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CFTR inhibitor
PTC124 also known as Ataluren is CFTR-G542X nonsense allele inhibitor.- Adi Amar-Schwartz, .et al. , Hum Mol Genet, 2023, Jul 20;32(15):2455-2463 PMID: 37145099
- L Kadunc, .et al. , FEBS Lett, 2020, May 13 PMID: 32401336
- Caspi M, .et al. , J Mol Med (Berl), 2016, Apr;94(4):469-82 PMID: 26620677
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TRPC1/4/5 channels inhibitor
Pico145 is a remarkable inhibitor of TRPC1/4/5 channels, inhibits (?)-englerin A-activated TRPC4/TRPC5 channels, with IC50s of 0.349 and 1.3 nM in cells, and shows no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, TRPM8.- Aki Teranishi, .et al. , Nat Commun, 2024, Dec 12;15(1):10476 PMID: 39668169
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myosin II inhibitor
Blebbistatin, a myosin II inhibitor, is photoinactivated by blue light.- Anastasiia Kovaleva, .et al. , Int J Mol Sci, 2025, Aug 9;26(16):7701 PMID: 40869022
- Anastasiia Kovaleva, .et al. , Cell and Developmental Biology, 2024, Dec 25
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MCT Inhibitor?€?
7ACC1 selectively interfere with lactate fluxes in the lactate-rich tumor microenvironment; inhibits lactate influx but not efflux in tumor cells expressing MCT1 and MCT4 transporters.- Daniel Gundel, .et al. , Int J Mol Sci, 2021, Feb; 22(4): 1645 PMID: 33562048
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a-K-ATPase inhibitor
Ouabain is a selective Na+, K+-ATPase inhibitor.- Daniel J Pfau, .et al. , Autophagy Rep, 2025, 4(1):2473765 PMID: 40265045
- Paul Mark Medina, .et al. , Transl Oncol, 2021, Jan;14(1):100940 PMID: 33221682
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CFTR inhibitor
CFTRinh-172 is a voltage-independent, selective CFTR inhibitor- Dao-Lai Zhang, .et al. , eLife, 2018, 7: e33432 PMID: 29393851
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CFTR inhibitor
CFTR inhibitor II, also known as GlyH-101, is a glycine hydrazide that selectively and reversibly blocks the CFTR channel (Ki = 4.3 uM).- Dao-Lai Zhang, .et al. , eLife, 2018, 7: e33432 PMID: 29393851
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Ferroptosis inhibitor
RSL3 is a ferroptosis activator in a VDAC-independent manner,exhibiting selectivity for tumor cells bearing oncogenic RAS.- Duo Shi, .et al. , Antioxid Redox Signal, 2025, Sep 30 PMID: 41027674
- Cheng Chen, .et al. , Neurochem Res, 2025, Mar 18;50(2):122 PMID: 40100474
- Xiaona Cao, .et al. , J Nanobiotechnology, 2025, Feb 24;23(1):136 PMID: 39994619
- Naoya Yamada, .et al. , Nat Commun, 2024, 15:2195 PMID: 38472233
- Ning Li, .et al. , J Ovarian Res, 2024, Feb 23;17(1):49 PMID: 38396022
- Yuki Kojima, .et al. , Journal of Gastroenterology, 2023, Nov 10
- Qingyu Zhang, .et al. , Cell Death Discov, 2023, Mar 8;9(1):83 PMID: 36882396
- Sampilvanjil A, .et al. , Am J Physiol Heart Circ Physiol, 2020, Mar 1;318(3):H508-H518 PMID: 31975626
- Fujiki K, .et al. , Cell Death Differ, 2019, Feb 25 PMID: 30804470
- Samantha W. Alvarez, .et al. , Nature, 2017, Nov 30; 551(7682): 639-643 PMID: 29168506
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sodium-potassium pump inhibitor
Digoxin is a sodium-potassium pump inhibitor.- Ella Martin, .et al. , ACS Pharmacol Transl Sci, 2025, May 12;8(9):2996-3006 PMID: 40969890
- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
