ATPase

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V-ATPase F-ATPase SERCA RecA AAA ATPase family

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ATPase製品

All (53)
ATPase阻害剤 (46)
ATPase活性剤(6)
ATPase拮抗剤(1)
新製品

製品コード	製品名称	製品説明	文献中Selleckの製品使用例
S1413	Bafilomycin A1 (Baf-A1)	バフィロマイシン A1 (Bafilomycin A1(Baf-A1)) は液胞 H⁺-ATPase 阻害剤で、IC50 は 0.44 nM です。バフィロマイシン A1 は、オートファジー (autophagy) を阻害する一方で、アポトーシス (apoptosis) を誘導することがわかっています。	Nature, 2024, 626(8000):874-880 Nature, 2024, 626(8000):874-880 Cell, 2024, 187(21):6055-6070.e22
S1478	Oligomycin A	Oligomycin A (MCH 32), a dominant analog of the isomers, is an inhibitor of mitochondrial F1FO ATP synthase which inhibits oxidative phosphorylation and all the ATP-dependent processes occurring on the coupling membrane of mitochondria. It inhibits ATP synthase by blocking its proton channel (Fo subunit), which is necessary for oxidative phosphorylation of ADP to ATP. It also induces apoptosis in a variety of cell types.	Nat Commun, 2024, 15(1):686 Autophagy, 2024, 1-22. PLoS Biol, 2024, 22(8):e3002753
S7046	Brefeldin A (BFA)	Brefeldin A (BFA) is a lactone antibiotic and ATPase inhibitor for protein transport with IC50 of 0.2 μM in HCT 116 cells, induces cancer cell differentiation and apoptosis. It could also improve the HDR(homology-directed repair) efficiency and be an enhancer of CRISPR-mediated HDR. Brefeldin A is also an inhibitor of autophagy and mitophagy.	Nat Commun, 2024, 15(1):203 Cancer Commun (Lond), 2024, 10.1002/cac2.12583 Cell Rep Med, 2024, S2666-3791(24)00544-5
S1238	Tamoxifen	Tamoxifen is an orally active, selective estrogen receptor modulator (SERM) which exhibits both estrogenic agonist and antagonist effects. It blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells. Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity.	Nat Commun, 2024, 15(1):2377 Breast Cancer Res, 2024, 26(1):33 Toxics, 2024, 12(4)247
S8276	FCCP	FCCP (Trifluoromethoxy carbonylcyanide phenylhydrazone, Carbonyl cyanide 4-(trifluoromethoxy)phenylhydrazone) is a potent uncoupler of oxidative phosphorylation in mitochondria that disrupts ATP synthesis by transporting protons across cell membranes.	Autophagy, 2024, 1-22. Theranostics, 2024, 14(4):1561-1582 iScience, 2024, 27(3):109265
S7099	(-)-Blebbistatin	(-)-Blebbistatin ((S)-(-)-Blebbistatin) is a cell-permeable inhibitor for non muscle myosin II ATPase with IC50 of ~2 μM in cell-free assays, does not inhibit myosin light chain kinase, inhibits contraction of the cleavage furrow without disrupting mitosis or contractile ring assembly.	Nat Commun, 2024, 15(1):2093 EMBO J, 2024, Heliyon, 2024, 10(11):e31653
S8101	CB-5083	CB-5083 is a potent, selective, and orally bioavailable p97 AAA ATPase inhibitor with IC50 of 11 nM. Phase 1.	Cell, 2024, 187(20):5698-5718.e26 Nat Cell Biol, 2024, 10.1038/s41556-024-01401-2 J Clin Invest, 2024, e173861
S2623	Omecamtiv mecarbil (CK-1827452)	Omecamtiv mecarbil (CK-1827452) is a specific cardiac myosin activator and a clinical drug for left ventricular systolic heart failure. Phase 2.	Acta Neuropathol, 2024, 147(1):72 bioRxiv, 2024, 2024.05.14.594252 , 2023,
S7895	Thapsigargin	Thapsigargin is a potent, non-competitive inhibitor of the sarco/endoplasmic reticulum Ca²⁺ ATPase (SERCA) with IC50 of 0.353 nM or 0.448 nM for the carbachol-evoked [Ca2+]i-transients with or without a KCl-prestimulation. Thapsigargin induces cell apoptosis. Thapsigargin is extracted from a plant, Thapsia garganica.	Nat Commun, 2024, 15(1):2207 Nat Commun, 2024, 15(1):2371 Cancer Commun (Lond), 2024, 10.1002/cac2.12583
S4290	Digoxin	Digoxin is a classical Na,K-ATPase inhibitor, with selectivity for the α2β3 isoform over the common α1β1 isoform, used in the treatment of atrial fibrillation and heart failure.This product is a hazardous chemical (acute toxicity/flammable/skin corrosive). Please use it while wearing a protective face mask, gloves, and clothing.	Gastroenterology, 2024, S0016-5085(24)00062-3 J Immunother Cancer, 2024, 12(11)e009805 Pharmaceuticals (Basel), 2024, 17(9)1140
S2000	Sodium orthovanadate	Sodium orthovanadate is an alkaline phosphatase and (Na,K)-ATPase inhibitor with IC50 of 10 μM.	Cell Death Dis, 2022, 13(6):524 Toxicol Appl Pharmacol, 2022, 441:115988 PLoS Pathog, 2021, 17(7):e1009752
