transport inhibitor

Dapagliflozin ((2S)-1,2-propanediol, hydrate) (BMS-512148 (2S)-1,2-propanediol, hydrate) is a selective, orally active inhibitor of the renal sodium-glucose co-transporter type 2 (SGLT2), in development for treating type 2 diabetes mellitus (T2DM). It inhibits SGLT2, responsible for at least 90% of glucose reabsorption in the kidney.

N-Ethylmaleimide (NEM) is a reagent for alkylation of free sulfhydryl groups, a cysteine protease inhibitor used in experimental biochemistry. N-Ethylmaleimide is also a deubiquitinating enzyme inhibitor that specifically inhibits phosphate transport in mitochondria.

Ceftibuten dihydrate (Sch-39720 dihydrate) is the dihydrate form of ceftibuten, and is a third-generation cephalosporin with antibacterial activity.

Arprinocide is a hypoxanthine-guanine transport inhibitor.

Guanidinoethyl sulfonate (Taurocyamine) is a competitive glycine receptor antagonist.

D-Histidine is an enantiomer of L-histidine. L-Histidine is an inhibitor of mitochondrial glutamine transport and also an essential amino acid for infants.

Hexaflumuron is a chitin synthesis inhibitor used to bait and eliminate termite colonies. Termites are unable to metabolize hexaflumuron and clearance is slow, resulting in up to 100% elimination. Hexaflumuron has also been tested for use with the raisin

Rotenone (Rotocide) is a natural product and a botanical insecticide. Rotenone is a mitochondrial electron transport complex I inhibitor that promotes the production of reactive oxygen species in mitochondria and induces apoptosis.

7-Methoxy-1-naphthaleneacetic acid is an inhibitor of auxin action in plants. 7-Methoxy-1-naphthaleneacetic acid inhibits polar auxin transport and tropic responses associated with asymmetric auxin distribution in Arabidopsis and maize. 7-Methoxy-1-naphthaleneacetic acid inhibits auxin transport mediated by AUX1, PIN, and ABCB proteins expressed in yeast.

Malonic acid (propanedioic acid) is the archetypal example of a competitive inhibitor: it acts against succinate dehydrogenase (complex II) in the respiratory electron transport chain. Malonic acid is found to be associated with malonyl-CoA decarboxylase deficiency, which is an inborn error of metabolism.

Metamitron is a photosynthetic electron transport chain inhibitor and can be used as a chemical thinner.

Proteinase K (Protease K) is a non-specific serine protease that can tolerate changes in SDS, urea, pH (4-12), salt concentration, and temperature. Proteinase K hydrolyzes a wide range of peptide bonds and is used for protein digestion.

Phloretin (NSC-407292) is a well-known inhibitor of eukaryotic urea transporters, blocks VacA-mediated urea and ion transport. Phloretin is a dihydrochalcone, a type of natural phenols. It can be found in apple tree leaves and the Manchurian apricot. It promotes potent antioxidative activities in peroxynitrite scavenging and the inhibition of lipid peroxidation. It has been found to inhibit the growth of several cancer cells and induce apoptosis of B16 melanoma and HL60 human leukemia cells.

(Iso)-WAY-260022 ((Iso)-NRI-022) is a stereoisomer of WAY-260022, a norepinephrine reuptake inhibitor and selective inhibitor of 5-hydroxytryptamine and dopamine transport proteins.

Diflufenzopyr (SAN 835H), an auxin transport inhibitor, is semicarbazone-type.

Hexazinone is a broad-spectrum herbicide from the triazine family. Hexazinone inhibits photosynthesis through binding to the D-1 quinone protein of the electron transport chain in photosystem II.

Adamantanine (NSC-145160) is an amino acid transport inhibitor.

MCT1-IN-3 is a monocarboxylate transporter 1 (MCT1) inhibitor, targeting solute carrier (SLC) monocarboxylate transporter 1 (MCT1; SLC16A1) for cancer treatment. MCT1-IN-3 (compound 24) showed the highest MCT1 transport inhibition with an IC50 value of 81.0 Nm and also exhibits significant inhibitory activity against the multidrug transporter ABCB1.

Sulfosuccinimidyl oleate (Sulfo-N-succinimidyl oleate) is a long-chain fatty acid that inhibits fatty acid transport into cells. It is a potent and irreversible inhibitor of the mitochondrial respiratory chain and binds the CD36 receptor on the surface of microglia. Sulfosuccinimidyl oleate is neuroprotective and alleviates stroke-induced neuroinflammation [1] [2].

Sulfosuccinimidyl oleate sodium (Sulfo-N-succinimidyl oleate sodium) is a long-chain fatty acid that inhibits the transport of fatty acids to cells, acts as an effective irreversible inhibitor of the mitochondrial respiratory chain, and binds to CD36 receptors on the surface of microglia.

Celiprolol hydrochloride (Selectrol) is a cardioselective beta-1 adrenergic antagonist that has intrinsic sympathomimetic activity. It is used in the management of ANGINA PECTORIS and HYPERTENSION.

Maralixibat Chloride (LUM001 chloride), an apical, sodium-dependent, bile acid transport inhibitor, prevents enterohepatic bile acid recirculation.

(Rac)-AMXT-1501 4HCl is a polyamine transport inhibitor that inhibits polyamine transport and acts synergistically with cisplatin in HNSCC. (Rac)-AMXT-1501 4HCl has potential antimicrobial activity and inhibits neuroblastoma cell proliferation and pneumococcal pod biosynthesis by targeting ornithine decarboxylase and polyamine transport.