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Sodium Channel inhibitor
AmbroxolHCl is a potent inhibitor of the neuronal Na+ channels, inhibits TTX-resistant Na+ currents with IC50 of 35.2 uM and 22.5 μM for tonic and phasic block, inhibits TTX-sensitive Na+ currents with IC50 of 100 μM. Phase 3.- Giovanni Bocci, .et al. , ACS Pharmacol Transl Sci, 2020, Oct 14 PMID: 33330842
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LAT-1 inhibitor
JPH203 is a potent and selective L-type amino acid transporter 1 (LAT-1) inhibitor.- Kaito Yamashiro, .et al. , J Toxicol Sci, 2026, 51(2):141-147 PMID: 41621859
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TRPC3 inhibitor
Pyr10is a novel TRPC3-selective inhibitor, IC50 of Ca2+ influx inhibition by Pyr10 in carbachol-stimulated YFP-TRPC3-transfected HEK293 cells for ROCE and thapsigargin-depleted native RBL-2H3 cells for SOCE is 0.72 uM and 13.08 uM.- Keisuke Obara, .et al. , Biol Pharm Bull, 2025, 48(9):1444-1455 PMID: 41033978
- Keisuke Obara, .et al. , Biol Pharm Bull, 2025, 48(6):932-940 PMID: 40582844
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P-gp & BCRP inhibitor
Elacridaris a prototypical BCRP inhibitor which inhibits the Bcrp1-mediated transport.- Leo Shen, .et al. , Sci Rep, 2021, Sep 16;11(1):18516 PMID: 34531456
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MCT1 inhibitor
AZD3965 is a selective inhibitor of monocarboxylate transporter 1 (MCT1) with a binding affinity of 1.6 nM, is 6 fold selective over MCT2 and does not inhibit MCT4 at 10 μM.- Lu Gao, .et al. , Int J Biol Sci, 2022, Jan 1;18(2):599-616 PMID: 35002512
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VDAC inhibitor
Erastin is a cell-permeable piperazinyl-quinazolinone compound that exhibits oncogene-selective lethality in cells with H-Ras mutations.- Mao Yang, .et al. , Biochem Biophys Res Commun, 2025, Sep 5:784:152599 PMID: 40972362
- Xuejie Huan, .et al. , Neurosci Bull, 2024, Dec 12 PMID: 39666195
- Filiz Bakar-Ates, .et al. , Naunyn Schmiedebergs Arch Pharmacol, 2024, Oct 11 PMID: 39392483
- Filiz Bakar-Ates, .et al. , Toxicol In Vitro, 2024, Feb:94:105732 PMID: 37956772
- Sureya Nijiati, .et al. , Mol Pharm, 2023, Oct 2;20(10):5185-5194 PMID: 37711135
- Erva Ozkan, .et al. , Life Sci, 2023, Jan 1;312:121222 PMID: 36442526
- Yuki Shibata, .et al. , Biochem Biophys Rep, 2021, Feb 24;26 PMID: 33681481
- Shibata Y, .et al. , PLoS One, 2019, Dec 4;14(12):e0225931 PMID: 31800616
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P-gp inhibitor
Tariquidar (XR9576) is a P-glycoprotein drug efflux pump inhibitor.- Maria Joao Moreno, .et al. , Pharmaceutics, 2023, Jan 3;15(1):174 PMID: 36678803
- Yuko Sasaki, .et al. , Biol Pharm Bull, 2022, 45(9):1246-1253 PMID: 36047192
- Sugisawa N, .et al. , Mol Pharm, 2018, Sep 4;15(9):4021-4030 PMID: 30052463
- Samy A. F. Morad, .et al. , Biochem Pharmacol, 2017, Apr 15; 130: 21-33 PMID: 28189725
- Debora Petroni, .et al. , Mol Imaging Biol, 2016, Dec;18(6):916-923 PMID: 27234445
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MCT1 and MCT2 inhibitor
AR-C155858 is a potent inhibitor of monocarboxylate transporters MCT1 and MCT2 that binds to an intracellular site involving transmembrane helices 7-10.- Min Chang Choi, .et al. , Arch Pharm Res, 2023, Dec;46(11-12):907-923 PMID: 38048029
- Charlotte Petersen, .et al. , Sci Rep, 2017, 7: 13101 PMID: 29026134
