic a

(-)-Blebbistatin ((S)-(-)-Blebbistatin) is an S enantiomer of blebbistatin. It is a potent and selective myosin II inhibitor with IC50 ranging from 0.5 to 5 μM.

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.

Oleic acid (Glycon Wo) is a natural product, a common monounsaturated fatty acid found in a variety of animal and vegetable fats and oils. Palmitic acid is a Na+ K+ ATPase activator.

Chebulinic acid is a potent inhibitor of M. tuberculosis DNA gyrase. It also can inhibit SMAD-3 phosphorylation and H+ K+-ATPase activity.

Cinobufagin (Cinobufagine) is a selective Na+ K+-ATPase inhibitor. The activity of Cinobufagin is same as ouabain.

Blebbistatin ((±)-Blebbistatin) is a non-muscle myosin II (NMII)-selective and non-muscle myosin heavy chain 9 (MYH9)-specific inhibitor that promotes directional migration of corneal endothelial cells (CECs) and accelerates wound healing, while preserving the integrity of cell junctions and barrier function.

FCCP (Trifluoromethoxy carbonylcyanide phenylhydrazone) is an oxidative phosphorylation (OXPHOS) inhibitor and mitochondrial proton carrier uncoupler. FCCP is often used as an apoptosis inducer.

Cytochalasin D is an actin inhibitor, the removal of actin stress fibers is crucial for the chondrogenic differentiation. It may be an inhibitor of some fertilization processes such as sperm penetration or sperm head decondensation. Cytochalasin D inhibit

Licoflavone B has schistosomicidal activity, it showed high S. mansoni ATPase (IC50 of 23.78 μM) and ADPase (IC50 of 31.50 μM) inhibitory activities.

Ginsenoside Rb1 (Gypenoside Ⅲ) is part of a class of steroid glycosides; may have properties that inhibit or prevent the growth of tumors.

SKF96067 is a reversible gastric H+ K+-ATPase inhibitor that can induce relaxation of human airway smooth muscle in vitro.

Ciclopirox (HOE296b) exerts its action by binding to and chelating trivalent cations, such as Fe3+ and Al3+, thereby inhibiting the availability of essential co-factors for enzymes. Ciclopirox is a synthetic, broad-spectrum antifungal agent with additional antibacterial and anti-inflammatory activities. This may lead to a loss of activity of enzymes that are essential for cellular metabolism, the organization of cell wall structure and other crucial cell functions. In addition, ciclopirox exerts its anti-inflammatory activity by inhibiting 5-lipoxygenase and cyclooxygenase (COX).

Strictosamide possesses antibacterial and antiviral activities, it also may have important effects on inflammation and inflammatory pain.

AGN-201904 is an omeprazole prodrug and proton pump inhibitor, which may delay aging and be used for the prevention and treatment of peptic ulcers.

NC-1300-B inhibits H(+)-K(+)-ATPase and is used in the study of gastric ulcers.

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

Digitoxin (Digitoxinum) is an effective Na+ K+-ATPase inhibitor (EC50 value: 0.78 μM).

Sodium oleate (cis-9-Octadecenoic acid sodium salt) (Oleic acid sodium) is an abundant monounsaturated fatty acid sodium. Sodium oleate is a Na+ K+ ATPase activator.

L-Palmitoylcarnitine (L-PC) is an important endogenous fatty acid metabolite that inhibits Na K ATPase activity and potentiates fibrinolytic enzymes and tPA to inhibit thrombosis.

Ciliobrevin D is a AAA+ ATPase motor cytoplasmic dynein inhibitor. Ciliobrevin D inhibits Hedgehog (Hh) signaling and primary cilia formation and it also inhibits dynein-dependent microtubule gliding and ATPase activity in vitro.

Lanatoside C (Ceglunate) is a cardiac glycoside, a type of drug that can be used in the treatment of congestive heart failure and cardiac arrhythmia (irregular heartbeat). Lanatoside C can be used orally or by the intravenous route.

L-Palmitoylcarnitine chloride (Palmitoyl-L-carnitine chloride) is a fatty acid metabolite with antithrombotic properties that protects mice from ischemic stroke by counteracting intracerebral thrombosis in the tMCAO model.L-Palmitoylcarnitine chloride (Palmitoyl-L-carnitine chloride) is a fatty acid metabolite with antithrombotic properties. Palmitoylcarnitine chloride inhibits the Na K pump in the heart and inhibits FeCl 3-induced arterial thrombosis Attenuates intracerebral thrombosis and inflammation in a mouse model of transient middle cerebral artery occlusion (tMCAO).

Bacoside A3 has antioxidant potential, it shows comparatively higher neuroprotective response analysed as higher cell viability and decreased intracellular ROS.

Deslanoside (Desacetyllanatoside C) is a rapidly acting cardiac glycoside used to treat congestive heart failure and supraventricular arrhythmias associated with reentry mechanisms. It inhibits the Na-K-ATPase membrane pump, increasing intracellular sodium and calcium concentrations.

