WZB117

Catalog No.S7927 Batch:S792702

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Technical Data

Formula

C20H13FO6
Molecular Weight 368.31 CAS No. 1223397-11-2
Solubility (25°C)* In vitro 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description 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.
Targets
GLUT1 [1]
(In cancer cells)
10μM
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].

Protocol (from reference)

Cell Assay:

Cell viability assay[1]
  • Cell lines

    cancer cell 

  • Concentrations

    10μM

  • Incubation Time

    24 or 48 hours

  • Method

    Cells are treated with compound WZB117 for 24 or 48 hours. Mock-treated and glucose deprivation samples served as negative and positive controls, respectively.
Animal Study:

[1]
  • Animal Models

    Nude mice

  • Dosages

    10mg/kg

  • Administration

    i.p.

Selleck's WZB117 has been cited by 13 publications

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

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.