S2233	Esomeprazole sodium	Esomeprazole Sodium((S)-Omeprazole sodium, (-)-Omeprazole sodium) is a sodium salt of esomeprazole that is a potent proton pump inhibitor with an IC50 of 0.076 mg/kg.	J Pers Med, 2022, 12(2)258 Hum Cell, 2022, 10.1007/s13577-022-00671-y Hum Cell, 2021, 10.1007/s13577-021-00639-4
S7266	Golgicide A	Golgicide A is a potent and rapidly reversible GBF1 inhibitor.	J Exp Clin Cancer Res, 2024, 43(1):255 Autophagy, 2021, 1-13 Front Cell Dev Biol, 2021, 9:706768
S3019	Ciclopirox ethanolamine	Ciclopirox ethanolamine (Ciclopirox olamine, HOE 296,Ciclopiroxolamine) is a broad-spectrum antifungal agent working as an iron chelator.	Commun Biol, 2023, 6(1):402 Commun Biol, 2023, 6(1):402 J Clin Invest, 2022, 132(9)e152345
S2343	Phlorizin	Phlorizin (Phloridzin) is a dihydrochalcone found in the bark of pear (Pyrus communis), apple, cherry and other fruit trees. Phlorizin is a non-selective SGLT inhibitor with Ki of 300 nM and 39 nM for hSGLT1 and hSGLT2, respectively. Phlorizin is also a Na+/K+-ATPase inhibitor.	Mol Ther Methods Clin Dev, 2022, 24:11-19 J Ginseng Res, 2022, 46(5):700-709 J Med Virol, 2019, 91(8):1440-1447
S1389	Omeprazole	Omeprazole is a proton pump inhibitor that blocks H(+)-K(+)-ATPase, used to treat dyspepsia, peptic ulcer disease, gastroesophageal reflux disease, laryngopharyngeal reflux, and Zollinger–Ellison syndrome.	J Extracell Vesicles, 2024, 13(4):e12426 J Extracell Vesicles, 2024, 13(4):e12426 J Transl Med, 2024, 22(1):676
S2528	Ciclopirox	Ciclopirox(HOE 296b, Penlac) is a broad-spectrum antifungal agent working as an iron chelator.	Cell Death Dis, 2021, 12(12):1141 J Transl Med, 2021, 19(1):347 Int J Mol Sci, 2021, 22(15)8299
S5623	Bedaquiline	Bedaquiline (TMC-207, R207910), a diarylquinoline, binds to subunit c of mycobacterial ATP synthase and inhibits its activity. It is highly selective for mycobacterial ATP synthase enzyme compared to homologous eukaryotic enzyme (Selectivity Index >20 000).	Sci Rep, 2023, 13(1):3825 Microbiol Spectr, 2023, e0046523. Adv Healthc Mater, 2022, e2102117
S2105	Pantoprazole	Pantoprazole (SKF96022, BY-1023) is a proton pump inhibitor drug that inhibits gastric acid secretion. It works on gastric parietal cells to irreversibly inhibit (H+/K+)-ATPase function and suppress the production of gastric acid.	Med Oncol, 2024, 41(8):188 Int J Mol Sci, 2022, 23-158572 Eur J Drug Metab Pharmacokinet, 2022, 10.1007/s13318-022-00780-x
S1354	Lansoprazole	Lansoprazole (A-65006, AG-1749) is a proton-pump inhibitor (PPI) that binds covalently to parietal cell H(+),K(+)-ATPase. Lansoprazole prevents the stomach from producing gastric acid.	Front Cell Dev Biol, 2021, 9:655559 J Virol, 2021, JVI.00190-21 Front Microbiol, 2019, 10:2790
S7460	BTB06584	BTB06584 is an IF1-dependent, selective inhibitor of the mitochondrial F1 Fo-ATPase.	Int J Mol Sci, 2023, 24(15)12460 J Cell Physiol, 2018, 234(1):940-949 Oncotarget, 2017, 8(32):53602-53612
S3924	Ginsenoside Rb1	Ginsenoside Rb1 (Gypenoside Ⅲ) is a protopanaxadiol that has diverse in vitro and in vivo effects, including neuroprotective, anti-inflammatory, and anti-obesity actions. Ginsenoside Rb1, a main constituent of the root of Panax ginseng, inhibits Na+, K+-ATPase activity with IC50 of 6.3±1.0 μM. Ginsenoside also inhibits IRAK-1 activation and phosphorylation of NF-κB p65. Ginsenoside Rb1 reduces the expressions of TLR3, TLR4 and TRAF-6, and down-regulates the levels of TNF-α, IFN-β and iNOS.	J Biol Chem, 2024, 300(8):107542 J Ethnopharmacol, 2021, S0378-8741(21)00169-0 J Biol Chem, 2021, S0021-9258(21)00790-0
S8828	Gboxin	Gboxin is an inhibitor of oxidative phosphorylation in cancer cells. Gboxin inhibits the activity of F0F1 ATP synthase. It specifically inhibits the growth of primary mouse and human glioblastoma cells but not that of mouse embryonic fibroblasts or neonatal astrocytes.	Cell Rep, 2024, 43(10):114775 Mol Oncol, 2023, 17(9):1821-1843 Mol Oncol, 2023, 17(9):1821-1843
S4099	Dexlansoprazole	Dexlansoprazole (T 168390, TAK 390,(R)-Lansoprazole), the dextrorotatory enantiomer of lansoprazole, is a proton pump inhibitor (PPI) formulated to have dual delayed-release properties. Dexlansoprazole selectively suppresses gastric acid secretion by direct inhibition of the H(+),K(+)-ATPase proton pump in the gastric parietal cell.	J Immunother Cancer, 2024, 12(11)e009805 J Virol, 2021, JVI.00190-21 Front Microbiol, 2019, 10:2790
