Membrane Transporters/Ion Channels
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Protein translocation Inhibitor
Brefeldin A blocks binding of ADP-ribosylation factor to the Golgi apparatus and inhibits GDP-GTP exchange.
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ATPase antagonist
PF 3716556 is H+,K+-ATPase inhibitor (pIC50 = 6 in human recombinant ion-leaky assays).
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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.
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Artemisinin and its derivatives are a group of drugs that possess the most rapid action of all current drugs against Plasmodium falciparum malaria.
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Ciclopirox is currently being investigated as an alternative treatment to ketoconazole for seborrhoeic dermatitis as it suppresses growth of the yeast Malassezia furfur.It acts by inhibiting the membrane transfer system by interrupting the Na+ K+ ATPase.
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- Katsuhisa Morita, .et al. Decomposition profile data analysis of multiple drug effects identifies endoplasmic reticulum stress-inducing ability as an unrecognized factor, Sci Rep, 2020, 10: 13139 PMID: 32753643
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Pantoprazole is a proton pump inhibitor drug that inhibits gastric acid secretion.
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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.
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Bufalin is an active component isolated from Chan Su, acts as a potent Na+/K+-ATPase inhibitor, binds to the subunit α1, α2 and α3, with Kd of 42.5, 45 and 40 nM, respectively. Anti-cancer activity.
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Resibufogenin is a specific Na+/K+-ATPase inhibitor.
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Bufotalin is a less potent Na+/K+-ATPase inhibitor than other bufadienolides. Potent immunosuppressor.
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Cinobufagin is a specific Na+/K+-ATPase inhibitor. About as active as ouabain
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a-K-ATPase inhibitor
Ouabain is a selective Na+, K+-ATPase inhibitor.
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- Paul Mark Medina, .et al. Revealing the anticancer potential of candidate drugs in vivo using Caenorhabditis elegans mutant strains, Transl Oncol, 2021, Jan;14(1):100940 PMID: 33221682
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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.
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- Makoto Kawatani, .et al. Identification of a Small-Molecule Glucose Transporter Inhibitor, Glutipyran, That Inhibits Cancer Cell Growth, ACS Chem Biol, 2021, 16, 8, 1576-1586
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ATPase Inhibitors
Omeprazole is a cell-permeable, selective proton pump inhibitor.
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Istaroxime is a positive inotropic agent that mediates its action through inhibition of sodium/potassium adenosine triphosphatase (Na+/K+ ATPase).
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Na+/K+ ATPase modulator
Rostafuroxin (PST-2238) is an ouabain-inhibitor counteracting specific forms of hypertension.
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myosin II inhibitor
Blebbistatin, a myosin II inhibitor, is photoinactivated by blue light.
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F1 Fo-ATPase inhibitor
BTB06584 is an IF1-dependent, selective inhibitor of the mitochondrial F1 Fo-ATPase.
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Na+/K+ ATPase inhibitor
Melittin is a Na+/K+ ATPase inhibitor. It inhibits Gs and stimulates Gi activity. It inhibits protein kinase C and cAMP-dependent protein kinases.
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ATP synthase inhibitor
Oligomycin is a macrolide that acts as a specific inhibitor of the mitochondrial ATP-synthase and blocks oxidative phosphorylation.
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SERCA inhibitor
Cyclopiazonic acid is an inhibitor of SERCA (endoplasmic reticulum Ca2+-ATPase) which induces the release of intracellular stored Ca2+, without increasing IP3 levels.
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Ca 2+ /Mg 2+ -ATPase inhibitor
Glucagon (19-29) (human) is a potent Ca 2+ /Mg 2+ -ATPase inhibitor.
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CFTR inhibitor
PTC124 also known as Ataluren is CFTR-G542X nonsense allele inhibitor.
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- L Kadunc, .et al. Increased Gene Translation Stringency in Mammalian Cells by Nonsense Suppression at Multiple Permissive Sites With a Single Noncanonical Amino Acid, FEBS Lett, 2020, May 13 PMID: 32401336
- Caspi M, .et al. A flow cytometry-based reporter assay identifies macrolide antibiotics as nonsense mutation read-through agents, J Mol Med (Berl), 2016, Apr;94(4):469-82 PMID: 26620677
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CFTR activator
VX-770 (Ivacaftor) is known as a CFTR potentiator.
