BCH (LAT1-IN-1)
(Synonyms: 2-氨基-2-去甲菠烷羧酸,2-amino-2-Norbornanecarboxylic Acid) 目录号 : GC16516
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BCH (LAT1-IN-1)是一种具有选择性和竞争性的L型氨基酸转运蛋白1（LAT1）抑制剂。
Cas No.:20448-79-7
Sample solution is provided at 25 µL, 10mM.
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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.
BCH (LAT1-IN-1)是一种具有选择性和竞争性的L型氨基酸转运蛋白1（LAT1）抑制剂。BCH通过抑制细胞对氨基酸的摄取和mTOR磷酸化来抑制癌细胞生长并诱导细胞凋亡。BCH可用于食管癌等癌症的相关研究[1-4]。
在体外，BCH（10mM）处理子宫内膜癌细胞系（Ishikawa、RL95-2、HEC1A、KLE）15分钟至8天。BCH显著抑制细胞对亮氨酸的摄取；BCH抑制细胞生长和球体形成，同时降低mTORC1信号通路激活[5]。BCH（0.3–50mM）处理KB人口腔表皮样癌细胞、Saos2人骨肉瘤细胞及C6大鼠胶质瘤细胞0–3天。BCH显著抑制细胞生长，同时诱导DNA片段化、细胞凋亡并激活caspase-3/7[6]。
在体内，BCH（240mg/kg）腹腔注射于HFD/STZ诱导的T2DM和db/db小鼠模型，持续一周。BCH缓解了糖尿病神经性疼痛症状[7]。BCH（200mg/kg）静脉注射于接种了HuCCT1胆管癌细胞的BALB/c裸鼠，持续14天。BCH显著抑制了肿瘤生长，并增加了吉西他滨和5-FU的治疗效果[8]。
| 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: | |
| Cas No. | 20448-79-7 | SDF | |
| 别名 | 2-氨基-2-去甲菠烷羧酸,2-amino-2-Norbornanecarboxylic Acid | ||
| 化学名 | (1S,2S,4R)-2-aminobicyclo[2.2.1]heptane-2-carboxylic acid | ||
| Canonical SMILES | OC([C@]1([C@@H](CC2)C[C@@H]2C1)N)=O | ||
| 分子式 | C8H13NO2 | 分子量 | 155.2 |
| 溶解度 | 10mg/mL in PBS, pH 7.2 | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 6.4433 mL | 32.2165 mL | 64.433 mL |
| 5 mM | 1.2887 mL | 6.4433 mL | 12.8866 mL |
| 10 mM | 644.3 μL | 3.2216 mL | 6.4433 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >95.00% Appearance: A solid
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