| Name | WZB117 |
| Description | WZB117 is a Glucose Transporter 1 (GLUT1) inhibitor. when IC50 of WZB117 approximate 10 μM, it inhibits lung cancer A549 cells and breast cancer MCF7 cells proliferation. |
| Cell Research | Human non–small cell lung cancer (NSCLC) cell lines H1299 and A549 are treated with compound WZB117（10 μM） for 24 or 48 hours. |
| Kinase Assay | Recombinant proteins expressed with Sf21 cells and baculovirus vectors are purified with affinity chromatography. JAK kinase assay is done by a homogeneous time-resolved fluorescence assay with the peptide substrate (-EQEDEPEGDYFEWLE). Each enzyme reaction is carried out with Ruxolitinib or control, JAK enzyme, 500 nM peptide, adenosine triphosphate (ATP; 1 mM), and 2% dimethyl sulfoxide (DMSO) for 1 hour. IC50 is the INCB018424 concentration required for inhibition of 50% of the fluorescent signal. |
| Animal Research | Male NU/J nude mice were given intraperitoneal injection with WZB117 (10 mg/kg) daily for 10 weeks. |
| In vitro | WZB117 treats Cancer cell resulting in decreases in levels of Glut1 protein, intracellular ATP, and glycolytic enzymes. And WZB117 inhibits glucose transport in human red blood cells. The declines in cyclin E2 as well as phosphorylated retinoblastoma and increases in ATP-sensing enzyme AMP-activated protein kinase (AMPK), lead to the cell-cycle arrest, senescence, and necrosis. |
| In vivo | WZB117 inject 10 mg/kg daily intraperitoneal into nude mice, which were grafted human A549 lung cancer, show 70% reduction in tumor volume. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 36.8 mg/mL (100 mM)
Ethanol : 36.8 mg/mL (100 mM)
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| Keywords | GLUT | Inhibitor | WZB-117 | inhibit | Glucose transporter | WZB 117 | WZB117 |
| Inhibitors Related | MSNBA | Fraxin | LDN-212320 | Venuloside A | Brilliant Yellow | WAY-213613 hydrochloride | Jujuboside A | IPN60090 | SLC26A3-IN-1 | BAY-876 | Phloretin | Telaglenastat |
| Related Compound Libraries | Target-Focused Phenotypic Screening Library | Bioactive Compound Library | Glutamine Metabolism Compound Library | Anti-Obesity Compound Library | Inhibitor Library | Metabolism Compound Library | Bioactive Compounds Library Max | Fluorochemical Library | Anti-Cancer Compound Library | Anti-Cancer Active Compound Library |
United States
