transporter

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

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.

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.

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.

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

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.

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

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.

Jujuboside A, a glycoside extracted from Semen Ziziphi Spinosae, exhibits neurophysiological inhibitory effects and is considered a potential therapeutic agent for the treatment of Alzheimer’s disease.

1.(-)-Licarin B (Licarine B) has anti-mycobacterial activity.

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].

MitoPQ (MitoParaquat) is a mitochondria-targeted small molecule compound that selectively enhances mitochondrial superoxide and hydrogen peroxide levels and inhibits insulin-stimulated glucose uptake and translocation of glucose transport protein 4 (GLUT4) to the plasma membrane in adipocytes and myotubes.MitoPQ can be used to MitoPQ can be used to study mitochondrial oxidative stress and regulated GLUT4 transporter.

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.

Fraxin (Fraxoside) is a glucoside of fraxetin.

Tetramethylkaempferol is a PPARγ agonist, it can improve insulin sensitivity by increasing the levels of adiponectin, an important adipocytokine associated with insulin sensitivity in adipose tissue. Tetramethylkaempferol can concentration-dependently enh

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.

Troriluzole is an orally active glutamate modulator with anticancer activity.Troriluzole enhances the expression of excitatory amino acid transporters located in glial cells and is used in the study of spinocerebellar ataxia, Alzheimer's disease, and generalized anxiety disorder (GAD).

Lavendustin B is a Tyrosine Kinase Inhibitor and an inhibitor of HIV-1 integrase (IN) interaction with its cognate cellular cofactor, lens epithelium-derived growth factor (LEDGF p75).

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.

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

Nepodin has antimalarial, and anti-inflammatory activities, it shows significant cyclooxygenase (COX) inhibitory activity. Nepodin has an antidiabetic effect, which is at least partly mediated by stimulation of GLUT4 translocation via AMPK activation by n

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].

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.

T-1095 is an inhibitor of renal glucose reabsorption and the expression of Na+-glucose cotransporters (SGLTs) and facilitative glucose transporter 2 (GLUT2).

GLUT4-IN-2 is a specific GLUT4 inhibitor that inhibits GLUT1 and GLUT4.GLUT4-IN-2 has antitumor activity, induces apoptosis and cell cycle arrest, and can be used for cancer research.

MSNBA is a selective and potent inhibitor of fructose transport through GLUT5 and also acts as a probe of the GLUT5 transporter. MSNBA inhibited GLUT5 fructose uptake in MCF7 cells with KI of 3.2±0.4 μM.

SW157765 is a selective glucose transporter GLUT8 (SLC2A8) inhibitor, a prodrug of many compounds, that selectively inhibits the uptake of fluorescent 2-deoxyglucose (2DG) in SW157765-sensitive cells in a dose-dependent manner, and can be used for the study of lung cancer.

Glutaminase-IN-1 (CB839 derivative), a novel 1,3,4-selenodiazepine inhibitor of the renal-type glutaminase (KGA) variant, exhibited antitumor activity in an aggressive H22 hepatocellular carcinoma xenograft model.

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

Procyanidin A2 is a potential precursor of 5-(3',4'-dihydroxyphenyl)-γ-valerolactone, exhibits antioxidant, anti-inflammary, anti-hyperglycemia, and anti-type 2 diabetes activities. Procyanidin A2 demonstrates liver cell regenerative activity in scratch w

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

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

UCPH-101 is an inhibitor of excitatory amino acid transporter subtype 1 (EAAT1) with an IC50 of 0.66 μM.

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

EAAT2 activator 1 (3-[(2-Chloro-6-fluorobenzyl)thio]-6-pyridin-2-ylpyridazine) is a thiopyridazine derivative that has been found to increase EAAT2 protein levels in astrocytes.

Dodoviscin J can promote adipocyte differentiation as characterized by increased triglyceride levels in 3T3L1 cells.

Dodoviscin I can promote adipocyte differentiation as characterized by increased triglyceride levels in 3T3L1 cells.

Ficusin has antioxidant, antilipidemic and antidiabetic effects, it can lower the levels of fasting blood glucose, plasma insulin, body weight gain in HFD-STZ induced diabetic rats, and can significantly enhance the PPARγ expression and improve the transl

Dodoviscin A may be a new promising pigmentation-altering agent for cosmetic and therapeutic applications, it can inhibit melanin biosynthesis induced by 3-isobutyl-1-methylxanthine and PD98059.Dodoviscin A can promote adipocyte differentiation as charact

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.

Sennidin A, has two hydroxyanthraquinone-like moieties, exerts inhibition on NS3 helicase with IC50 values of 0.8 μM.

Sennidin B stimulates glucose incorporation in rat adipocytes.

GLUT inhibitor-1 is an orally active GLUT inhibitor with IC50 s of 242 nM and 179 nM for GLUT1 and GLUT3. GLUT inhibitor-1 can be used in studies about cancers and autoimmune diseases.

WAY-213613 is a potent and selective nonsubstrate reuptake inhibitor of GLT-1 EAAT2 (IC50: 85 nM EAAT2), displaying 59- and 44-fold selectivity over EAAT1 and EAAT3 (IC50s: 5 and 3.8 μM, respectively). WAY-213613 shows no activity at ionotropic and metabotropic glutamate receptors.

1β-Hydroxy-2-oxopomolic acid inhibits adipocyte differentiation through downregulation of various adipocytokines by blocking PPARγ and C/EBPα expression.

Dodoviscin H can promote adipocyte differentiation as characterized by increased triglyceride levels in 3T3L1 cells.