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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C20H13FO6 |
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分子量 | 368.31 | CAS No. | 1223397-11-2 | |
Solubility (25°C)* | 体外 | DMSO | 73 mg/mL (198.2 mM) | |
Ethanol | 73 mg/mL (198.2 mM) | |||
Water | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | WZB117 is an inhibitor of Glucose Transporter 1 (GLUT1). It inhibited cell proliferation in lung cancer A549 cells and breast cancer MCF7 cells with an IC50 of approximately 10 μM. |
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in vitro | WZB117 inhibits glucose transport in human red blood cells. Cancer cell treatment with WZB117 leads to decreases in levels of Glut1 protein, intracellular ATP, and glycolytic enzymes. All these changes are followed by increase in ATP-sensing enzyme AMP-activated protein kinase (AMPK) and declines in cyclin E2 as well as phosphorylated retinoblastoma, resulting in cell-cycle arrest, senescence, and necrosis[1]. |
in vivo | Daily intraperitoneal injection of WZB117 at 10mg/kg resultes in 70% reduction in tumor volume of human A549 lung cancer grafted on nude mice[1]. |
細胞アッセイ | 細胞株 | cancer cell |
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濃度 | 10μM | |
反応時間 | 24 or 48 hours | |
実験の流れ | Cells are treated with compound WZB117 for 24 or 48 hours. Mock-treated and glucose deprivation samples served as negative and positive controls, respectively. |
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動物実験 | 動物モデル | Nude mice |
投薬量 | 10mg/kg | |
投与方法 | i.p. |
GLUT1 promotes NLRP3 inflammasome activation of airway epithelium in lipopolysaccharide-induced acute lung injury [ Am J Pathol, 2024, S0002-9440(24)00116-0] | PubMed: 38548270 |
Accumulation of branched-chain amino acids reprograms glucose metabolism in CD8+ T cells with enhanced effector function and anti-tumor response [ Cell Rep, 2023, 42(3):112186] | PubMed: 36870057 |
De novo pyrimidine synthesis fuels glycolysis and confers chemoresistance in gastric cancer [ Cancer Lett, 2022, S0304-3835(22)00321-4] | PubMed: 35921972 |
WZB117 enhanced the anti-tumor effect of apatinib against melanoma via blocking STAT3/PKM2 axis [ Front Pharmacol, 2022, 13:976117] | PubMed: 36188586 |
Glucose transporter‑1 inhibition overcomes imatinib resistance in gastrointestinal stromal tumor cells [ Oncol Rep, 2022, 47(1)7] | PubMed: 34738628 |
Physiologic Mechanical Stress Directly Induces Bone Formation by Activating Glucose Transporter 1 (Glut 1) in Osteoblasts, Inducing Signaling via NAD+-Dependent Deacetylase (Sirtuin 1) and Runt-Related Transcription Factor 2 (Runx2) [ Int J Mol Sci, 2021, 22(16)9070] | PubMed: 34445787 |
Glucose Protects Cochlear Hair Cells Against Oxidative Stress and Attenuates Noise-Induced Hearing Loss in Mice [ Neurosci Bull, 2021, 10.1007/s12264-020-00624-1] | PubMed: 33415566 |
Glucose regulates hypoxia-induced NLRP3 inflammasome activation in macrophages. [ J Cell Physiol, 2020, 10.1002] | PubMed: 32115713 |
CD36 inhibits β-catenin/c-myc-mediated glycolysis through ubiquitination of GPC4 to repress colorectal tumorigenesis. [ Nat Commun, 2019, 10(1):3981] | PubMed: 31484922 |
BRCA1 Deficiency Upregulates NNMT, Which Reprograms Metabolism and Sensitizes Ovarian Cancer Cells to Mitochondrial Metabolic Targeting Agents [ Cancer Res, 2019, 79(23):5920-5929] | PubMed: 31619387 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。