- Kong SC, .et al. , Pancreas, 2016, Aug;45(7):1036-47 PMID: 26765963
- Anne Poder, .et al. , Mol Cancer, 2016, 15: 45 PMID: 27266704
- Eumorphia G. Konstantakou, .et al. , Mol Cancer, 2015, 14: 135 PMID: 26198749
- Álvarez Z, .et al. , Biomaterials., 2014, 35(17):4769-81 PMID: 24636215
- Álvarez Z, .et al. , Cereb Cortex., 2014, 26(3):1046-58 PMID: 25452568
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ATPase inhibitor
Bafilomycin A1 prevents maturation of autophagic vacuoles by inhibiting fusion between autophagosomes and lysosomes in rat hepatoma cell line, H-4-II-E cells.- Ravindra Pramod Deshpande, .et al. , EMBO Mol Med, 2025, Apr;17(4):797-822 PMID: 40087501
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Calcium Channel inhibitor
Nimodipine is a L-type Ca2+ channel blocker.- Shiqian Han, .et al. , iScience, 2023, Apr 8;26(5):106613 PMID: 37128603
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MSCs Inhibitor
GsMTX4 is a 34 amino acid peptidyl toxin isolated from the Grammostola rosea (Chilean rose) tarantula venom and belongs to the huwentoxin-1 family.- Shota Inoue, .et al. , Bone, 2023, Dec:177:116916 PMID: 37777037
- Jean-Baptiste Cavin, .et al. , J Physiol, 2023, Apr;601(7):1183-1206 PMID: 36752210
- Yong Chen, .et al. , Gastroenterology, 2021, Apr 2 PMID: 33819485
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MDR1/P-gp Inhibitor
PSC-833 is a kind of P-glycoprotein (P-gp) modulator that inhibits P-gp-mediated multidrug-resistance (MDR).- Somin Lee, .et al. , Methods Mol Biol, 2022, 2492:251-263 PMID: 35733049
- Somin Lee, .et al. , Biotechnol Bioeng, 2019, 10 November
- Somin Lee, .et al. , bioRxiv, 2018, Nov. 18 PMID: 31709508
- Watanabe N, .et al. , Biopharm Drug Dispos, 2018, Jan;39(1):30-37 PMID: 29055041
- Higashi H, .et al. , Biol Pharm Bull, 2017, 40(8):1314-1319 PMID: 28769012
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SGLT1/SGLT2 inhibitor
Phlorizin is a competitive inhibitor of SGLT1 and SGLT2; this reduces renal glucose transport, lowering the amount of glucose in the blood.- Subramaniam M, .et al. , Am J Physiol Regul Integr Comp Physiol, 2019, Nov 20 PMID: 31746628
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ATPase inhibitor
Oligomycin A is a mitochondrial ATPase inhibitor. Oligomycin A inhibits ATP5 (mitochondrial ATPases, F1F0) bound to the cell membrane.- Suzanna H Harrison, .et al. , Nat Commun, 2025, Nov 25;16(1):11018 PMID: 41290674
- Makoto Kawatani, .et al. , ACS Chem Biol, 2021, 16, 8, 1576-1586 PMID: 34296611
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NHE3 inhibitor
Tenapanor acts as an inhibitor of the sodium-proton exchanger NHE3. This antiporter protein is found in the kidney and intestines, and normally acts to regulate the levels of sodium absorbed and secreted by the body.- Takuto Fujii, .et al. , Am J Physiol Cell Physiol, 2026, 330: C1605-C1615 PMID: 41962948
- Ju Wang, .et al. , Am J Physiol Cell Physiol, 2025, Jul 1;329(1):C50-C67 PMID: 40434024
- Mahdi Amiri, .et al. , Am J Physiol Cell Physiol, 2024, Mar 1;326(3):C829-C842 PMID: 38223928
- Kuniko Hunter, .et al. , Tissue Eng Part A, 2022, Nov 18 PMID: 36274231
- Xingjie Tan, .et al. , Authorea, 2022, May 25
- Kunyan Zhou, .et al. , Am J Physiol Cell Physiol, 2021, Sep 1;321(3):C471-C488 PMID: 34288721
- Qinghai Tan, .et al. , Br J Pharmacol, 2021, Mar;178(5):1018-1036 PMID: 33179259
- Y Liu, .et al. , Biochem Pharmacol, 2020, May 16;178:114040 PMID: 32422138
