human eaat2

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

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].

DL-TBOA ammonium is a potent, non-transportable inhibitor of excitatory amino acid transporters. Its inhibitory effects are demonstrated by IC50 values of 70 μM, 6 μM, and 6 μM for excitatory amino acid transporter-1 (EAAT1), EAAT2, and EAAT3, respectively. Additionally, DL-TBOA ammonium significantly hampers the uptake of [14C]glutamate in COS-1 cell lines expressing human EAAT1 and EAAT2, evident by Ki values of 42 μM and 5.7 μM, respectively. Furthermore, this compound competitively blocks EAAT4 and EAAT5, with Ki values of 4.4 μM and 3.2 μM, respectively.

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.

SN05 is a potent inhibitor of amino acid transport (AAT) that can be used in anticancer research. The Ki values of SN05 for human ASCT1, rat ASCT2, human ASCT2, EAAT1, EAAT2, EAAC1 and EAAT5 is 2.77 μM, 0.73 μM, 0.87 μM, 3.7 μM, 7.25 μM, 7.23 μM and 2.22 μM, respectively [1].

SN40 is a potent amino acid transport (AAT) inhibitor relevant for anticancer research, with Kis of 7.29 μM, 2.42 μM, 2.94 μM, 5.55 μM, 24.43 μM and 5.55 μM for human ASCT1, rat ASCT2, human ASCT2, EAAT1, EAAT2, EAAC1 and EAAT5, respectively [1].

SN40 hydrochloride is a potent inhibitor of amino acid transport (AAT), exhibiting inhibitory constants (Kis) of 7.29 μM, 2.42 μM, 2.94 μM, 5.55 μM, 24.43 μM, and 5.55 μM for rat ASCT2, human ASCT2, EAAT1, EAAT2, EAAC1, and EAAT5, respectively. It is utilized in cancer research. [1]