1. Signaling Pathways
  2. Membrane Transporter/Ion Channel
  3. ASCT

ASCT

Alanine Serine Cysteine Transporters

ASCT (Alanine Serine Cysteine Transporters) belongs to the SLC1 family and functions as a membrane protein responsible for the transport of neutral amino acids, including ASCT1 (SLC1A4) and ASCT2 (SLC1A5). ASCTs mediate Na+-dependent amino acid exchange but do not utilize the Na+ gradient as a driving force; instead, they maintain homeostasis by exchanging amino acids between the intracellular and extracellular environments. ASCT1 and ASCT2 exhibit different substrate selectivities, with ASCT1 showing a higher affinity for alanine and serine, whereas ASCT2 can also transport glutamine, playing a crucial role in tumor metabolism. ASCT2 is highly expressed in various tumor tissues, where it facilitates glutamine uptake, supplying nitrogen and energy to rapidly proliferating cancer cells, making it a potential target for cancer therapy. In contrast, ASCT1 is primarily associated with neurological disorders, as mutations in the SLC1A4 gene can lead to intellectual disability, postnatal microcephaly, spasticity, and thinning of the corpus callosum. ASCTs provide new strategies for research in both cancer and neurological diseases[1].

ASCT Isoform Specific Products:

Cat. No. Product Name Effect Purity Chemical Structure
  • 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.
    V-9302
  • 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.
    V-9302 hydrochloride
  • 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.
    GPNA hydrochloride
  • HY-I1070
    D-Isoleucine
    Agonist 99.83%
    D-Isoleucine is a selective competitive activator of the Asc-1 antiporter (Ki=0.98 mM). D-Isoleucine promotes the release of D-serine and glycine by binding to the Asc-1 protein on the neuronal cell membrane, and enhances NMDA receptor-dependent synaptic plasticity. D-Isoleucine can be used in the study of neurodegenerative diseases (such as Alzheimer's disease and schizophrenia). D-Isoleucine also acts as a non-classical D-amino acid, interferes with bacterial peptidoglycan synthesis, and inhibits the formation of Staphylococcus aureus biofilm, and has potential antibacterial application value[1][2].
    D-Isoleucine
  • HY-N2518
    Agnuside
    Inhibitor 99.90%
    Agnuside is used in the study of asthma, inflammation, and angiogenic diseases. Agnuside is an orally active compound that can be extracted from Vitex negundo.
    Agnuside
  • 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.
    Fluciclovine
  • HY-P11756
    P-LPK
    Ligand
    P-LPK is a dodecapeptide that specifically targets SLC1A5, which is highly expressed on the membrane of colorectal cancer cells, with a Kd value of 1.19 μM. P-LPK has no intrinsic cell proliferation regulatory activity. Gallium-68-labeled P-LPK selectively accumulates at colorectal cancer tumor sites in xenograft mouse models. P-LPK can serve as a targeted carrier to deliver Camptothecin (HY-16560) to colorectal cancer cells, forming the conjugate P-LPK-CPT. P-LPK can be used in the research of colorectal cancer.
    P-LPK
  • HY-78162
    cis-3-Hydroxyproline
    Substrate
    cis-L-3-Hydroxyproline is an Alanine-Serine-Cysteine transporter 2 (ASCT2, SLC1A5) substrate that can induces inwardly-directed anion current, and forms key interactions with ASCT2 binding site residues including Asn471.cis-L-3-Hydroxyproline can be used for the research of melanoma.
    cis-3-Hydroxyproline
  • 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.
    SN05
  • HY-120170
    BMS-466442
    Inhibitor 98.0%
    BMS-466442 is a potent and selective inhibitor of asc-1 (alanine serine cysteine transporter-1), with an IC50 of 11 nM. BMS-466442 inhibits [3H] D-serine uptake into rat brain synaptosomes, with an IC50 of 400 nM. BMS-466442 can be used for schizophrenia research.
    BMS-466442
  • 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.
    ASCT2-IN-1
  • HY-34611
    Boc-L-2,4-Diaminobutyric acid
    Ligand 98.0%
    Boc-L-2,4-Diaminobutyric acid (N-Boc-L-2,4-diaminobutyric acid; Boc-Dab-OH) is a versatile synthetic starting material with a cleavable protecting group. Boc-L-2,4-Diaminobutyric acid not only reduces the backbone cleavage rate by protecting the side-chain γ-amino group, but also triggers intramolecular cyclization of self-immolative linkers under acidic cleavage conditions, thus constructing stimuli-responsive materials. Boc-L-2,4-Diaminobutyric acid is also an important building block for bioactive molecules. It can be used in the synthesis of ASCT2 (SLC1A5) inhibitors and carboxynorspermine, and can also serve as an internal standard to support the quantitative detection of specific intracellular amino acids by UPLC-QQQ-MS.
    Boc-L-2,4-Diaminobutyric acid
  • HY-163199
    ASCT2-IN-2
    Inhibitor 99.10%
    ASCT2-IN-2 (compound 25e) is an ASCT2 inhibitor with IC50 of 5.14 μM. ASCT2-IN-2 regulates amino acid metabolism as well as mTOR signaling and thereby induces cell apoptosis. ASCT2-IN-2 inhibits tumor growth.
    ASCT2-IN-2
  • 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.
    S-Benzyl-DL-cysteine-2,3,3-d<sub>3</sub>
  • 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.
    SN40
  • HY-146241B
    SN40 hydrochloride
    Inhibitor 98.00%
    SN40 hydrochloride 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 hydrochloride can be used for researching anticancer.
    SN40 hydrochloride
  • HY-120139A
    (R)-KMH-233
    Control
    (R)-KMH-233 is the isomer of KMH-233 (HY-120139), and can be used as an experimental control. KMH-233, a potent, reversible and selective l-type amino acid transporter 1 (LAT1) inhibitor, inhibits the uptake of LAT1 substrate, l-leucin (IC50=18 μM) as well as cell growth. KMH-233 significantly potentiates the efficacy of Bestatin and Cisplatin even at low concentrations (25 μM).
    (R)-KMH-233
  • HY-N2518R
    Agnuside (Standard)
    Inhibitor
    Agnuside (Standard) is the analytical standard of Agnuside. This product is intended for research and analytical applications. Agnuside is used in the study of asthma, inflammation, and angiogenic diseases. Agnuside is an orally active compound that can be extracted from Vitex negundo.
    Agnuside (Standard)
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