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- Okiyoneda T, .et al. Chaperone-Independent Peripheral Quality Control of CFTR by RFFL E3 Ligase, Dev Cell, 2018, Mar 26;44(6):694-708.e7 PMID: 29503157
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CFTR modulator
VX-809 is the second investigational oral candidate compound for the treatment of cystic fibrosis (CF).
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- Kusumika Saha, .et al. Pharmacological chaperone-rescued cystic fibrosis CFTR-F508del mutant overcomes PRAF2-gated access to endoplasmic reticulum exit sites, Cell Mol Life Sci, 2022, Sep 27;79(10):530 PMID: 36167862
- Heledd H Jarosz-Griffiths, .et al. Different CFTR Modulator Combinations Downregulate Inflammation Differently in Cystic Fibrosis, Elife, 2020, Mar 2;9:e54556 PMID: 32118580
- Okiyoneda T, .et al. Chaperone-Independent Peripheral Quality Control of CFTR by RFFL E3 Ligase, Dev Cell, 2018, Mar 26;44(6):694-708.e7 PMID: 29503157
- Junko Kido, .et al. Cystic Fibrosis Transmembrane Conductance Regulator Reduces Microtubule-Dependent Campylobacter jejuni Invasion, Infect Immun, 2017, Oct; 85(10): e00311-17 PMID: 28784926
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CFTR corrector
VX-661 is another cystic fibrosis transmembrane conductance regulator (CFTR) corrector in development for the treatment of cystic fibrosis.
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- Kusumika Saha, .et al. Pharmacological chaperone-rescued cystic fibrosis CFTR-F508del mutant overcomes PRAF2-gated access to endoplasmic reticulum exit sites, Cell Mol Life Sci, 2022, Sep 27;79(10):530 PMID: 36167862
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K+ channel and CFTR Cl- channel blocker
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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).
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- Dao-Lai Zhang, .et al. Gq activity- and β-arrestin-1 scaffolding-mediated ADGRG2/CFTR coupling are required for male fertility, eLife, 2018, 7: e33432 PMID: 29393851
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CFTR chloride channel inhibitor
PPQ-102 is a compound that targets intracellular nucleotide binding domain(s) of CFTR and inhibits CFTR- mediated chloride current in a voltage-dependent and reversible manner.
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CFTR Inhibitor
Oridonin (Isodonol), an entkaurane diterpenoid isolated from Rabdosia rubescens, is an important traditional Chinese herbal remedy.
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CFTR inhibitor
CFTRinh-172 is a voltage-independent, selective CFTR inhibitor
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- Dao-Lai Zhang, .et al. Gq activity- and β-arrestin-1 scaffolding-mediated ADGRG2/CFTR coupling are required for male fertility, eLife, 2018, 7: e33432 PMID: 29393851
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F508del-CFTR trafficking corrector
KM 11060 corrects F508del-CFTR trafficking, increasing the amount of functional CFTR at the plasma membrane (~75%) and Inhibits PDE5 activity
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CFTR potentiator
PG 01 is a cystic fibrosis transmembrane conductance regulator (CFTR) potentiator. PG 01 is effective on G970R although with a significant decrease in potency relative to E193K and δF508.
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CFTR corrector
CFTR corrector 2 is a cystic fibrosis transmembrane conductance corrector (CFTR), extracted from patent US20140274933.
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CFTR potentiator
GLPG2451 is a cystic fibrosis transmembrane conductance regulator (CFTR) potentiator, which effectively potentiates low temperature rescued F508del CFTR with an EC50 of 11.1 nM.
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CFTR potentiator
Ivacaftor benzenesulfonate is an orally bioavailable CFTR potentiator, used for cystic fibrosis treatment.
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CFTR potentiator
Ivacaftor hydrate is an orally bioavailable CFTR potentiator, used for cystic fibrosis treatment.
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intracellular Ca2+ handling modulator
Caldaret is an intracellular Ca2+ handling modulator that acts through reverse mode Na+/Ca2+ exchanger inhibition.
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T-type Ca2+ channel blocker
ABT-639 hydrochloride is a novel, peripherally acting, selective T-type Ca2+ channel blocker.
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L-type Ca2+ channel agonist
(S)-(-)-Bay-K-8644 is an agonist of L-type Ca2+ channel. (S)-(-)-Bay-K-8644 activates Ba2+ currents (IBa) (EC50=32 nM).
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T-type Ca2+ channel antagonist
TTA-Q6 is a selective T-type Ca2+ channel antagonist, used in the neurological disease.