- Yu Y, .et al. , Cell Physiol Biochem, 2019, 52(5):1017-1038 PMID: 30977986
- Thammayon N, .et al. , Amino Acids, 2017, Apr;49(4):725-734 PMID: 27981415
- Charoenphandhu N, .et al. , Mol Cell Biochem, 2017, Mar;427(1-2):201-208 PMID: 27995414
- Jantarajit W, .et al. , Am J Physiol Cell Physiol, 2017, Jul 1;313(1):C118-C129 PMID: 28490422
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MCT inhibitor
CHC is a monocarboxylic acid transport (MCT) inhibitor. Exhibits antitumoral and antiangiogenic activity in gliomas; decreases glycolytic metabolism, migration, and invasion in U251 cells.- Tian Peng, .et al. , World J Gastroenterol, 2024, May 21;30(19):2575-2602 PMID: 38817665
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SGLT2 inhibitor
Dapagliflozin inhibits subtype 2 of the sodium-glucose transport proteins (SGLT2), which is responsible for at least 90% of the glucose reabsorption in the kidney.- Tingting Ding, .et al. , J Diabetes Complications, 2024, Dec 9;39(2):108930 PMID: 39673870
- David Papadopoli, .et al. , Neoplasia, 2021, Apr;23(4):391-399 PMID: 33784591
- Neil Tanday, .et al. , Biochem Pharmacol, 2020, Jul;177:114009 PMID: 32360307
- Subramaniam M, .et al. , Am J Physiol Regul Integr Comp Physiol, 2019, Nov 20 PMID: 31746628
- Marina Subramaniam, .et al. , Physiol Rep, 2019, May; 7(9): e14090 PMID: 31062524
- Angelopoulou A, .et al. , AAPS PharmSciTech, 2018, Feb;19(2):621-633 PMID: 8924948
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HIF-1α inhibitor
Minocycline hydrochloride is a broad-spectrum tetracycline antibiotic, acting by binding to the bacterial 30S ribosomal subunit and inhibiting protein synthesis.- Viktoria Lazar, .et al. , Nature, 2022, 610: 540-546 PMID: 36198788
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SGLT2 inhibitor
Canagliflozin hemihydrate is the hemihydrate form of canagliflozin, which is a SGLT2 inhibitor with IC50 of 2.2 nM for hSGLT2 in a cell-free assay, exhibits 413-fold selectivity over hSGLT1.- Wafaa N Albalawy, .et al. , Am J Physiol Renal Physiol, 2024, Jun 1;326(6):F1041-F1053 PMID: 38660713
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NCX inhibitor
SEA0400 is a novel and selective inhibitor of the Na+-Ca2+ exchanger with IC50 of 5-33 nM (inhibiting Na+-dependent Ca2+ uptake in cultured neurons, astrocytes, and microglia).- Wakana Shoda, .et al. , PLoS One, 2020, 15(6): e0235360 PMID: 32603346
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SGLT2 Inhibitor
Canagliflozin is an inhibitor of subtype 2 sodium-glucose transport protein (SGLT2).- Yiguan Chen, .et al. , Int J Biol Sci, 2026, 22(9):4618-4632 PMID: 42157939
- Ming-Jer Hsieh, .et al. , Naunyn Schmiedebergs Arch Pharmacol, 2025, Apr 30 PMID: 40304747
- Courtney Sakolish, .et al. , Biomedicines, 2025, 13(3), 563
- Jing Zhou, .et al. , Exp Mol Med, 2022, Nov; 54(11): 2007-2021 PMID: 36385558
- David Papadopoli, .et al. , Neoplasia, 2021, Apr;23(4):391-399 PMID: 33784591
- Angelopoulou A, .et al. , Nanomedicine, 2018, Oct;13(19):2435-2454 PMID: 30311542
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CRM1 inhibitor
KPT-330 inhibitor of CRM1 (XPO1)-mediated nuclear export has selective anti-leukaemic activity in preclinical models of T-cell acute lymphoblastic leukaemia and acute myeloid leukaemia.- Yingying Gao, .et al. , Am J Physiol Renal Physiol, 2025, Oct 1;329(4):F496-F509 PMID: 40897473
