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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. -
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.- 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. -
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.- 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).- 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. -
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. -
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. -
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.- 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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a-K-ATPase inhibitor
Ouabain is a selective Na+, K+-ATPase inhibitor.- 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
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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Serotonin transporter inhibitor
Imipramine Hydrochloride is a tricyclic antidepressant. Inhibits the serotonin and norepinephrine transporters but has little effect on the dopamine transporter. -
SGLT2 inhibitor
Ipragliflozin is a highly potent and selective SGLT2 inhibitor with IC50 of 2.8 nM; little and NO potency for SGLT1/3/4/5/6. -
myosin II inhibitor
Blebbistatin, a myosin II inhibitor, is photoinactivated by blue light. -
AMPA desensitization inhibitor
Cyclothiazide is a benzothiadiazide that acts as a potentiator of AMPA receptors, positively modulating its response to glutamic acid (EC50 = 3.8 M). -
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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NaV1.3 and NaV1.1 channels inhibitor
ICA-121431 is a potent and selective inhibitor of human NaV1.3 and NaV1.1 channels (IC50 values are 13 and 23 nM respectively). -
VDAC inhibitor
Erastin is a cell-permeable piperazinyl-quinazolinone compound that exhibits oncogene-selective lethality in cells with H-Ras mutations.- 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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sodium channel protein inhibitor
Oxcarbazepine is a sodium channel protein inhibitor.