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ATPase Signaling Pathway Map

ATPase Signaling Pathways

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Catalog No. Product Name Information Product Use Citations Product Validations
E0054New 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.
E0244New 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.
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.
S0166 BRITE338733 BRITE-338733 is a potent RecA (a DNA-dependent ATPase) inhibitor with IC50 of 4.7 µM.
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.
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
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
J Virol, 2021, JVI.00190-21
Biosci Rep, 2021, BSR20200842
S1413 Bafilomycin A1 (Baf-A1) Bafilomycin A1(Baf-A1) is a vacuolar H+-ATPase inhibitor with IC50 of 0.44 nM. Bafilomycin A1 is found to inhibit autophagy while induces apoptosis.
Nature, 2022, 603(7899):159-165
Cell Res, 2022, 32(2):119-138
Autophagy, 2022, 1-20
S1478 Oligomycin A 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.
Sci Signal, 2022, 15(721):eabi9983
J Agric Food Chem, 2022, 70(9):2898-2910
Nat Commun, 2021, 12(1):5203
S1743 NEXIUM (esomeprazole magnesium) Esomeprazole Magnesium is a proton pump inhibitor to reduce gastric acid secretion through inhibition of H(+)/K(+)-ATPase in gastric parietal cells.
S2000 Sodium orthovanadate Sodium orthovanadate is an alkaline phosphatase and (Na,K)-ATPase inhibitor with IC50 of 10 μM.
Toxicol Appl Pharmacol, 2022, 441:115988
PLoS Pathog, 2021, 17(7):e1009752
Anal Chim Acta, 2021, 1143:144-156
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.
J Virol, 2021, JVI.00190-21
Front Microbiol, 2019, 10:2790
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.
S2233 Esomeprazole sodium Esomeprazole Sodium is a sodium salt of esomeprazole that is a potent proton pump inhibitor with an IC50 of 0.076 mg/kg.
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Hum Cell, 2021, 34(6):1911-1918
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
Int J Biol Sci, 2019, 15(11):2497-2508
Am J Physiol Renal Physiol, 2019, 316(5):F1078-F1089
S2528 Ciclopirox Ciclopirox is a broad-spectrum antifungal agent working as an iron chelator.
Cell Death Dis, 2021, 12(12):1141
Int J Mol Sci, 2021, 22(15)8299
J Transl Med, 2021, 19(1):347
S3019 Ciclopirox ethanolamine Ciclopirox ethanolamine (Ciclopirox olamine, HOE 296) is a broad-spectrum antifungal agent working as an iron chelator.
Front Cell Dev Biol, 2021, 9:719187
ACS Omega, 2021, 6(12):8477-8487
bioRxiv, 2019, 10.1101/748129
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.

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.
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).
Oncogene, 2021, 40(6):1128-1146
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
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, 2021, S0021-9258(21)00790-0
Mol Immunol, 2021, 139:140-152
J Ethnopharmacol, 2021, S0378-8741(21)00169-0
S4016 Ouabain Ouabain (NSC 25485) is a selective Na+/K+, -ATPase inhibitor, binds to α2 /α3 subunit with Ki of 41 nM/15 nM.
Nat Methods, 2021, 18(1):84-91
Mol Oncol, 2020, 10.1002/1878-0261.12853
bioRxiv, 2020, 2020/9/20.4.7.30734
S4099 Dexlansoprazole Dexlansoprazole (T 168390, TAK 390), 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
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
S4212 Tenatoprazole Tenatoprazole (TU-199) 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
S4290 Digoxin (NSC 95100) Digoxin (NSC 95100) 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.
J Cell Mol Med, 2021, 10.1111/jcmm.16272
J Cell Mol Med, 2021, 25(3):1700-1711
PLoS Pathog, 2020, 16;16(3):e1008341
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.
J Virol, 2021, JVI.00190-21
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.
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
S5608 Pantoprazole sodium hydrate Pantoprazole (BY10232, SKF96022) sodium hydrate (Protonix) is a potent inhibitor of H+/K(+)-ATPase with IC50 of 6.8 μM.
J Virol, 2021, JVI.00190-21
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).
Adv Healthc Mater, 2022, e2102117
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.
S7046 Brefeldin A Brefeldin A 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.
Cell Mol Immunol, 2022, 10.1038/s41423-022-00841-w
PLoS One, 2022, 17(3):e0265805
Nat Cell Biol, 2021, 10.1038/s41556-021-00704-y
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, 2021, 12(1):5315
Biomaterials, 2021, 279:121235
Acta Biomater, 2021, S1742-7061(21)00586-9
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
S7460 BTB06584 BTB06584 is an IF1-dependent, selective inhibitor of the mitochondrial F1 Fo-ATPase.