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T-type Ca2+ channel antagonist
TTA-Q6(isomer) is an isomer of TTA-Q6. TTA-Q6 is a selective T-type Ca2+ channel antagonist.
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Ca2+-dependent blocker
TV-519 free base (K201 free base) is a Ca2+-dependent blocker of sarcoplasmic reticulum Ca2+-stimulated ATPase (SERCA) and a partial agonist of ryanodine receptors in striated muscle. Antiarrhythmic and cardioprotective properties.
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N- and P/Q-type Ca2+ channels agonist
GV-58 is a potent, selective N- and P/Q-type Ca2+ channels agonist with EC50 of 7.21/8.81 uM for N-type/P-Q-type Ca2+ channel; 20-fold less potent CDK inhibitor activity.
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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.
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Ca2+ signaling modulator
Astragaloside A is a novel regulator of HIF-1α and angiogenesis through the PI3K/Akt pathway in HUVECs that are exposed to hypoxia.
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Myosin activator
CK-1827452 is a selective cardiac specific myosin activator.
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- Oleg Lookin, .et al. Omecamtiv mecarbil attenuates length-tension relationship in healthy rat myocardium and preserves it in monocrotaline-induced pulmonary heart failure, Clin Exp Pharmacol Physiol, 2021, Aug 29 PMID: 34459025
- Gabor A. Fulop, .et al. Omecamtiv mecarbil evokes diastolic dysfunction and leads to periodic electromechanical alternans, Basic Res Cardiol, 2021, 116(1): 24 PMID: 33844095
- Wanjian Tang, .et al. Dilated cardiomyopathy mutation in the converter domain of human cardiac myosin alters motor activity and response to omecamtiv mecarbil, J Biol Chem, 2019, October 2 PMID: 31578282
- Thinh T. Kieu, .et al. Omecamtiv Mecarbil Slows Myosin Kinetics in Skinned Rat Myocardium at Physiological Temperature, Biophysical Journal, 2019, 2019 PMID: 31103235
- Alexandre J. S. Ribeiro, .et al. Multi-Imaging Method to Assay the Contractile Mechanical Output of Micropatterned Human iPSC-Derived Cardiac Myocytes, Circ Res, 2017, May 12; 120(10): 1572-1583 PMID: 28400398
- Anja M. Swenson, .et al. Omecamtiv Mecarbil Enhances the Duty Ratio of Human β-Cardiac Myosin Resulting in Increased Calcium Sensitivity and Slowed Force Development in Cardiac Muscle, J Biol Chem, 2017, Mar 3; 292(9): 3768-3778 PMID: 28082673
- Nánási P Jr, .et al. Omecamtiv mecarbil activates ryanodine receptors from canine cardiac but not skeletal muscle, Eur J Pharmacol, 2017, Aug 15;809:73-79 PMID: 28506910
- Horv??th B, .et al. Frequency-dependent effects of omecamtiv mecarbil on cell shortening of isolated canine ventricular cardiomyocytes, Naunyn Schmiedebergs Arch Pharmacol, 2017, Dec;390(12):1239-1246 PMID: 28940010
- Szentandrassy N, .et al. Dose-dependent electrophysiological effects of the myosin activator omecamtiv mecarbil in canine ventricular cardiomyocytes, J Physiol Pharmacol, 2016, Aug;67(4):483-489 PMID: 27779469
- L Nagy, .et al. The novel cardiac myosin activator omecamtiv mecarbil increases the calcium sensitivity of force production in isolated cardiomyocytes and skeletal muscle fibres of the rat, Br J Pharmacol, 2015, Sep; 172(18): 4506-4518 PMID: 26140433
- Larissa Butler, .et al. Enhanced characterization of contractility in cardiomyocytes during early drug safety assessment, Toxicol Sci, 2015, Jun;145(2):396-406 PMID: 25820236
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Manidipine 2HCl is a HCl salt form of Manidipine which is a calcium channel blocker for Ca2+ current with IC50 of 2.6 nM.
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- Noriaki Ikemura,, .et al. Inhibitory effects of antihypertensive drugs on human cytochrome P450 2J2 activity: Potent inhibition by azelnidipine and manidipine, Chem -Biol Interact, 2019, 306:1-9
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L-type calcium channel blocker
Amlodipin is L-type calcium channel blocker that displays antihypertensive properties. It inhibits Ca2+-induced contractions in depolarized rat aorta (IC50 = 1.9 nM) and displays vasoprotective effects in cardiovascular disease.
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