WZB117
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
IC50: ~0.6 μM for blocking glucose transport in diverse cancer cells
WZB117 is a glucose transporter 1 (Glut1) inhibitor.
Glucose transporter 1 (GLUT1), a uniporter protein that in humans is encoded by the SLC2A1 gene, facilitates the transport of glucose across the plasma membranes of mammalian cells. GLUT1 is responsible for the low level of basal glucose uptake to maintain respiration. Expression levels of GLUT1 in cell membranes are increased by reduced glucose levels and decreased by increased glucose.
In vitro: Previous study found that WZB117 could inhibit glucose transport in human red blood cells expressing Glut1 as their sole glucose transporter. Moreover, cancer cell treatment with WZB117 resulted in decreased levels of Glut1 protein, intracellular ATP, as well as glycolytic enzymes. All these changes were followed by increase in ATP-sensing enzyme AMP-activated protein kinase and declined in cyclin E2 as well as phosphorylated retinoblastoma, leading to cell-cycle arrest, senescence, and necrosis [1].
In vivo: Animal study showed that the daily ip injection of WZB117 at 10 mg/kg led to a more than 70% reduction in the size of human lung cancer of A549 cell origin [1].
Clinical trial: So far, no clinical study has been conducted.
Reference:
[1] Liu, Y. ,Cao, Y.,Zhang, W., et al. A small-molecule inhibitor of glucose transporter 1 downregulates glycolysis, induces cell-cycle arrest, and inhibits cancer cell growth in vitro and in vivo. Mol. Cancer Ther. 11(8), 1672-1682 (2012).
- 1. Nan Jing, Jiaxing Song, et al. "Glycosylation of anthocyanins enhances the apoptosis of colon cancer cells by handicapping energy metabolism." BMC Complement Med Ther. 2020 Oct 15;20(1):312. PMID: 33059637
- 2. Li Y, Hong W, et al. "Photothermally triggered cytosolic drug delivery of glucose functionalized polydopamine nanoparticles in response to tumor microenvironment for the GLUT1-targeting chemo-phototherapy." J Control Release. 2019 Nov 26. pii: S0168-3659(19)30690-X. PMID: 31783048
Storage | Store at -20°C |
M.Wt | 368.3 |
Cas No. | 1223397-11-2 |
Formula | C20H13FO6 |
Synonyms | Glucose Transporter Inhibitor IV |
Solubility | insoluble in H2O; ≥18.4 mg/mL in DMSO; ≥42.6 mg/mL in EtOH |
Chemical Name | 3-hydroxy-benzoic acid, (3-fluoro-1,2-phenylene)ester |
SDF | Download SDF |
Canonical SMILES | OC1=CC=CC(C(OC2=CC=CC(F)=C2OC(C3=CC(O)=CC=C3)=O)=O)=C1 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
质量控制和MSDS
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