J Cell Physiol, 2018, 234(1):940-949
Oncotarget, 2017, 8(32):53602-53612
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.
Front Oncol, 2021, 11:743824
bioRxiv, 2020, 2020/9/20.4.7.30734
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.
Cell Res, 2021, 10.1038/s41422-021-00565-y
Sci Adv, 2021, 7(3)eabc6364
Autophagy, 2021, 1-16
S8101 CB-5083 CB-5083 is a potent, selective, and orally bioavailable p97 AAA ATPase inhibitor with IC50 of 11 nM. Phase 1.
Cell Death Dis, 2022, 13(3):203
Nat Commun, 2021, 12(1):713
J Cell Biol, 2021, 220(8)e202009147
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.
Exp Mol Med, 2022, 10.1038/s12276-022-00745-9
Sci Signal, 2022, 15(721):eabi9983
Cell Death Discov, 2022, 8(1):69
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.
A5267 MSH6 Rabbit Recombinant mAb MSH6 Rabbit Recombinant mAb detects endogenous level of MSH6.
A5286 ATPB Rabbit Recombinant mAb ATPB Rabbit Recombinant mAb detects endogenous level of total ATPB.
S1238 Tamoxifen (ICI 46474) Tamoxifen (ICI 46474, (Z)-Tamoxifen, trans-Tamoxifen) is a selective estrogen receptor modulator (SERM). Tamoxifen enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen induces apoptosis.
Blood Cancer J, 2022, 12(3):36
Clin Cancer Res, 2021, 10.1158/1078-0432.CCR-20-3905
Cancers (Basel), 2021, 13(9)2116
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.
Elife, 2021, 10e63691
J Biol Chem, 2021, S0021-9258(21)00245-3
J Pharmacokinet Pharmacodyn, 2021, 10.1007/s10928-021-09787-4
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 is an abundant monounsaturated fatty acid. Oleic acid is a Na+/K+ ATPase activator.
Diabetes Metab Syndr Obes, 2021, 14:4165-4177
S6815 CDN1163 CDN1163 is a small molecular allosteric activator of the sarco/endoplasmic reticulum Ca2+-ATPase (SERCA) that improves Ca2+ homeostasis.
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.
E0054New 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.
E0244New 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.
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.
S0166 BRITE338733 BRITE-338733 is a potent RecA (a DNA-dependent ATPase) inhibitor with IC50 of 4.7 µM.
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.
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
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
J Virol, 2021, JVI.00190-21
Biosci Rep, 2021, BSR20200842
S1413 Bafilomycin A1 (Baf-A1) Bafilomycin A1(Baf-A1) is a vacuolar H+-ATPase inhibitor with IC50 of 0.44 nM. Bafilomycin A1 is found to inhibit autophagy while induces apoptosis.
Nature, 2022, 603(7899):159-165
Cell Res, 2022, 32(2):119-138
Autophagy, 2022, 1-20
S1478 Oligomycin A 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.
Sci Signal, 2022, 15(721):eabi9983
J Agric Food Chem, 2022, 70(9):2898-2910
Nat Commun, 2021, 12(1):5203
S1743 NEXIUM (esomeprazole magnesium) Esomeprazole Magnesium is a proton pump inhibitor to reduce gastric acid secretion through inhibition of H(+)/K(+)-ATPase in gastric parietal cells.
S2000 Sodium orthovanadate Sodium orthovanadate is an alkaline phosphatase and (Na,K)-ATPase inhibitor with IC50 of 10 μM.
Toxicol Appl Pharmacol, 2022, 441:115988
PLoS Pathog, 2021, 17(7):e1009752
Anal Chim Acta, 2021, 1143:144-156
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.
J Virol, 2021, JVI.00190-21
Front Microbiol, 2019, 10:2790
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.
S2233 Esomeprazole sodium Esomeprazole Sodium is a sodium salt of esomeprazole that is a potent proton pump inhibitor with an IC50 of 0.076 mg/kg.
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Hum Cell, 2021, 10.1007/s13577-021-00639-4
Hum Cell, 2021, 34(6):1911-1918
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
Int J Biol Sci, 2019, 15(11):2497-2508
Am J Physiol Renal Physiol, 2019, 316(5):F1078-F1089
S2528 Ciclopirox Ciclopirox is a broad-spectrum antifungal agent working as an iron chelator.
