المراجع (Citations)
1 publicationsمنشورات الباحثين الذين استخدموا هذا المنتجالوصف (Description)
BCAT-IN-2 is a selective mitochondrial branched-chain aminotransferase (BCATm; pIC50=7.3) inhibitor that inhibits branched-chain amino acid transaminase 1 (BCATc; pIC50=6.6). BCAT-IN-2 can be used in research related to obesity, dyslipidemia, and prostate cancer PARP inhibitor resistance[1-4].
In vitro, BCAT-IN-2 (80μM) treated A2058 and A375 melanoma cells for 24 hours or 14 days. BCAT-IN-2 significantly inhibited colony formation, invasion, and migration, reduced the expression of fatty acid synthase (FASN) and ATP-citrate lyase (ACLY), and decreased intracellular lipid and palmitic acid content[5]. BCAT-IN-2 (0–100μM) co-treated LO2 and HepG2 cells with oleic acid (0.5mM) for 48 hours. BCAT-IN-2 showed no significant effect on oleic acid-induced lipid accumulation, and intracellular triglyceride and cholesterol levels remained unchanged[6].
In vivo, BCAT2-IN-2 (100mg/kg; once every 3 days) was administered by gavage to nude mice subcutaneously injected with DU145 cells for 2 weeks. BCAT2-IN-2 significantly reduced tumor volume and mass, and decreased PCBP1 expression[7]. BCAT-IN-2 (20mg/kg) was administered daily by gavage to BALB/c nude mice subcutaneously injected with HCT116 cells for 21 days. BCAT-IN-2 significantly promoted tumor growth[8].
References:
[1] Bertrand SM, Ancellin N, Beaufils B, et al. The Discovery of in Vivo Active Mitochondrial Branched-Chain Aminotransferase (BCATm) Inhibitors by Hybridizing Fragment and HTS Hits. J Med Chem. 2015 Sep 24;58(18):7140-63.
[2] Zheng J, Wu M, Pang Y, et al. Interior decorative volatile organic compounds exposure induces sleep disorders through aberrant branched chain amino acid transaminase 2 mediated glutamatergic signaling resulting from a neuroinflammatory cascade. Sci Total Environ. 2024 Jul 15;934:173254.
[3] Nam H, Kundu A, Karki S, et al. HDAC7 promotes renal cancer progression by reprogramming branched-chain amino acid metabolism. Sci Adv. 2025 Jun 6;11(23):eadt3552.
[4] Chen S, Hu T, Zhu K, et al. 16-h fasting optimizes cancer immunotherapy in mice and humans. Cell Metab. 2026 May 5;38(5):944-962.e14.
[5] Tian Y, Ma J, Wang H, et al. BCAT2 promotes melanoma progression by activating lipogenesis via the epigenetic regulation of FASN and ACLY expressions. Cell Mol Life Sci. 2023 Oct 6;80(11):315.
[6] Lu Z, Sun GF, Pan XA, et al. BCATc inhibitor 2 ameliorated mitochondrial dysfunction and apoptosis in oleic acid-induced non-alcoholic fatty liver disease model. Front Pharmacol. 2022 Oct 28;13:1025551.
[7] Mei W, Wei M, Tang C, et al. BCAT2 binding to PCBP1 regulates the PI3K/AKT signaling pathway to inhibit autophagy-related apoptosis and ferroptosis in prostate cancer. Cell Death Dis. 2025 Apr 24;16(1):337.
[8] Kang ZR, Jiang S, Han JX, et al. Deficiency of BCAT2-mediated branched-chain amino acid catabolism promotes colorectal cancer development. Biochim Biophys Acta Mol Basis Dis. 2024 Feb;1870(2):166941.
البروتوكول (Protocol)
| Cell experiment [1]: | |
Cell lines | LO2 and HepG2 cells (human hepatic cell lines) |
Preparation Method | LO2 and HepG2 cells were cultured in DMEM supplemented with 10% fetal bovine serum (FBS) and maintained at 37°C containing 5% CO₂. LO2 and HepG2 cells were treated with indicated concentrations of BCAT-IN-2 for 48h for MTT assay. For lipid accumulation experiments, cells were incubated with 0.5mM Oleic acid and 0, 25, 50μM BCAT-IN-2 for 48h. |
Reaction Conditions | 0-100μM; 48h |
Applications | BCAT-IN-2 had no obvious cytotoxicity on LO2 cells at indicated concentrations and HepG2 cell viability was slightly inhibited at the concentration of 100μM. BCAT-IN-2 showed no effect on OA-induced lipid accumulation and did not change OA-induced TG and TC production. |
| Animal experiment [2]: | |
Animal models | Male BALB/c nude mice |
Preparation Method | Male BALB/c nude mice (6-8 weeks old) were subcutaneously injected with 3 x 106 HCT116 cells for xenograft experiments. The BCAT2 inhibitor BCAT-IN-2 was dissolved in corn oil and gavaged daily (20mg/kg). |
Dosage form | 20mg/kg; daily gavage for 21 days |
Applications | BCAT-IN-2 significantly enhanced tumor growth and increased the positive rate of Ki-67 cells in tumor tissues. |
References: | |
وثائق المنتج (Product Documents)
الخصائص الكيميائية (Chemical Properties)
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.
الحاسبات (Calculators)المولارية / التخفيف / الوزن الجزيئي / تحويل الوحدات / تركيبة داخل الجسم الحي / الذوبانية
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