GLPBio

BCH (LAT1-IN-1)

Catalog No.: GC16516Purity:>95.00%Synonyms: 2-amino-2-Norbornanecarboxylic Acid
COASDSData Sheet
BCH (BCH) es un inhibidor selectivo y competitivo del transportador de aminoÁcidos neutros grandes 1 (LAT1) que inhibe significativamente la absorciÓn celular de aminoÁcidos y la fosforilaciÓn de mTOR, lo que induce la supresiÓn del crecimiento del cÁncer y la apoptosis.

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BCH (LAT1-IN-1)
Cas No.: 20448-79-7
10mM (in 1mL Water)In Stock
$53.00
1
50mgIn Stock
$48.00
1
100mgIn Stock
$80.00
1
Tel: (909) 407-4943 / (909) 689-7124Email: sales@glpbio.com

Citas (Citations)

1 publicationsPublicaciones de investigadores que utilizan este producto
IF 10

Descripción (Description)

BCH (LAT1-IN-1) is a selective and competitive inhibitor of the L-type amino acid transporter 1 (LAT1). BCH inhibits cancer cell growth and induces apoptosis by suppressing cellular amino acid uptake and mTOR phosphorylation. BCH can be used in research related to cancers such as esophageal cancer[1-4].

In vitro, BCH (10mM) treated endometrial cancer cell lines (Ishikawa, RL95-2, HEC1A, KLE) for 15 minutes to 8 days. BCH significantly inhibited cellular leucine uptake; it suppressed cell growth and spheroid formation while reducing mTORC1 signaling pathway activation[5]. BCH (0.3–50mM) treated KB human oral epidermoid carcinoma cells, Saos2 human osteosarcoma cells, and C6 rat glioma cells for 0–3 days. BCH significantly inhibited cell growth and induced DNA fragmentation, apoptosis, and activation of caspase-3/7[6].

In vivo, BCH (240mg/kg) was intraperitoneally injected into HFD/STZ-induced T2DM and db/db mouse models for one week. BCH alleviated diabetic neuropathic pain symptoms[7]. BCH (200mg/kg) was intravenously injected into BALB/c nude mice inoculated with HuCCT1 cholangiocarcinoma cells for 14 days. BCH significantly suppressed tumor growth and enhanced the therapeutic efficacy of gemcitabine and 5-FU[8].

References:
[1] Ohshima Y, Kaira K, Yamaguchi A, et al. Efficacy of system l amino acid transporter 1 inhibition as a therapeutic target in esophageal squamous cell carcinoma. Cancer Sci. 2016 Oct;107(10):1499-1505.
[2] Singh N, Scalise M, Galluccio M, et al. Discovery of Potent Inhibitors for the Large Neutral Amino Acid Transporter 1 (LAT1) by Structure-Based Methods. Int J Mol Sci. 2018 Dec 21;20(1):27.
[3] Wang Q, Holst J. L-type amino acid transport and cancer: targeting the mTORC1 pathway to inhibit neoplasia. Am J Cancer Res. 2015 Mar 15;5(4):1281-94.
[4] Lee Y, Jin C, Ohgaki R, et al. Structural basis of anticancer drug recognition and amino acid transport by LAT1. Nat Commun. 2025 Feb 14;16(1):1635.
[5] Marshall AD, van Geldermalsen M, Otte NJ, et al. LAT1 is a putative therapeutic target in endometrioid endometrial carcinoma. Int J Cancer. 2016 Dec 1;139(11):2529-39.
[6] Kim CS, Cho SH, Chun HS, et al. BCH, an inhibitor of system L amino acid transporters, induces apoptosis in cancer cells. Biol Pharm Bull. 2008 Jun;31(6):1096-100.
[7] Zhou ZY, Wang JY, Li ZX, et al. Branched-Chain Amino Acids Deficiency Promotes Diabetic Neuropathic Pain Through Upregulating LAT1 and Inhibiting Kv1.2 Channel. Adv Sci (Weinh). 2024 Sep;11(33):e2402086.
[8] Kaira K, Sunose Y, Ohshima Y, et al. Clinical significance of L-type amino acid transporter 1 expression as a prognostic marker and potential of new targeting therapy in biliary tract cancer. BMC Cancer. 2013 Oct 16;13:482.