Cell Death Dis, 2021, 12(12):1141
Int J Mol Sci, 2021, 22(15)8299
J Transl Med, 2021, 19(1):347
S3019 Ciclopirox ethanolamine Ciclopirox ethanolamine (Ciclopirox olamine, HOE 296) is a broad-spectrum antifungal agent working as an iron chelator.
Front Cell Dev Biol, 2021, 9:719187
ACS Omega, 2021, 6(12):8477-8487
bioRxiv, 2019, 10.1101/748129
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.

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.
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).
Oncogene, 2021, 40(6):1128-1146
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
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, 2021, S0021-9258(21)00790-0
Mol Immunol, 2021, 139:140-152
J Ethnopharmacol, 2021, S0378-8741(21)00169-0
S4016 Ouabain Ouabain (NSC 25485) is a selective Na+/K+, -ATPase inhibitor, binds to α2 /α3 subunit with Ki of 41 nM/15 nM.
Nat Methods, 2021, 18(1):84-91
Mol Oncol, 2020, 10.1002/1878-0261.12853
bioRxiv, 2020, 2020/9/20.4.7.30734
S4099 Dexlansoprazole Dexlansoprazole (T 168390, TAK 390), 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
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
S4212 Tenatoprazole Tenatoprazole (TU-199) 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
S4290 Digoxin (NSC 95100) Digoxin (NSC 95100) 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.
J Cell Mol Med, 2021, 10.1111/jcmm.16272
J Cell Mol Med, 2021, 25(3):1700-1711
PLoS Pathog, 2020, 16;16(3):e1008341
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.
J Virol, 2021, JVI.00190-21
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.
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
S5608 Pantoprazole sodium hydrate Pantoprazole (BY10232, SKF96022) sodium hydrate (Protonix) is a potent inhibitor of H+/K(+)-ATPase with IC50 of 6.8 μM.
J Virol, 2021, JVI.00190-21
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).
Adv Healthc Mater, 2022, e2102117
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.
S7046 Brefeldin A Brefeldin A 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.
Cell Mol Immunol, 2022, 10.1038/s41423-022-00841-w
PLoS One, 2022, 17(3):e0265805
Nat Cell Biol, 2021, 10.1038/s41556-021-00704-y
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, 2021, 12(1):5315
Biomaterials, 2021, 279:121235
Acta Biomater, 2021, S1742-7061(21)00586-9
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
S7460 BTB06584 BTB06584 is an IF1-dependent, selective inhibitor of the mitochondrial F1 Fo-ATPase.
J Cell Physiol, 2018, 234(1):940-949
Oncotarget, 2017, 8(32):53602-53612
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.
Front Oncol, 2021, 11:743824
bioRxiv, 2020, 2020/9/20.4.7.30734
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.
Cell Res, 2021, 10.1038/s41422-021-00565-y
Sci Adv, 2021, 7(3)eabc6364
Autophagy, 2021, 1-16
S8101 CB-5083 CB-5083 is a potent, selective, and orally bioavailable p97 AAA ATPase inhibitor with IC50 of 11 nM. Phase 1.
Cell Death Dis, 2022, 13(3):203
Nat Commun, 2021, 12(1):713
J Cell Biol, 2021, 220(8)e202009147
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.
Exp Mol Med, 2022, 10.1038/s12276-022-00745-9
Sci Signal, 2022, 15(721):eabi9983
Cell Death Discov, 2022, 8(1):69
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.
A5267 MSH6 Rabbit Recombinant mAb MSH6 Rabbit Recombinant mAb detects endogenous level of MSH6.
A5286 ATPB Rabbit Recombinant mAb ATPB Rabbit Recombinant mAb detects endogenous level of total ATPB.
S1238 Tamoxifen (ICI 46474) Tamoxifen (ICI 46474, (Z)-Tamoxifen, trans-Tamoxifen) is a selective estrogen receptor modulator (SERM). Tamoxifen enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen induces apoptosis.
Blood Cancer J, 2022, 12(3):36
Clin Cancer Res, 2021, 10.1158/1078-0432.CCR-20-3905
Cancers (Basel), 2021, 13(9)2116
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.
Elife, 2021, 10e63691
J Biol Chem, 2021, S0021-9258(21)00245-3
J Pharmacokinet Pharmacodyn, 2021, 10.1007/s10928-021-09787-4
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 is an abundant monounsaturated fatty acid. Oleic acid is a Na+/K+ ATPase activator.
Diabetes Metab Syndr Obes, 2021, 14:4165-4177
S6815 CDN1163 CDN1163 is a small molecular allosteric activator of the sarco/endoplasmic reticulum Ca2+-ATPase (SERCA) that improves Ca2+ homeostasis.
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.
E0054New 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.
E0244New 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.
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