S6815	CDN1163	CDN1163 is a small molecular allosteric activator of the sarco/endoplasmic reticulum Ca2+-ATPase (SERCA) that improves Ca2+ homeostasis.	Cell Rep, 2024, 43(10):114784 J Clin Invest, 2022, 132(8)e149160 Front Pharmacol, 2022, 13:877175
S5608	Pantoprazole sodium hydrate	Pantoprazole (BY10232, SKF96022) sodium hydrate (Protonix) is a potent inhibitor of H+/K(+)-ATPase with IC50 of 6.8 μM.	Eur J Drug Metab Pharmacokinet, 2022, 10.1007/s13318-022-00780-x J Virol, 2021, JVI.00190-21
S3628	BHQ	BHQ (2,5-di-t-butyl-1,4-benzohydroquinone) is a potent and selective inhibitor of the sarco-endoplasmic reticulum Ca2+-ATPase (SERCA).	Diabetes, 2022, 71(8):1660-1678 Oncogene, 2021, 40(6):1128-1146
S4538	Pantoprazole sodium	Pantoprazole (SKF96022, BY-1023) is a proton pump inhibitor drug that inhibits gastric acid secretion. It works on gastric parietal cells to irreversibly inhibit (H+/K+)-ATPase function and suppress the production of gastric acid.	Eur J Drug Metab Pharmacokinet, 2022, 10.1007/s13318-022-00780-x J Virol, 2021, JVI.00190-21
S9181	Periplocin	Periplocin (Periplocoside), extracted from the traditional herbal medicine cortex periplocae, has cardiac and anticancer activity. Periplocin could significantly boost proliferation, migration and stimulate collagen production in fibroblast L929 cells, which is dependent on activation of Src/ERK and PI3K/Akt pathways mediated by Na/K-ATPase, and thus promoting wound healing.	Cancers (Basel), 2023, 15(5)1526 Cancers (Basel), 2023, 15(5)1526 J Oncol, 2022, 2022:8055004
S5502	Ilaprazole sodium	Ilaprazole (IY-81149) sodium is the sodium salt form of ilaprazole, which is a proton pump inhibitor. Ilaprazole sodium irreversibly inhibits H(+)/K(+)-ATPase in a dose-dependent manner with IC50 of 6 μM in rabbit parietal cell preparation.	J Virol, 2021, JVI.00190-21
S4166	Chlorpropamide	Chlorpropamide inhibits Na(+),K(+)-ATPase and stimulates a high affinity cyclic AMP-phosphodiesterase of isolated liver plasma membrane. Chlorpropamide is a sulfonylurea class drug for type 2 diabetes mellitus.	Nat Commun, 2017, 8(1):573
S3666	Ilaprazole	Ilaprazole (IY-81149) is a new proton pump inhibitor (PPI) used in the treatment of dyspepsia, peptic ulcer disease (PUD), gastroesophageal reflux disease (GORD/GERD) and duodenal ulcer. It inhibits H+/K+-ATPase with an IC50 of 6.0 μM.	Med Oncol, 2024, 41(8):188 J Virol, 2021, JVI.00190-21
S3577	Rhodamine 123	Rhodamine 123 (RH-123, R-22420) is a fluorescent cationic dye used to label mitochondria in living cells. Rhodamine 123 inhibits ADP-stimulated respiration of mitochondria with Ki = 12 μM and ATPase activity of inverted inner membrane vesicles with Ki of 126 μM and partially purified F1-ATPase with Ki of 177 μM.	Am J Transl Res, 2023, 15(6):4065-4078
S4212	Tenatoprazole	Tenatoprazole (TU-199,STU-Na) is a prodrug of the proton pump inhibitor (PPI) class, which inhibits proton transport with IC50 of 3.2 μM. Tenatoprazole labels only the gastric H(+),K(+)-ATPase alpha-subunit, approximately 2.6 nM/mg of tenatoprazole is bound to the H(+),K(+)-ATPase.	J Virol, 2021, JVI.00190-21
E1166	tetrathiomolybdate	Tetrathiomolybdate (TM) is used in the clinic for the treatment of Wilson’s disease by inducing dimerization of the metal-binding domain of the cellular copper efflux protein ATP7B (WLN4) through a unique sulfur-bridged Mo2S6O2 cluster.	J Exp Clin Cancer Res, 2024, 43(1):68 Cell Death Dis, 2024, 15(2):149 Am J Cancer Res, 2023, 13(11):5590-5609
S5058	Revaprazan Hydrochloride	Revaprazan Hydrochloride (YH1885) is a new reversible proton pump inhibitor with long-lasting acid-suppressive effects. Revaprazan Hydrochloride reversibly inhibits H(+)/K(+)-ATPase via binding to the K+-binding site of the pump.	ACS Infect Dis, 2021, 10.1021/acsinfecdis.0c00754
S5454	Saikosaponin D	Saikosaponin D, a calcium mobilizing agent (SERCA inhibitor), is a type of Saponin derivative, which is a component extracted from Bupleurum falactum. Saikosaponin D has anti-cancer activities.	Adv Healthc Mater, 2023, e2300591.