AU1235 is a Mycobacterium tuberculosis inhibitor.

Importazole is an inhibitor of the nuclear transport receptor importin-β.

Oligomycin is an antifungal antibiotic that is an inhibitor of H+-ATP synthetase. The Oligomycin blocks oxidative phosphorylation and the electron transport chain. Oligomycin inhibited HIF-1alpha expression in hypoxic tumor cells.

SL327 is a selective inhibitor for MEK1/2 with IC50 of 0.18 μM/0.22 μM; able to transport through the blood-brain barrier.

α-Cyano-4-hydroxycinnamic acid (α-CHCA) is an inhibitor of monocarboxylate transporter 1 (MCT1), which blocks pyruvate transport in rat heart mitochondria (IC50: 1.5 μM).

GSK137647A (GSK 137647) is a selective agonist of FFA4.

Lipofermata, a fatty acid transport protein (FATP) inhibitor, prevents lipid transport to melanoma cells and reduces their growth and invasion.

IACS-010759 is an orally bioavailable inhibitor of complex I of oxidative phosphorylation of the mitochondrial electron transport chain.

U18666A is a cell-permeable drug and is a cholesterol synthesis and transport inhibitor. It inhibits replication of Ebola virus, dengue virus, and human hepatitis C virus.

MitoBloCK-11 (MB-11) is a s mall molecule inhibitor of mitochondrial protein import possibly acts through transport protein Seo1, but not Tom70 or Tom20; inhibits precursor proteins that contain hydrophobic segments, confers growth in media lacking uracil in a specific manner and affects zebrafish development.

CHIR-98014 (CT98014) is a selective GSK3 inhibitor; potentiate insulin activation of glucose transport and utilization in vitro and in vivo.

Spastazoline is a potent and selective inhibitor of spastin(Human spastin with IC50 of 99 nM ).

Anthracene-9-carboxylic acid is an inhibitor of chloride transport with a moderate to strong inhibitory action on PKA activated cardiac IcI.

Antimalarial agent 14 (NSC-102533) is a bioactive chemical.

Fasentin (N-[4-chloro-3-(trifluoromethyl)phenyl]-3-oxobutanamide) is an inhibitor of GluT1.

Tenatoprazole (TU-199), a prodrug of the proton pump inhibitor (PPI) class, can inhibit proton transport (IC50: 3.2 μM).

(S)-SNAP5114 is a selective inhibitor of GABA transport, exhibiting IC50 values of 5 μM for hGAT-3 and 21 μM for rGAT-2, and possesses anticonvulsant properties.

1. Atractyloside potassium salt (Atractyloside Dipotassium Salt) inhibits oxidative phosphorylation by blocking the transfer of adenosine nucleotides through the mitochondrial membrane.

LY2183240 inhibits fatty acid amide hydrolase (FAAH) activity (IC50 = 12.4 nM). LY2183240 is a novel and highly effective blocker of anandamide uptake (IC50 = 270 pM).

Compound 5C, referred to as Pkm2-in-4, is a selective PKM2 inhibitor (IC50 = 0.35 µM) that modulates pyruvate-dependent respiration and promotes mitochondrial H2O2 production rate and electron transport system coupling [1].

Phenylarsine Oxide (Oxophenylarsine) is a membrane-permeable tyrosine phosphatase inhibitor with an IC50 value of 18 µM that stimulates 2-deoxyglucose transport in insulin-resistant human skeletal muscle.

3',4'-Dichlorobenzamil HCl is an inhibitor of Na+ transport, Na+/Ca2+ exchanger, sarcoplasmic reticulum Ca2+ release channels.

6,8-Diprenylnaringenin (Senegalensin) is a natural product from hop Humulus lupulus. 6,8-Diprenylnaringenin is a breast cancer resistance protein(BCRP) inhibitor with some estrogenicity.

L594881, also known as 3',4'-Dichlorobenzamil or DCB, is an inhibitor of Na+/Ca2+ exchanger, Na+ transport and sarcoplasmic reticulum Ca2+ release channels. L594881 can inhibit Na+/Ca2+ exchanger, Na+ transport and sarcoplasmic reticulum Ca2+ release channels.

AMXT1501 is a polyamine uptake inhibitor, also inhibiting the putrescine transport in epimastigotes (the insect stage of t. cruzi)

Tetrabenazine D6 is the deuterium-labeled Tetrabenazine. Tetrabenazine is a VMAT-inhibitor used for the treatment of hyperkinetic movement disorder.

Tetrabenazine methanesulfonate is a medicine formerly utilized as an antipsychotic and therapy for various movement disorders. Tetrabenazine methanesulfonate blocks neurotransmitter uptake into adrenergic storage vesicles and has been used as a high-affin

Tetrabenazine Racemate (Rubigen) is a selective and reversible inhibitor of vesicular monoamine transporter-2 (VMAT-2). Tetrabenazine Racemate blocks neurotransmitter uptake into adrenergic storage vesicles and has been used as a high-affinity label for the vesicle transport system.

(+)-Tetrabenazine ((3R,11bR)-Tetrabenazine) is a reversible vesicular monoamine transporter 2 (VMAT-2) inhibitor, inhibits transport by VMAT2 with 10-fold greater potency than transport by VMAT1.

Tetrabenazine (Ro 1-9569) is a former antipsychotic drug used to treat various movement disorders. It inhibits neurotransmitter uptake into adrenergic storage vesicles and serves as a high-affinity label for the vesicle transport system.