GLPBio

BCH (LAT1-IN-1)

Catalog No.: GC16516Purity:>95.00%Synonyms: 2-amino-2-Norbornanecarboxylic Acid
BCH (BCH) هو مثبط انتقائي وتنافسي لناقل الأحماض الأمينية المحايدة الكبيرة 1 (LAT1) يمنع بشكل كبير الامتصاص الخلوي للأحماض الأمينية و mTOR الفسفرة ، مما يؤدي إلى قمع نمو السرطان وموت الخلايا المبرمج.

المنتجات مخصصة للاستخدام البحثي فقط، وليست للاستخدام البشري. نحن لا نبيع للمرضى.


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

المراجع (Citations)

1 publicationsمنشورات الباحثين الذين استخدموا هذا المنتج
IF 10

الوصف (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.

البروتوكول (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.

وثائق المنتج (Product Documents)

Purity:>95.00%Appearance:A solid

الخصائص الكيميائية (Chemical Properties)

رقم CAS
20448-79-7
المرادفات
2-amino-2-Norbornanecarboxylic Acid
الاسم الكيميائي
(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
الصيغة الجزيئية
C8H13NO2
الوزن الجزيئي
155.2
الذوبانية
10mg/mL in PBS, pH 7.2
التخزين
Store at -20°C
إرشادات عامة
اختر مذيبًا مناسبًا وفقًا لبيانات ذوبانية المنتج. بعد التحضير، قسّم المحلول المخزون إلى أجزاء لتجنب دورات التجميد والذوبان المتكررة.
استخدم المحاليل المخزونة خلال 6 أشهر عند حفظها في -80°C، أو خلال شهر واحد عند حفظها في -20°C.
لتحسين الذوبانية، سخّن الأنبوب إلى 37°C وعرّضه للموجات فوق الصوتية لمدة مناسبة.
شروط الشحن
تُشحن عينات التقييم مع عبوات تبريد. وتُشحن الأحجام الأخرى المتاحة في درجة حرارة الغرفة، أو مع عبوات تبريد عند الطلب.

الحاسبات (Calculators)المولارية / التخفيف / الوزن الجزيئي / تحويل الوحدات / تركيبة داخل الجسم الحي / الذوبانية

g/mol

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