S1743	Esomeprazole magnesium	Esomeprazole Magnesium(NEXIUM) is a proton pump inhibitor to reduce gastric acid secretion through inhibition of H(+)/K(+)-ATPase in gastric parietal cells.
S2222	PF-3716556	PF 3716556 is a potent and selective P-CAB (potassium-competitive acid blocker), with pIC50 of 6.026 and 7.095 for the inhibition of porcine H⁺,K⁺-ATPase activity in ion-leaky and ion-tight assay, respectively, inhibits gastric acid secretion, displays no activity at Na⁺,K⁺-ATPase, used for the treatment of gastroesophageal reflux disease.
S3143	Pyruvic acid	Pyruvic acid (Acetylformic acid) is an important organic chemical intermediate that plays a role in cardiomyocyte pathophysiology and therapy. Pyruvic acid markedly increases the level of lactate dehydrogenase (LDH) and creatine kinase (CK) and reduces the level of Ca²⁺Mg²⁺-ATPase and Na⁺K⁺-ATPase.
E0244	Acevaltrate	Acevaltrate, an active component derived from the herbal plant Valeriana jatamansi Jones, is strikingly potent to induce GBM cell apoptosis. Acevaltrate inhibits the Na+/K+-ATPase activity in the rat kidney and brain hemispheres with IC50 of 22.8 μM and 42.3 μM, respectively.
S7821	Bufalin	Bufalin (BF) is a potent inhibitor of steroid receptor coactivator SRC-3, SRC-1 and Na+/K+-ATPase. Bufalin binds to the subunit α1, α2 and α3 of Na+/K+-ATPase with Kd of 42.5 nM, 45 nM and 40 nM, respectively. Bufalin is a major digoxin-like immunoreactive component isolated from the Chinese medicine Chan Su with anti-cancer activity.	Lipids Health Dis, 2024, 23(1):318 Acta Biochim Biophys Sin (Shanghai), 2024, 56(2):199-209 Drug Resist Updat, 2023, 71:101005
E1178	FHD-286	FHD-286 is a BRG1/BRM ATPase inhibitor for the treatment of BAF-related disorders such as acute myeloid leukemia.
E4087	Sodium oleate	Sodium oleate (Oleic acid sodium salt) is an abundant monounsaturated fatty acid sodium. It is a Na+/K+ ATPase activator and inhibits cancer cell growth and survival in low metastatic carcinoma cells, such as gastric carcinoma SGC7901 and breast carcinoma MCF-7 cell lines.
E0054	Tegoprazan	Tegoprazan (CJ-12420, IN-A001, K-CAB, LXI-15028, RQ-00000004) is a novel potent and highly selective inhibitor of gastric H+/K+-ATPase with IC50s ranging from 0.29 μM to 0.52 μM for porcine, canine, and human H+/K+-ATPases in vitro, respectively.	Sci Rep, 2024, 14(1):27173
S0161	ML367	ML367 is a potent, micromolar inhibitor of ATPase family AAA domain-containing protein 5 (ATAD5) stabilization. ML367 blocks DNA repair pathways and general DNA damage responses including RPA32-phosphorylation and CHK1-phosphorylation in response to UV irradiation.
E0680	Deslanoside	Deslanoside(Desacetyllanatoside C) is a cardenolide glycoside, has the effects of anti-arrhythmia and cardiotonic, also is used as an EC 3.6.3.9 (Na⁺/K⁺-transporting ATPase) inhibitor.
S0166	BRITE338733	BRITE 338733 is a novel ATPase inhibitor. BRITE 338733 inhibits the expression of RecA in bacteria with IC50 of 4.7 µM for the treatment of bacterial infections.
S6918	Oleandrin (PBI-05204)	Oleandrin (PBI-05204, Foliandrin, Neriolin, Neriostene, Folinerin, Corrigen, Neriol) is an inhibitor of Na+/K+-ATPase with IC50 of 0.62 μM. Oleandrin induces apoptosis and reduces migration of human glioma cells in vitro.
S4707	Oleic Acid	Oleic acid (Oleate, 9-Octadecenoic Acid, Elaidoic acid) is a fatty acid that occurs naturally in various animal and vegetable fats and oils. It is used commercially in the preparation of oleates and lotions, and as a pharmaceutical solvent. Oleic Acid can be used to induce animal models of Renal Failure.	Cancer Lett, 2024, 597:217068 Cell Rep Med, 2023, 4(10):101234 Antioxid Redox Signal, 2023, 39(1-3):166-185.
E0483	Calmidazolium chloride	Calmidazolium chloride (R 24571) is a calmodulin (CaM) antagonist, antagonizing CaM-stimulated fraction of rat brain phosphodiesterase and CaM-induced activation of erythrocyte Ca²⁺-transporting ATPase with IC50s of 0.15 and 0.35 μM, respectively, also shows a CaM-binding Kd value of 3 nM.
S0219	ML241 hydrochloride	ML241 hydrochloride is a potent and selective inhibitor of p97 with IC50 of 0.11 μM and 3.5 μM for p97 ATPase and Ub^G76V–GFP, respectively.
