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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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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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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. -
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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ATPase inhibitor
Oligomycin A is a mitochondrial ATPase inhibitor. Oligomycin A inhibits ATP5 (mitochondrial ATPases, F1F0) bound to the cell membrane.- Makoto Kawatani, .et al. , ACS Chem Biol, 2021, 16, 8, 1576-1586
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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. -
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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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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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. -
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
- 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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SGLT2 Inhibitor
Canagliflozin is an inhibitor of subtype 2 sodium-glucose transport protein (SGLT2).- 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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SGLT2 inhibitor
PF-04971729 is a potent and selective inhibitor of the sodium-dependent glucose cotransporter 2. -
Protein translocation Inhibitor
Brefeldin A blocks binding of ADP-ribosylation factor to the Golgi apparatus and inhibits GDP-GTP exchange. -
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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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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PDE1 inhibitor
Vinpocetine is a Ca2+-calmodulin-dependent phosphodiesterase I (PDE1) inhibitor. -
serotonin transporter (SER) inhibitor
Vilazodone Hydrochloride (EMD 68843 Hydrochloride) is a serotonin transporter (SER) inhibitor and 5-HT1A receptor partial agonist. -
Na+/Ca2+ Exchanger Inhibitor
KB-R7943 mesylate is a cell permeable, potent, selective NCKX inhibitor of the reverse mode of Na+/Ca2+ exchange in cells expressing NCX1. -
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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Nav inhibitor
Nav1.7-IN-2 is an inhibitor of voltage-gated sodium channels (Nav), in particular Nav 1.7, with IC50 of 80 nM. -
Ca2+ channel agonist/CDK2 inhibitor
Ca2+ channel agonist 1 is an agonist of N-type Ca2+ channel and an inhibitor of Cdk2, with EC50s of 14.23 μM and 3.34 μM, respectively, and is used as a potential treatment for motor nerve terminal dysfunction. -
P-gp inhibitor
Norverapamil hydrochloride ((±)-Norverapamil hydrochloride), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor. -
TRPC6 inhibitor
TRPC6-IN-1 is a Transient Receptor Potential Canonical 6 Channel (TRPC6) inhibitor, with an EC50 of 4.66 μM. -
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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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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CNT2 Inhibitor
CNT2 inhibitor-1 is a potent concentrative nucleoside transporter 2 Inhibitor (CNT2), with an IC50 of 640 nM for hCNT2. -
SGLT2 inhibitor
Tofogliflozin is an inhibitor of subtype 2 sodium-glucose transport protein (SGLT2), which is responsible for at least 90% of the glucose reabsorption in the kidney. -
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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SGLT1/SGLT2 inhibitor
Licogliflozin is a sodium glucose cotransporter (SGLT1 and SGLT2) inhibitor. -
Na+/H+-exchange inhibitor
FR183998 free base is a potent Na+/H+-exchange inhibitor, with IC50s of 0.3 nM, 3.1 nM and 6.5 nM by measurement of pHi change in rat lymphocytes, rat and human platelets, respectively. -
Na+/H+ exchange inhibitor
Cariporide (HOE-642) is a selective Na+/H+ exchange inhibitor. -
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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glutamate release inhibitor
Sipatrigine, a neuroprotective agent, is a glutamate release inhibitor, voltage-dependent sodium channel and calcium channel inhibitor, penetrating the central nervous system. Has potential to treat focal cerebral ischemia and stroke.