- Suhyun Lee, .et al. , Pharmaceutics, 2025, Jul 16;17(7):919 PMID: 40733127
- Youjin Na, .et al. , Oncogene, 2023, Mar;42(13):1038-1047 PMID: 36759572
- Chie Ishikawa, .et al. , Invest New Drugs, 2022, Aug;40(4):718-727 PMID: 35477814
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AMPA Receptor Inhibitor
Aniracetam is an ampakine and nootropic of the racetam chemical class purported to be considerably more potent than piracetam. -
Protein kinase inhibitor
Apigenin, found in many plants, is a natural product belonging to the flavone class that is the aglycone of several naturally-occurring glycosides. Apigenin acts as a monoamine transporter activator, one of the few chemicals demonstrated to possess this property. Apigenin is a ligand for central benzodiazepine receptors that competitively inhibited the binding of flunitrazepam with a Ki of 4μM, exerting anxiolytic and slight sedative effects.
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Proton pump inhibitor
Esomeprazole sodium is a proton pump inhibitor which reduces acid secretion through inhibition of the H+ / K+ ATPase in gastric parietal cells. -
Kir6.2/SUR inhibitor
Glimepiride is a potent Kir6.2/SUR inhibitor with IC50 of 3.0 nM, 5.4 nM, and 7.3 nM for SUR1, SUR2A and SUR2B, used in the treatment of type 2 diabetes mellitus. -
proton pump inhibitor
Lansoprazole(AG 1749) is a proton pump inhibitor which prevents the stomach from producing acid. -
PDE4 inhibitor
Luteolin is a PDE4 inhibitor, phosphodiesterase inhibitor, and an interleukin 6 inhibitor, affecting xylazine/ketamine-induced anesthesia in mice. Luteolin acts as a monoamine transporter activator, and is one of the few chemicals demonstrated to possess this property. -
ATPase Inhibitors
Omeprazole is a cell-permeable, selective proton pump inhibitor. -
CFTR Inhibitor
Oridonin (Isodonol), an entkaurane diterpenoid isolated from Rabdosia rubescens, is an important traditional Chinese herbal remedy. -
Potassium Channel inhibitor
Repaglinide is a potent short-acting insulin secretagogue that acts by closing ATP-sensitive potassium (KATP) channels in the plasma membrane of the pancreatic beta cell. -
protein tyrosine phosphatases inhibitor
Sodium orthovanadate is the chemical compound Na3VO4. It is an inhibitor of protein tyrosine phosphatases, alkaline phosphatases and a number of ATPases, most likely acting as a phosphate analogue. -
Calcium Channel inhibitor
Tetrandrine is a calcium channel blocker. It inhibits the degranulation of mast cells.Tetrandrine has anti-inflammatory and anti-fibrogenic actions, which make tetrandrine and related compounds potentially useful in the treatment of lung silicosis, liver cirrhosis, and rheumatoid arthritis. -
SGLT2 inhibitor
PF-04971729 is a potent and selective inhibitor of the sodium-dependent glucose cotransporter 2. -
Calcium channel antagonist
Felodipine is a 1,4-dihydropyridine antagonist and calcium channel protein inhibitor.
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noradrenalin transporters inhibitor
Desipramine hydrochloride is a tricyclic antidepressant that is a selective inhibitor of noradrenalin transporters (Ki values are 4, 61 and 78720 nM for NET, SERT and DAT transporters respectively).
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TRPV1 antagonist and TNF-alpha production inhibitor
LASSBio-1135 is a dual TRPV1 antagonist and TNF-alpha production inhibitor.