S0856	KM91104	KM 91104 is a cell-permeable inhibitor of V-ATPase that specifically targets the interaction between V-ATPase subunit a3 and subunit B2.
S1413	Bafilomycin A1 (Baf-A1)	バフィロマイシン A1 (Bafilomycin A1(Baf-A1)) は液胞 H⁺-ATPase 阻害剤で、IC50 は 0.44 nM です。バフィロマイシン A1 は、オートファジー (autophagy) を阻害する一方で、アポトーシス (apoptosis) を誘導することがわかっています。	Nature, 2024, 626(8000):874-880 Nature, 2024, 626(8000):874-880 Cell, 2024, 187(21):6055-6070.e22
S1478	Oligomycin A	Oligomycin A (MCH 32), a dominant analog of the isomers, is an inhibitor of mitochondrial F1FO ATP synthase which inhibits oxidative phosphorylation and all the ATP-dependent processes occurring on the coupling membrane of mitochondria. It inhibits ATP synthase by blocking its proton channel (Fo subunit), which is necessary for oxidative phosphorylation of ADP to ATP. It also induces apoptosis in a variety of cell types.	Nat Commun, 2024, 15(1):686 Autophagy, 2024, 1-22. PLoS Biol, 2024, 22(8):e3002753
S7046	Brefeldin A (BFA)	Brefeldin A (BFA) is a lactone antibiotic and ATPase inhibitor for protein transport with IC50 of 0.2 μM in HCT 116 cells, induces cancer cell differentiation and apoptosis. It could also improve the HDR(homology-directed repair) efficiency and be an enhancer of CRISPR-mediated HDR. Brefeldin A is also an inhibitor of autophagy and mitophagy.	Nat Commun, 2024, 15(1):203 Cancer Commun (Lond), 2024, 10.1002/cac2.12583 Cell Rep Med, 2024, S2666-3791(24)00544-5
S8276	FCCP	FCCP (Trifluoromethoxy carbonylcyanide phenylhydrazone, Carbonyl cyanide 4-(trifluoromethoxy)phenylhydrazone) is a potent uncoupler of oxidative phosphorylation in mitochondria that disrupts ATP synthesis by transporting protons across cell membranes.	Autophagy, 2024, 1-22. Theranostics, 2024, 14(4):1561-1582 iScience, 2024, 27(3):109265
S7099	(-)-Blebbistatin	(-)-Blebbistatin ((S)-(-)-Blebbistatin) is a cell-permeable inhibitor for non muscle myosin II ATPase with IC50 of ~2 μM in cell-free assays, does not inhibit myosin light chain kinase, inhibits contraction of the cleavage furrow without disrupting mitosis or contractile ring assembly.	Nat Commun, 2024, 15(1):2093 EMBO J, 2024, Heliyon, 2024, 10(11):e31653
S8101	CB-5083	CB-5083 is a potent, selective, and orally bioavailable p97 AAA ATPase inhibitor with IC50 of 11 nM. Phase 1.	Cell, 2024, 187(20):5698-5718.e26 Nat Cell Biol, 2024, 10.1038/s41556-024-01401-2 J Clin Invest, 2024, e173861
S7895	Thapsigargin	Thapsigargin is a potent, non-competitive inhibitor of the sarco/endoplasmic reticulum Ca²⁺ ATPase (SERCA) with IC50 of 0.353 nM or 0.448 nM for the carbachol-evoked [Ca2+]i-transients with or without a KCl-prestimulation. Thapsigargin induces cell apoptosis. Thapsigargin is extracted from a plant, Thapsia garganica.	Nat Commun, 2024, 15(1):2207 Nat Commun, 2024, 15(1):2371 Cancer Commun (Lond), 2024, 10.1002/cac2.12583
S4290	Digoxin	Digoxin is a classical Na,K-ATPase inhibitor, with selectivity for the α2β3 isoform over the common α1β1 isoform, used in the treatment of atrial fibrillation and heart failure.This product is a hazardous chemical (acute toxicity/flammable/skin corrosive). Please use it while wearing a protective face mask, gloves, and clothing.	Gastroenterology, 2024, S0016-5085(24)00062-3 J Immunother Cancer, 2024, 12(11)e009805 Pharmaceuticals (Basel), 2024, 17(9)1140
S2000	Sodium orthovanadate	Sodium orthovanadate is an alkaline phosphatase and (Na,K)-ATPase inhibitor with IC50 of 10 μM.	Cell Death Dis, 2022, 13(6):524 Toxicol Appl Pharmacol, 2022, 441:115988 PLoS Pathog, 2021, 17(7):e1009752
S2233	Esomeprazole sodium	Esomeprazole Sodium((S)-Omeprazole sodium, (-)-Omeprazole sodium) is a sodium salt of esomeprazole that is a potent proton pump inhibitor with an IC50 of 0.076 mg/kg.	J Pers Med, 2022, 12(2)258 Hum Cell, 2022, 10.1007/s13577-022-00671-y Hum Cell, 2021, 10.1007/s13577-021-00639-4
S7266	Golgicide A	Golgicide A is a potent and rapidly reversible GBF1 inhibitor.	J Exp Clin Cancer Res, 2024, 43(1):255 Autophagy, 2021, 1-13 Front Cell Dev Biol, 2021, 9:706768
