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P-gp inhibitor
P-gp inhibitor 1 is a novel inhibitor reversing P-glycoprotein-mediated multidrug resistance. -
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
Luseogliflozin is an orally active second-generation sodium-glucose co-transporter 2 (SGLT2) inhibitor developed by Taisho Pharmaceutical for the treatment of patients with type 2 diabetes mellitus (T2DM). -
P-gp inhibitor
Laniquidar is a third-generation P-gp inhibitor, which has been used in clinic trials for modulating multidrug resistance transporters. -
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. -
voltage-gated sodium channel Nav1.7 inhibitor
Nav1.7-IN-3 is a selective, orally bioavailable voltage-gated sodium channel Nav1.7 inhibitor with an IC50 of 8 nM. Pain relief. Limited CNS penetration. -
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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hASBT inhibitor
GSK2330672 is a highly potent, nonabsorbable apical sodium-dependent bile acid transporter inhibitor. -
Ca2+ release inhibitor
Dantrolene sodium is a muscle relaxant that acts by abolishing excitation-contraction coupling in muscle cells, probably by action on the ryanodine receptor. -
sodium channel protein inhibitor
Oxcarbazepine is a sodium channel protein inhibitor. -
SGLT2 inhibitor
Remogliflozin inhibits the sodium-glucose transport (SGLT2) proteins, which are responsible for glucose reabsorption in the kidney. -
ATP synthase inhibitor
Oligomycin is a macrolide that acts as a specific inhibitor of the mitochondrial ATP-synthase and blocks oxidative phosphorylation. -
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. -
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.- 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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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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Sodium channel blocker/DNMT inhibitor
Procainamide HCl is a sodium channel blocker, and also a DNA methyltransferase inhibitor. -
sodium-potassium pump inhibitor
Digoxin is a sodium-potassium pump inhibitor.- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
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proton pump inhibitor
Tenatoprazole is a prodrug of the proton pump inhibitor (PPI) class, which inhibits proton transport with IC50 of 3.2 uM. -
MCT1 inhibitor
AR-C117977 is a potent MCT1 inhibitor, which can reduce vimmune responses both in vitro and in vivo, maintains long-term graft survival, and induces operational tolerance. -
Ca 2+ /Mg 2+ -ATPase inhibitor
Glucagon (19-29) (human) is a potent Ca 2+ /Mg 2+ -ATPase inhibitor. -
serotonin reuptake inhibitor
Azaphen is a potent inhibitor of the reuptake of serotonin. -
Glycine reuptake inhibitor
RG1678 (Bitopertin) is a potent and noncompetitive glycine reuptake inhibitor (GlyT1). -
Glycine reuptake inhibitor
RG1678 (Bitopertin) is a potent and noncompetitive glycine reuptake inhibitor (GlyT1). -
P-gp inhibitor
Elacridar hydrochloride is a P-glycoprotein inhibitor, and has been used both in vitro and in vivo as a tool inhibitor of P-glycoprotein (Pgp) to investigate the role of transporters in the disposition of various test molecules. -
Proton pump inhibitor
Esomeprazole Magnesium trihydrate is a proton pump inhibitor which reduces acid secretion through inhibition of the H+ / K+ ATPase in gastric parietal cells. -
Na+,K+-ATPase inhibitor
Istaroxime (PST2744) is a potent inhibitor of Na+,K+-ATPase with IC50 of 0.11 μM. -
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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Sodium Channel inhibitor
Sodium Channel inhibitor 1, one of 3-Oxoisoindoline-1-carboxamides, is a novel and selective voltage-gated sodium channel for pain treatment. -
P-gp inhibitor
Zosuquidar is a potent modulator of P-glycoprotein-mediated multi-drug resistance with Ki of 60 nM. -
elastogenesis inhibitor
L-Ascorbic acid (L-Ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid inhibits selectively Cav3.2 channels with an IC50 of 6.5 μM. L-Ascorbic acid is also a collagen deposition enhancer and an elastogenesis inhibitor. -
CaCCs Inhibitor
CaCCinh-A01 inhibits CaCC currents in human bronchial and intestinal cells. Also inhibits TMEM16A channels (IC50 = 2.1 uM, in TMEM16A-expressing FRT cells).