transporter

BAY-876 is an orally active, selective inhibitor of glucose transporter 1 (GLUT1, IC50= 2 nM), exhibiting over 130-fold greater selectivity for GLUT1 than GLUT2, GLUT3, and GLUT4. It also inhibits glycolytic metabolism and ovarian cancer growth.

KL-11743 specifically blocks glucose metabolism, triggering an acute collapse in NADH pools and a striking accumulation of aspartate, indicating a dramatic shift toward oxidative phosphorylation in the mitochondria.

Cinromide (trans-3-Bromo-N-ethylcinnamamide) is used as a novel anticonvulsant agent.

D-Carnitine hydrochloride ((S)-Carnitine Hydrochloride) is a component of striated muscle and liver, used therapeutically to stimulate gastric and pancreatic secretions and to treat hyperlipoproteinemias.

Tormentic acid is a natural product. It has anticancer, anti-inflammatory, anti-atherogenic , anti-allodynic, and hepatoprotective properties,

Venuloside A (ESK246), a monoprostane glycoside from Pittosporum venulosum, is a LAT3 inhibitor and a leucine uptake inhibitor that inhibits the transporter of leucine through LAT3, and may be used in the study of prostate cancer.

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.

Brilliant Yellow (Direct Yellow 4) is a potent and selective VGLUT inhibitor, a dye that is photodegradable.

Telaglenastat (CB 839) (IC50 of 24 nM), an effective, specific, and oral inhibitor, which is bioavailable glutaminase, for recombinant human GAC.

WAY-213613 hydrochloride is a potent, selective nonsubstrate reuptake inhibitor of GLT-1 EAAT2 with IC 50 of 85 nM. WAY-213613 hydrochloride inhibits EAAT1 and EAAT3 with IC50 values of 5 and 3.8 microM, respectively. WAY-213613 hydrochloride shows no activity at ionotropic and metabotropic glutamate receptors. It is a potential tool for the elucidation of EAAT2 function and can be used for the research of central nervous system [1] [2].

Gentianine is an effective Swertiamarin derivative, which has anti-diabetic, antipsychotic, anti-inflammatory, hypotensive, diuretic and other effects, and has the potential to be developed into a safe antihypertensive drug.

Homoeriodictyol, a naturally occurring, bitter-masking flavanone, as a promising agent to increase appetite and food intake. The flavanone homoeriodictyol can increase SGLT-1-mediated glucose uptake but decrease serotonin release in differentiated Caco-2 cells.

Marein shows neuroprotective effect on PC12 cell damage induced by methylglyoxal, which is due to a reduction of damage to mitochondria function and activation of the AMPK signal pathway, it may be a potent compound for preventing counteracting diabetic e

STF-31 is an inhibitor of glucose transporter 1 (GLUT1) with IC50 of 1 μM.

WZB117 is a Glucose Transporter 1 (GLUT1) inhibitor. when IC50 of WZB117 approximate 10 μM, it inhibits lung cancer A549 cells and breast cancer MCF7 cells proliferation.

DL-TBOA is an inhibitor of excitatory amino acid transporter proteins, inhibiting excitatory amino acid transporter protein 1 (EAAT1), EAAT2, and EAAT3.

IPN60090 is a novel, potent, orally bioavailable, renal-type glutaminase (GLS1)-specific inhibitor with an IC50 value of 31 nM for GLS1. IPN60090 has potential anticancer and immunostimulant immunomodulatory activity, selectively targets, binds, and inhibits human glutaminase, and can be used to study GLS1-mediated diseases.

SLC26A3-IN-1 is an inhibitor of the anion-exchange protein SLC26A3 with an IC50 value of 340 nM. SLC26A3, a solute carrier (SLC) protein and member of the SLC26 family, exhibits a wide range of anionic specificities for chloride, bicarbonate, sulfate, and oxalate. Downregulated in adenomas (DRA), SLC26A3 is involved in intestinal absorption of chloride and oxalate and is associated with chloride-losing diarrhea.

LDN-212320 (OSU-0212320) is a glutamate transporter EAAT2 activator. It also enhances EAAT2 levels by > 6 fold at concentrations < 5 μM after 24 h.

Rhoifolin (Apigenin 7-O-neohesperidoside) is extracted from Turpinia arguya Seem dried leaves.

Fraxin (Fraxoside) is a glucoside of fraxetin.

BPTES(IC50 of 0.16 μM) is an effective and specific GlutamiN Ase GLS1 (KGA) inhibitor.

GT 949 is a selective excitatory positive allosteric modulator of amino acid transporter-2 (EAAT2) with an EC50 of 0.26 nM.

DRB18 is a highly effective pan-class inhibitor of glucose transporter proteins (GLUT). It significantly modulates energy-related metabolism in A549 cells by inducing alterations in the abundance of metabolites associated with glucose-related pathways. DRB18 exerts its effects by promoting G1 S phase arrest, increasing oxidative stress, and prompting necrotic cell death, ultimately displaying notable anti-tumor activity [1].