S3019	Ciclopirox ethanolamine	Ciclopirox ethanolamine (Ciclopirox olamine, HOE 296,Ciclopiroxolamine) is a broad-spectrum antifungal agent working as an iron chelator.	Commun Biol, 2023, 6(1):402 Commun Biol, 2023, 6(1):402 J Clin Invest, 2022, 132(9)e152345
S2343	Phlorizin	Phlorizin (Phloridzin) is a dihydrochalcone found in the bark of pear (Pyrus communis), apple, cherry and other fruit trees. Phlorizin is a non-selective SGLT inhibitor with Ki of 300 nM and 39 nM for hSGLT1 and hSGLT2, respectively. Phlorizin is also a Na+/K+-ATPase inhibitor.	Mol Ther Methods Clin Dev, 2022, 24:11-19 J Ginseng Res, 2022, 46(5):700-709 J Med Virol, 2019, 91(8):1440-1447
S1389	Omeprazole	Omeprazole is a proton pump inhibitor that blocks H(+)-K(+)-ATPase, used to treat dyspepsia, peptic ulcer disease, gastroesophageal reflux disease, laryngopharyngeal reflux, and Zollinger–Ellison syndrome.	J Extracell Vesicles, 2024, 13(4):e12426 J Extracell Vesicles, 2024, 13(4):e12426 J Transl Med, 2024, 22(1):676
S2528	Ciclopirox	Ciclopirox(HOE 296b, Penlac) is a broad-spectrum antifungal agent working as an iron chelator.	Cell Death Dis, 2021, 12(12):1141 J Transl Med, 2021, 19(1):347 Int J Mol Sci, 2021, 22(15)8299
S5623	Bedaquiline	Bedaquiline (TMC-207, R207910), a diarylquinoline, binds to subunit c of mycobacterial ATP synthase and inhibits its activity. It is highly selective for mycobacterial ATP synthase enzyme compared to homologous eukaryotic enzyme (Selectivity Index >20 000).	Sci Rep, 2023, 13(1):3825 Microbiol Spectr, 2023, e0046523. Adv Healthc Mater, 2022, e2102117
S2105	Pantoprazole	Pantoprazole (SKF96022, BY-1023) is a proton pump inhibitor drug that inhibits gastric acid secretion. It works on gastric parietal cells to irreversibly inhibit (H+/K+)-ATPase function and suppress the production of gastric acid.	Med Oncol, 2024, 41(8):188 Int J Mol Sci, 2022, 23-158572 Eur J Drug Metab Pharmacokinet, 2022, 10.1007/s13318-022-00780-x
S1354	Lansoprazole	Lansoprazole (A-65006, AG-1749) is a proton-pump inhibitor (PPI) that binds covalently to parietal cell H(+),K(+)-ATPase. Lansoprazole prevents the stomach from producing gastric acid.	Front Cell Dev Biol, 2021, 9:655559 J Virol, 2021, JVI.00190-21 Front Microbiol, 2019, 10:2790
S7460	BTB06584	BTB06584 is an IF1-dependent, selective inhibitor of the mitochondrial F1 Fo-ATPase.	Int J Mol Sci, 2023, 24(15)12460 J Cell Physiol, 2018, 234(1):940-949 Oncotarget, 2017, 8(32):53602-53612
S3924	Ginsenoside Rb1	Ginsenoside Rb1 (Gypenoside Ⅲ) is a protopanaxadiol that has diverse in vitro and in vivo effects, including neuroprotective, anti-inflammatory, and anti-obesity actions. Ginsenoside Rb1, a main constituent of the root of Panax ginseng, inhibits Na+, K+-ATPase activity with IC50 of 6.3±1.0 μM. Ginsenoside also inhibits IRAK-1 activation and phosphorylation of NF-κB p65. Ginsenoside Rb1 reduces the expressions of TLR3, TLR4 and TRAF-6, and down-regulates the levels of TNF-α, IFN-β and iNOS.	J Biol Chem, 2024, 300(8):107542 J Ethnopharmacol, 2021, S0378-8741(21)00169-0 J Biol Chem, 2021, S0021-9258(21)00790-0
S8828	Gboxin	Gboxin is an inhibitor of oxidative phosphorylation in cancer cells. Gboxin inhibits the activity of F0F1 ATP synthase. It specifically inhibits the growth of primary mouse and human glioblastoma cells but not that of mouse embryonic fibroblasts or neonatal astrocytes.	Cell Rep, 2024, 43(10):114775 Mol Oncol, 2023, 17(9):1821-1843 Mol Oncol, 2023, 17(9):1821-1843
S4099	Dexlansoprazole	Dexlansoprazole (T 168390, TAK 390,(R)-Lansoprazole), the dextrorotatory enantiomer of lansoprazole, is a proton pump inhibitor (PPI) formulated to have dual delayed-release properties. Dexlansoprazole selectively suppresses gastric acid secretion by direct inhibition of the H(+),K(+)-ATPase proton pump in the gastric parietal cell.	J Immunother Cancer, 2024, 12(11)e009805 J Virol, 2021, JVI.00190-21 Front Microbiol, 2019, 10:2790
S5608	Pantoprazole sodium hydrate	Pantoprazole (BY10232, SKF96022) sodium hydrate (Protonix) is a potent inhibitor of H+/K(+)-ATPase with IC50 of 6.8 μM.	Eur J Drug Metab Pharmacokinet, 2022, 10.1007/s13318-022-00780-x J Virol, 2021, JVI.00190-21
