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CAS No. : 314045-39-1
MCE 国际站:BPTES
产品活性:BPTES是选择性的谷氨酰胺酶变构抑制剂,IC50 为0.16 μM。
研究领域:Metabolic Enzyme/Protease
作用靶点:Glutaminase
In Vitro: BPTES (10 μM) exhibits inhibition of PDAC cell proliferation. BPTES preferentially slows growth of mutant IDH1 cells without inducing apoptosis. BPTES (10 μM) reduces glutaminase activity in both WT and mutant IDH1 expressing cells, diminishes glutamate and α-KG levels, and increases glycolytic intermediates while leaving total 2-HG levels unaffected. BPTES (10 μM) shows a clear synergistic anti-cancer effect with 10 μM of 5-FU in A549 and EKVX cell lines, and results in a growth reduction response not only in EKVX and A549 but also in most of the NSCLC cell lines. BPTES (10 μM) effectively reduces the levels of the metabolites of the TCA cycle, with no changes in the levels of metabolites in glycolysis and the pentose phosphate pathway. BPTES treatment reduces about 30% ATP production under normoxia, and an additional 10% reduction of ATP production is observed under hypoxia in EKVX.
In Vivo: BPTES-NPs (BPTES nanoparticles, 1.2 mg BPTES in 100 μL nanoparticles, i.v.) significantly attenuates tumor growth in the patient-derived pancreatic orthotopic tumor model.
相关产品:Bioactive Compound Library Plus | Metabolism/Protease Compound Library | Anti-Cancer Compound Library | Glycolysis Compound Library | Glutamine Metabolism Compound Library | Anti-Lung Cancer Compound Library | Anti-Cancer Metabolism Compound Library | Mitochondria-Targeted Compound Library | Targeted Diversity Library | Human Metabolite Library | Cuproptosis Compound Library | Highly Selective Inhibitors Library | Glutaminase-IN-1 | ZED-1227 | Glutaminase-IN-4 | GLS1 Inhibitor-4 | Zampilimab | NC9 | Cystamine-d8 (dihydrochloride) | BJJF078 | GLS1 Inhibitor-6 | Telaglenastat | Cystamine | LWG-301 | Glutaminase C-IN-1 | IPN60090 | GK921 | JHU-083 | A-446 | 2-Amino-2-(p-tolyl)acetic acid | 6-Diazo-5-oxo-L-nor-Leucine | L-Albizziin | GLS-1-IN-1 | NTU281 | TG-2-IN-1 | α-Glucosidase-IN-5 | UPGL00004 | GLS1 Inhibitor-3 | Glutaminase-IN-3
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