Protocolo (Protocol)

Cell experiment [1]:

Cell lines

KB human oral epidermoid carcinoma cells, Saos2 human osteogenic sarcoma cells, C6 rat glioma cells

Preparation Method

KB cells were grown in MEM containing NEAA (non-essential amino acids) at a ratio of 100:1, supplemented with 5% FBS. Saos2 cells and C6 cells were grown in DMEM supplemented with 10% FBS. All cells were maintained as monolayers at 37°C in a humidified atmosphere containing 5% CO₂. Cells were treated with BCH at concentrations of 0.3, 1, 3, 10, 20, and 50mM for 0-3 days.

Reaction Conditions

0.3-50mM; 0-3 days.

Applications

BCH significantly inhibited cell growth in a time- and dose-dependent manner, with IC₅₀ values of 6.9±0.4mM (KB, 3 days), 5.6±0.7mM (Saos2, 3 days), and 6.5±0.9mM (C6, 3 days). BCH treatment induced internucleosomal DNA fragmentation, increased the number of TUNEL-positive cells, and promoted proteolytic cleavage of procaspase-7 in all three cell types, as well as procaspase-3 in KB and C6 cells, indicating activation of caspase-3/7 and induction of apoptotic cell death.

Animal experiment [2]:

Animal models

BALB/c nude mice

Preparation Method

HuCCT1 cells (1x10⁷ cells) were inoculated subcutaneously into the flank of the mice. After tumor volumes reached approximately 100mm³, mice were divided into control and treatment groups (n=10). The treatment groups mice treated with BCH (200mg/kg) for 14 days.

Dosage form

200mg/kg; i.v.; once daily for 14 days.

Applications

BCH significantly suppressed growth of the tumor and yielded an additive therapeutic efficacy to gemcitabine and 5-FU.

References:
[1] Kim CS, Cho SH, Chun HS, et al. BCH, an inhibitor of system L amino acid transporters, induces apoptosis in cancer cells. Biol Pharm Bull. 2008 Jun;31(6):1096-100.
[2] Kaira K, Sunose Y, Ohshima Y, et al. Clinical significance of L-type amino acid transporter 1 expression as a prognostic marker and potential of new targeting therapy in biliary tract cancer. BMC Cancer. 2013 Oct 16;13:482.

Documentos del producto (Product Documents)

Purity:>95.00%Appearance:A solid
COASDSData Sheet

Propiedades químicas (Chemical Properties)

N.º CAS
20448-79-7
Sinónimos
2-amino-2-Norbornanecarboxylic Acid
Nombre químico
(1S,2S,4R)-2-aminobicyclo[2.2.1]heptane-2-carboxylic acid
SMILES
OC([C@]1([C@@H](CC2)C[C@@H]2C1)N)=O
Fórmula molecular
C8H13NO2
Peso molecular
155.2
Solubilidad
10mg/mL in PBS, pH 7.2
Almacenamiento
Store at -20°C
Consejos generales
Seleccione un disolvente adecuado según los datos de solubilidad del producto. Una vez preparada, divida la solución madre en alícuotas para evitar ciclos repetidos de congelación y descongelación.
Utilice las soluciones madre en un plazo de 6 meses si se conservan a -80°C, o de 1 mes si se conservan a -20°C.
Para mejorar la solubilidad, caliente el tubo a 37°C y soníquelo durante un periodo adecuado.
Condiciones de envío
Las muestras de evaluación se envían con acumuladores de frío. Los demás tamaños se envían a temperatura ambiente o, previa solicitud, con acumuladores de frío.

Calculadoras (Calculators)Molaridad / Dilución / Peso molecular / Conversión de unidades / Formulación in vivo / Solubilidad

g/mol

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