ATPase

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ATPase製品

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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
Nat Commun, 2024, 15(1):631
Nat Commun, 2024, 15(1):1669
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
iScience, 2024, 27(3):109119
Cell Metab, 2023, 35(10):1767-1781.e6
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
Commun Biol, 2024, 7(1):161
Cancer Immunol Immunother, 2024, 73(1):7
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, 2023, 10.1038/s41467-023-39059-3
Nat Commun, 2023, 14(1):5242
Nat Commun, 2023, 14(1):3469
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.
Theranostics, 2024, 14(4):1561-1582
bioRxiv, 2024, 2024.02.06.579103
Cell Rep, 2023, 42(7):112731
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.
Cell, 2023, 186(14):3013-3032.e22
Elife, 2023, 12e83602
Acta Physiol (Oxf), 2023, e14004.
S8101 CB-5083 CB-5083 is a potent, selective, and orally bioavailable p97 AAA ATPase inhibitor with IC50 of 11 nM. Phase 1.
Cell Rep, 2024, 43(2):113769
Cell Rep, 2023, 42(11):113318
Elife, 2023, 12e92409
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.
Commun Biol, 2022, 5(1):1266
Naunyn Schmiedebergs Arch Pharmacol, 2022, 10.1007/s00210-022-02333-0
Elife, 2021, 10e63691
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.
EMBO J, 2023, e113118.
J Exp Clin Cancer Res, 2023, 42(1):238
Cell Rep, 2023, 10.1016/j.celrep.2023.113352
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.
Autophagy, 2021, 1-13
Front Cell Dev Biol, 2021, 9:706768
Nature, 2019, 567(7747):262-266
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
J Clin Invest, 2022, 132(9)e152345
Redox Biol, 2022, 56:102451
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.
Theranostics, 2021, 11(5):2364-2380
Theranostics, 2021, 11(5):2364-2380
J Virol, 2021, JVI.00190-21
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.
Cell Rep Med, 2023, 4(10):101234
Antioxid Redox Signal, 2023, 39(1-3):166-185.
J Transl Med, 2022, 20(1):222
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
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.
Drug Resist Updat, 2023, 71:101005
J Transl Med, 2023, 21(1):900
Biol Direct, 2023, 18(1):37
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.
Int J Mol Sci, 2022, 23-158572
Eur J Drug Metab Pharmacokinet, 2022, 10.1007/s13318-022-00780-x
J Virol, 2021, JVI.00190-21
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 Ethnopharmacol, 2021, S0378-8741(21)00169-0
J Biol Chem, 2021, S0021-9258(21)00790-0
Mol Immunol, 2021, 139:140-152
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.
Mol Oncol, 2023, 17(9):1821-1843
Mol Oncol, 2023, 17(9):1821-1843
EMBO Mol Med, 2022, 14(12):e16082
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 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.
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
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.
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.
Cell Death Dis, 2024, 15(2):149
Am J Cancer Res, 2023, 13(11):5590-5609
Front Cell Dev Biol, 2022, 10:996307
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.
E1178 FHD-286 FHD-286 is a BRG1/BRM ATPase inhibitor for the treatment of BAF-related disorders such as acute myeloid leukemia.
E4087New 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.
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.
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 UbG76V–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
Nat Commun, 2024, 15(1):631
Nat Commun, 2024, 15(1):1669
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
iScience, 2024, 27(3):109119
Cell Metab, 2023, 35(10):1767-1781.e6
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
Commun Biol, 2024, 7(1):161
Cancer Immunol Immunother, 2024, 73(1):7
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.
Theranostics, 2024, 14(4):1561-1582
bioRxiv, 2024, 2024.02.06.579103
Cell Rep, 2023, 42(7):112731
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.
Cell, 2023, 186(14):3013-3032.e22
Elife, 2023, 12e83602
Acta Physiol (Oxf), 2023, e14004.
S8101 CB-5083 CB-5083 is a potent, selective, and orally bioavailable p97 AAA ATPase inhibitor with IC50 of 11 nM. Phase 1.
Cell Rep, 2024, 43(2):113769
Cell Rep, 2023, 42(11):113318
Elife, 2023, 12e92409
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.
EMBO J, 2023, e113118.
J Exp Clin Cancer Res, 2023, 42(1):238
Cell Rep, 2023, 10.1016/j.celrep.2023.113352
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.
Autophagy, 2021, 1-13
Front Cell Dev Biol, 2021, 9:706768
Nature, 2019, 567(7747):262-266
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
J Clin Invest, 2022, 132(9)e152345
Redox Biol, 2022, 56:102451
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.
Theranostics, 2021, 11(5):2364-2380
Theranostics, 2021, 11(5):2364-2380
J Virol, 2021, JVI.00190-21
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
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.
Drug Resist Updat, 2023, 71:101005
J Transl Med, 2023, 21(1):900
Biol Direct, 2023, 18(1):37
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.
Int J Mol Sci, 2022, 23-158572
Eur J Drug Metab Pharmacokinet, 2022, 10.1007/s13318-022-00780-x
J Virol, 2021, JVI.00190-21
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 Ethnopharmacol, 2021, S0378-8741(21)00169-0
J Biol Chem, 2021, S0021-9258(21)00790-0
Mol Immunol, 2021, 139:140-152
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.
Mol Oncol, 2023, 17(9):1821-1843
Mol Oncol, 2023, 17(9):1821-1843
EMBO Mol Med, 2022, 14(12):e16082
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 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.
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.
Cell Death Dis, 2024, 15(2):149
Am J Cancer Res, 2023, 13(11):5590-5609
Front Cell Dev Biol, 2022, 10:996307
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.
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.
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 UbG76V–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, 2023, 10.1038/s41467-023-39059-3
Nat Commun, 2023, 14(1):5242
Nat Commun, 2023, 14(1):3469
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.
Commun Biol, 2022, 5(1):1266
Naunyn Schmiedebergs Arch Pharmacol, 2022, 10.1007/s00210-022-02333-0
Elife, 2021, 10e63691
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.
Cell Rep Med, 2023, 4(10):101234
Antioxid Redox Signal, 2023, 39(1-3):166-185.
J Transl Med, 2022, 20(1):222
S6815 CDN1163 CDN1163 is a small molecular allosteric activator of the sarco/endoplasmic reticulum Ca2+-ATPase (SERCA) that improves Ca2+ homeostasis.
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
J Oncol, 2022, 2022:8055004
E4087New 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.
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.
E4087New 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.

ATPase阻害剤の選択性比較

Tags: ATPase inhibition | ATPase pump | ATPase activity | ATPase assay | sodium potassium ATPase pump | Na K-ATPase pump | Na K-ATPase activity | mitochondrial ATPase | Ca-ATPase pump | Na K-ATPase inhibition | myosin ATPase activity | H-ATPase pump | ATPase phosphorylation | ATPase assay protocol | HK-ATPase pump | Ca-ATPase activity | V-ATPase pump | sodium potassium ATPase activity | actomyosin ATPase activity | P-type ATPase pump