Tiludronate disodium (Tiludronic acid disodium) is an osteoclast vacuolar H(+)-ATPase inhibitor with antiresorptive and anti-inflammatory properties. Tiludronate disodium can be used in studies about metabolic bone disorders.

Strophanthidin (Strophanthidine) can induce calcium overload in vivo.

Ouabain octahydrate (Acocantherine) is a cardiac glycoside that inhibits Na(+) K(+) ATPase. Ouabain octahydrate regulates transcription of MDR (increase, Pgp) and MRP (increase MRP1 and decrease CFTR, cyctic fibrosis transport receptor or cAMP-activated Cl- channel) genes, also alters localization of MRP1.

Istaroxime hydrochloride (PST2744 hydrochloride) is a Na+ K+-ATPase inhibitor and sarcoplasmic endoplasmic reticulum calcium ATPase 2 (SERCA 2) activator, a novel positive inotropic compound that can be used to study acute heart failure.

Neriifolin (17β-Neriifolin), a cardiac glycoside extracted from the unripe fruit of Cerbera manghas, is a Na+K+-ATPase inhibitor with anticancer activity that inhibits cell proliferation by suppressing HOXA9-dependent gene expression and inducing apoptosis in the human acute myeloid cell line, THP-1. Neriifolin induces cell cycle arrest and apoptosis in human hepatocellular carcinoma HepG2 cells and can be used in prostate cancer research.

Fenbufen (Lederfen) is a non-steroidal anti-inflammatory drug used primarily to treat inflammation in osteoarthritis, ankylosing spondylitis, and tendinitis. It can also be used to relieve backaches, sprains, and fractures. Fenbufen is available as a capsule or tablet sold with the brand names Cepal, Cinopal, Cybufen, Lederfen, and Reugast. Fenbufen acts by preventing cyclooxygenase from producing prostaglandins which can cause inflammation.

Sudoterb free base (Sudoterb) , also known as LL3858, is an anti-tubercular drug candidate.

FR-167356 is a specific inhibitor of a3 isoform vacuolar type H⁺-ATPase with IC50s of 170 nM, 370 nM and 220 nM for osteoclast plasma membranes, renal brush border membranes and macrophage microsomes. FR-167356 reduces bone metastasis of B16-F10 cells.

Ciclopirox olamine is a broad-spectrum antifungal agent with additional antibacterial and anti-inflammatory activities.

(+)-SJ733 (SJ000557733) is a potent Na+-ATPase PfATP4 inhibitor with antimalarial activity for the study of malaria.

D-α-Hydroxyglutaric acid disodium [Disodium (R)-2-Hydroxyglutarate] is a competitive inhibitor of α-ketoglutarate-dependent dioxygenases with a Ki of 0.628 mM.

SCH28080 is a reversible and K+-competitive inhibitor of gastric H+ K+-ATPase with an IC50 value of 20 nM (rabbit microsomal membrane).SCH28080 is a potent inhibitor of acid secretion in vivo with anti-ulcer activity, anti-secretory and cytoprotective activity.

Suloctidil is a peripheral vasodilator that was formerly used in the management of peripheral and cerebral vascular disorders. It is hepatotoxic and fatalities have occurred.

3'4'7-Trihydroxyflavone can markedly inhibit the receptor activator of nuclear factor kappa B ligand (RANKL) induced osteoclastic differentiation from mouse bone marrow derived macrophages (BMMs), it inhibits osteoclastogenesis via nuclear factor of activ

(-)-Denudatin B (Denudatin B) is derived from Magnolia fargesii. (-)-Denudatin B has nonspecific antiplatelet action at high concentration by inhibiting phosphoinositides breakdown induced by collagen and thrombin.

Phlorizin (Phloridzin) is a non-selective SGLT inhibitor found in apple, for hSGLT1( Ki=300 nM) and hSGLT2( Ki=39 nM) .

Diazoxide (Proglycem) is a benzothiadiazine derivative that is a peripheral vasodilator used for hypertensive emergencies. It lacks diuretic effect, apparently because it lacks a sulfonamide group.

BRITE-338733 is a novel inhibitor of ATPase. BRITE 338733 inhibits the expression of RecA in bacteria with IC50 value of 4.7 μM for the bacterial infections treatment.

KM 91104 is a cell permeable inhibitor of V-ATPase. KM91104 specifically targets the interaction between V-ATPase subunit A3 and subunit B2.

1. Acevaltrate (Acevaltratum) displays high cytotoxicity against GLC(4), a human small-cell lung cancer cell line, and against COLO 320, a human colorectal cancer cell line, with IC50 values of 1-6 uM.

Wilforine, a sesquiterpene pyridine alkaloid, is an important bioactive compound in T. wilfordii plants and is effective in treating idiopathic pulmonary fibrosis. Wilforine exhibits an anti-inflammatory effect, which might be mediated by the down-regulation of inflammatory factors TNF-α, IL-6, and NO. Additionally, it has insecticidal activity by inhibiting the Na+-K+-ATPase in the central nervous system.