2. Signaling Pathways
  3. Membrane Transporter/Ion Channel
  4. ASCT
  5. ASCT2 Isoform

ASCT2

ASCT2 (SLC1A5) is a sodium-dependent neutral amino acid transporter that primarily mediates glutamine exchange across the plasma membrane and maintains intracellular amino acid homeostasis through an antiport mechanism[1]. ASCT2 supports glutamine-dependent metabolic programs that regulate anabolic growth, amino acid balance, and signaling pathways linked to cellular proliferation[1][2]. Mechanistically, glutamine transported through ASCT2 contributes to tricarboxylic acid cycle fueling and provides substrates required for nucleotide, lipid, and non-essential amino acid biosynthesis, thereby supporting metabolic reprogramming in rapidly proliferating cells and tumors[1][3]. Increased ASCT2 expression is frequently observed in highly proliferative tissues and multiple cancers, where glutamine demand is elevated and transporter activity contributes to tumor growth and survival[1][2][4]. In experimental cancer models, genetic deletion or inhibition of ASCT2 reduces amino acid uptake and suppresses tumor growth, supporting its value as a functional target for studying glutamine-dependent metabolism[2][4]. Compared with the closely related isoform ASCT1 (SLC1A4), ASCT2 displays distinct substrate preferences and functions predominantly as a high-affinity glutamine transporter, highlighting its specialized role in cancer-associated nutrient utilization[1]. A mitochondrial SLC1A5 variant further expands ASCT2-related biology by transporting glutamine into mitochondria, where it promotes ATP production, glutathione synthesis, hypoxia adaptation, and metabolic reprogramming in cancer cells[5]. For experimental applications, pharmacological inhibitors such as GPNA and V-9302 are widely used to interrogate ASCT2-dependent glutamine transport, although inhibitor selectivity and off-target effects require careful interpretation of mechanistic studies[6][7].

ASCT2 Related Products (8):

Cat. No. Product Name Effect Purity
  • HY-112683
    V-9302
    		Antagonist 99.46%
    V-9302 is a competitive antagonist of transmembrane glutamine flux. V-9302 selectively and potently targets the amino acid transporter ASCT2 (SLC1A5) not ASCT1. V-9302 inhibits ASCT2-mediated glutamine uptake (IC50=9.6 μM) in HEK-293 cells.
  • HY-112683A
    V-9302 hydrochloride
    		Antagonist 99.10%
    V-9302 hydrochloride is a competitive antagonist of transmembrane glutamine flux. V-9302 hydrochloride selectively and potently targets the amino acid transporter ASCT2 (SLC1A5) not ASCT1. V-9302 hydrochloride inhibits ASCT2-mediated glutamine uptake (IC50=9.6 µM) in HEK-293 cells.
  • HY-W011391
    GPNA hydrochloride
    		Inhibitor 99.91%
    GPNA hydrochloride is a well known substrate of the enzyme γ-glutamyltransferase (GGT). GPNA hydrochloride is a specific glutamine (Gln) transporter ASCT2 inhibitor. GPNA hydrochloride also inhibit Na+-dependent carriers, such as SNAT family (SNAT1/2/4/5), and the Na+-independent leucine transporters LAT1/2. GPNA reversibly induces apoptosis in A549 cells.
  • HY-146242
    SN05
    		Inhibitor 98.03%
    SN05 is a potent amino acid transport (AAT) inhibitor with Ki values of 2.77 μM, 0.73 μM, 0.87 μM, 3.7 μM, 7.25 μM, 7.23 μM and 2.22 μM for hASCT1, rASCT2, hASCT2, EAAT1, EAAT2, EAAC1 and EAAT5, respectively. SN05 can be used in the study of cancer.
  • HY-163198
    ASCT2-IN-1
    		Inhibitor 98.21%
    ASCT2-IN-1 (compound 20k) is an ASCT2 inhibitor with IC50 values of 5.6 μM and 3.5 μM in cells A549 and HEK293, respectively. ASCT2-IN-1 induces cell apoptosis. ASCT2-IN-1 inhibits tumor growth.
  • HY-14889
    Fluciclovine
    Fluciclovine is an amino acid analogue that can enter cells by targeting the amino acid transporters on the cell surface (mainly ASCT2 and LAT1). After being labeled with ¹⁸F, ¹⁸F-fluciclovine can be used as an imaging agent for positron emission tomography (PET) for prostate diagnosis imaging.
  • HY-144354S
    S-Benzyl-DL-cysteine-2,3,3-d3
    		Inhibitor 99.90%
    S-Benzyl-DL-cysteine-2,3,3-d3 is a deuterium labeled Benzylcysteine. Benzylcysteine is an ASCT2 inhibitor that binds to ASCT2 with an apparent Ki of 780 μM. Benzylcysteine inhibit ASCT2 function based on a competitive mechanism, indicating that Benzylcysteine binds to the substrate-binding site of ASCT2.
  • HY-146241
    SN40
    		Inhibitor 99.26%
    SN40 is a potent amino acid transport (AAT) inhibitor with 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. SN40 can be used for researching anticancer.