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.

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].

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.

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.

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