S3628	BHQ	BHQ (2,5-di-t-butyl-1,4-benzohydroquinone) is a potent and selective inhibitor of the sarco-endoplasmic reticulum Ca2+-ATPase (SERCA).	Diabetes, 2022, 71(8):1660-1678 Oncogene, 2021, 40(6):1128-1146
S4538	Pantoprazole sodium	Pantoprazole (SKF96022, BY-1023) is a proton pump inhibitor drug that inhibits gastric acid secretion. It works on gastric parietal cells to irreversibly inhibit (H+/K+)-ATPase function and suppress the production of gastric acid.	Eur J Drug Metab Pharmacokinet, 2022, 10.1007/s13318-022-00780-x J Virol, 2021, JVI.00190-21
S5502	Ilaprazole sodium	Ilaprazole (IY-81149) sodium is the sodium salt form of ilaprazole, which is a proton pump inhibitor. Ilaprazole sodium irreversibly inhibits H(+)/K(+)-ATPase in a dose-dependent manner with IC50 of 6 μM in rabbit parietal cell preparation.	J Virol, 2021, JVI.00190-21
S4166	Chlorpropamide	Chlorpropamide inhibits Na(+),K(+)-ATPase and stimulates a high affinity cyclic AMP-phosphodiesterase of isolated liver plasma membrane. Chlorpropamide is a sulfonylurea class drug for type 2 diabetes mellitus.	Nat Commun, 2017, 8(1):573
S3666	Ilaprazole	Ilaprazole (IY-81149) is a new proton pump inhibitor (PPI) used in the treatment of dyspepsia, peptic ulcer disease (PUD), gastroesophageal reflux disease (GORD/GERD) and duodenal ulcer. It inhibits H+/K+-ATPase with an IC50 of 6.0 μM.	Med Oncol, 2024, 41(8):188 J Virol, 2021, JVI.00190-21
S3577	Rhodamine 123	Rhodamine 123 (RH-123, R-22420) is a fluorescent cationic dye used to label mitochondria in living cells. Rhodamine 123 inhibits ADP-stimulated respiration of mitochondria with Ki = 12 μM and ATPase activity of inverted inner membrane vesicles with Ki of 126 μM and partially purified F1-ATPase with Ki of 177 μM.	Am J Transl Res, 2023, 15(6):4065-4078
S4212	Tenatoprazole	Tenatoprazole (TU-199,STU-Na) is a prodrug of the proton pump inhibitor (PPI) class, which inhibits proton transport with IC50 of 3.2 μM. Tenatoprazole labels only the gastric H(+),K(+)-ATPase alpha-subunit, approximately 2.6 nM/mg of tenatoprazole is bound to the H(+),K(+)-ATPase.	J Virol, 2021, JVI.00190-21
E1166	tetrathiomolybdate	Tetrathiomolybdate (TM) is used in the clinic for the treatment of Wilson’s disease by inducing dimerization of the metal-binding domain of the cellular copper efflux protein ATP7B (WLN4) through a unique sulfur-bridged Mo2S6O2 cluster.	J Exp Clin Cancer Res, 2024, 43(1):68 Cell Death Dis, 2024, 15(2):149 Am J Cancer Res, 2023, 13(11):5590-5609
S5058	Revaprazan Hydrochloride	Revaprazan Hydrochloride (YH1885) is a new reversible proton pump inhibitor with long-lasting acid-suppressive effects. Revaprazan Hydrochloride reversibly inhibits H(+)/K(+)-ATPase via binding to the K+-binding site of the pump.	ACS Infect Dis, 2021, 10.1021/acsinfecdis.0c00754
S5454	Saikosaponin D	Saikosaponin D, a calcium mobilizing agent (SERCA inhibitor), is a type of Saponin derivative, which is a component extracted from Bupleurum falactum. Saikosaponin D has anti-cancer activities.	Adv Healthc Mater, 2023, e2300591.
S1743	Esomeprazole magnesium	Esomeprazole Magnesium(NEXIUM) is a proton pump inhibitor to reduce gastric acid secretion through inhibition of H(+)/K(+)-ATPase in gastric parietal cells.
S2222	PF-3716556	PF 3716556 is a potent and selective P-CAB (potassium-competitive acid blocker), with pIC50 of 6.026 and 7.095 for the inhibition of porcine H⁺,K⁺-ATPase activity in ion-leaky and ion-tight assay, respectively, inhibits gastric acid secretion, displays no activity at Na⁺,K⁺-ATPase, used for the treatment of gastroesophageal reflux disease.
S3143	Pyruvic acid	Pyruvic acid (Acetylformic acid) is an important organic chemical intermediate that plays a role in cardiomyocyte pathophysiology and therapy. Pyruvic acid markedly increases the level of lactate dehydrogenase (LDH) and creatine kinase (CK) and reduces the level of Ca²⁺Mg²⁺-ATPase and Na⁺K⁺-ATPase.
E0244	Acevaltrate	Acevaltrate, an active component derived from the herbal plant Valeriana jatamansi Jones, is strikingly potent to induce GBM cell apoptosis. Acevaltrate inhibits the Na+/K+-ATPase activity in the rat kidney and brain hemispheres with IC50 of 22.8 μM and 42.3 μM, respectively.
S7821	Bufalin	Bufalin (BF) is a potent inhibitor of steroid receptor coactivator SRC-3, SRC-1 and Na+/K+-ATPase. Bufalin binds to the subunit α1, α2 and α3 of Na+/K+-ATPase with Kd of 42.5 nM, 45 nM and 40 nM, respectively. Bufalin is a major digoxin-like immunoreactive component isolated from the Chinese medicine Chan Su with anti-cancer activity.	Lipids Health Dis, 2024, 23(1):318 Acta Biochim Biophys Sin (Shanghai), 2024, 56(2):199-209 Drug Resist Updat, 2023, 71:101005
E1178	FHD-286	FHD-286 is a BRG1/BRM ATPase inhibitor for the treatment of BAF-related disorders such as acute myeloid leukemia.
E0054	Tegoprazan	Tegoprazan (CJ-12420, IN-A001, K-CAB, LXI-15028, RQ-00000004) is a novel potent and highly selective inhibitor of gastric H+/K+-ATPase with IC50s ranging from 0.29 μM to 0.52 μM for porcine, canine, and human H+/K+-ATPases in vitro, respectively.	Sci Rep, 2024, 14(1):27173
S0161	ML367	ML367 is a potent, micromolar inhibitor of ATPase family AAA domain-containing protein 5 (ATAD5) stabilization. ML367 blocks DNA repair pathways and general DNA damage responses including RPA32-phosphorylation and CHK1-phosphorylation in response to UV irradiation.
E0680	Deslanoside	Deslanoside(Desacetyllanatoside C) is a cardenolide glycoside, has the effects of anti-arrhythmia and cardiotonic, also is used as an EC 3.6.3.9 (Na⁺/K⁺-transporting ATPase) inhibitor.
S0166	BRITE338733	BRITE 338733 is a novel ATPase inhibitor. BRITE 338733 inhibits the expression of RecA in bacteria with IC50 of 4.7 µM for the treatment of bacterial infections.
S6918	Oleandrin (PBI-05204)	Oleandrin (PBI-05204, Foliandrin, Neriolin, Neriostene, Folinerin, Corrigen, Neriol) is an inhibitor of Na+/K+-ATPase with IC50 of 0.62 μM. Oleandrin induces apoptosis and reduces migration of human glioma cells in vitro.
S0219	ML241 hydrochloride	ML241 hydrochloride is a potent and selective inhibitor of p97 with IC50 of 0.11 μM and 3.5 μM for p97 ATPase and Ub^G76V–GFP, respectively.
S0856	KM91104	KM 91104 is a cell-permeable inhibitor of V-ATPase that specifically targets the interaction between V-ATPase subunit a3 and subunit B2.
S1238	Tamoxifen	Tamoxifen is an orally active, selective estrogen receptor modulator (SERM) which exhibits both estrogenic agonist and antagonist effects. It blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells. Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity.	Nat Commun, 2024, 15(1):2377 Breast Cancer Res, 2024, 26(1):33 Toxics, 2024, 12(4)247
S2623	Omecamtiv mecarbil (CK-1827452)	Omecamtiv mecarbil (CK-1827452) is a specific cardiac myosin activator and a clinical drug for left ventricular systolic heart failure. Phase 2.	Acta Neuropathol, 2024, 147(1):72 bioRxiv, 2024, 2024.05.14.594252 , 2023,
S6815	CDN1163	CDN1163 is a small molecular allosteric activator of the sarco/endoplasmic reticulum Ca2+-ATPase (SERCA) that improves Ca2+ homeostasis.	Cell Rep, 2024, 43(10):114784 J Clin Invest, 2022, 132(8)e149160 Front Pharmacol, 2022, 13:877175
S9181	Periplocin	Periplocin (Periplocoside), extracted from the traditional herbal medicine cortex periplocae, has cardiac and anticancer activity. Periplocin could significantly boost proliferation, migration and stimulate collagen production in fibroblast L929 cells, which is dependent on activation of Src/ERK and PI3K/Akt pathways mediated by Na/K-ATPase, and thus promoting wound healing.	Cancers (Basel), 2023, 15(5)1526 Cancers (Basel), 2023, 15(5)1526 J Oncol, 2022, 2022:8055004
E4087	Sodium oleate	Sodium oleate (Oleic acid sodium salt) is an abundant monounsaturated fatty acid sodium. It is a Na+/K+ ATPase activator and inhibits cancer cell growth and survival in low metastatic carcinoma cells, such as gastric carcinoma SGC7901 and breast carcinoma MCF-7 cell lines.
S4707	Oleic Acid	Oleic acid (Oleate, 9-Octadecenoic Acid, Elaidoic acid) is a fatty acid that occurs naturally in various animal and vegetable fats and oils. It is used commercially in the preparation of oleates and lotions, and as a pharmaceutical solvent. Oleic Acid can be used to induce animal models of Renal Failure.	Cancer Lett, 2024, 597:217068 Cell Rep Med, 2023, 4(10):101234 Antioxid Redox Signal, 2023, 39(1-3):166-185.
E0483	Calmidazolium chloride	Calmidazolium chloride (R 24571) is a calmodulin (CaM) antagonist, antagonizing CaM-stimulated fraction of rat brain phosphodiesterase and CaM-induced activation of erythrocyte Ca²⁺-transporting ATPase with IC50s of 0.15 and 0.35 μM, respectively, also shows a CaM-binding Kd value of 3 nM.

ATPase阻害剤の選択性比較