WZB117 (Synonyms: Glucose Transporter Inhibitor IV) |
Catalog No.GC13381
One-Click Copy Product Info
|
WZB117 is a small molecule inhibitor targeting glucose transporter 1 (GLUT1).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1223397-11-2
Sample solution is provided at 25 µL, 10mM.
WZB117 is a small molecule inhibitor targeting glucose transporter 1 (GLUT1) [1]. WZB117 reduces glucose uptake in cancer cells, lowers intracellular ATP levels, and activates AMPK, which in turn triggers cell cycle arrest, senescence, and necrosis [2-3]. WZB117 is mainly used in the field of tumor research to inhibit the glucose metabolism and growth of cancer cells [4].
In A375 and SK-MEL-28 cells, Apatinib combined with WZB117 (0-160μM; 24h, 48h, 72h) showed synergistic cell growth inhibitory effects on cell [5]. In PANC-1 cells, WZB117 (10μM, 25μM; 24h) significantly reduced glycogenolysis in cells in a dose-dependent manner [6]. In SH-SY5Y cells, WZB117 (1-30μM; 72h) treatment reduces tumor cell viability and downregulates GLUT1 protein levels [7].
In P. berghei ANKA-infected mice model, WZB117 (10mg/kg; iv; 11d) effectively inhibits the growth of blood-stage parasites [8]. In PANC-1 CSLC subcutaneous tumor mice model, WZB117 (20mg/kg; ip; 20d) inhibits the tumor-initiating ability of PANC-1 CSLCs in vivo [9].
References:
[1]. Ojelabi OA, Lloyd KP, Simon AH, et al. WZB117 (2-Fluoro-6-(m-hydroxybenzoyloxy) Phenyl m-Hydroxybenzoate) inhibits GLUT1-mediated sugar transport by binding reversibly at the exofacial sugar binding site. Journal of Biological Chemistry. 2016 Dec 1;291(52):26762-26772.
[2]. 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. Molecular cancer therapeutics. 2012 Aug 1; 11(8): 1672-1682.
[3]. Ojelabi O, DeZutter J, Lloyd K, et al. Novel small molecule, WZB117, competitively inhibit GLUT1‐mediated glucose transport to halt cancer growth. The FASEB Journal. 2016 Apr; 30: 1099.
[4]. Qian Y, Shriwas P, Wang X, et al. Screening and identification of new generation glucose transporter inhibitors as anticancer therapeutics. Cancer Research. 2017 Jul 1; 77(13_Supplement): 1157.
[5]. Zhang RS, Li ZK, Liu J, et al. WZB117 enhanced the anti-tumor effect of apatinib against melanoma via blocking STAT3/PKM2 axis. Frontiers in Pharmacology. 2022 Sep 16; 13: 976117.
[6]. Poonprasartporn A, Xiao J, Chan KA. A study of WZB117 as a competitive inhibitor of glucose transporter in high glucose treated PANC-1 cells by live-cell FTIR spectroscopy. Talanta. 2024 Jan 1; 266: 125031.
[7]. Peng Y, Xing SN, Tang HY, et al. Influence of glucose transporter 1 activity inhibition on neuroblastoma in vitro. Gene. 2019 Mar 20; 689: 11-17.
[8]. Wei M, Lu L, Sui W, et al. Inhibition of GLUTs by WZB117 mediates apoptosis in blood-stage Plasmodium parasites by breaking redox balance. Biochemical and biophysical research communications. 2018 Sep 5; 503(2): 1154-1159.
[9]. Shibuya K, Okada M, Suzuki S, et al. Targeting the facilitative glucose transporter GLUT1 inhibits the self-renewal and tumor-initiating capacity of cancer stem cells. Oncotarget. 2014 Nov 26; 6(2): 651.
| Cell experiment [1]: | |
Cell lines | A375 and SK-MEL-28 melanoma cells |
Preparation Method | cells were exposed to various concentrations of drugs (apatinib: range from 0 to 100μM; WZB117: range from 0 to 160μM) for 24h/48h/72h. Following apatinib or WZB117 treatment, 20μL of 0.5mg/mL MTT was added to each well and incubated for another 4h at 37℃. Then the supernatants were carefully removed and added 150μL DMSO per well. At last, the light absorbance at 570nm was determined in a luminescence plate reader according to the manufacturer’s instructions. |
Reaction Conditions | 0-160μM; 24h, 48h, 72h |
Applications | Apatinib combined with WZB117 showed synergistic cell growth inhibitory effects on A375 and SK-MEL-28 cells. |
| Animal experiment [2]: | |
Animal models | P. berghei ANKA-infected mice model |
Preparation Method | For in vivo WZB117 treatment,1.5 × 106 P. berghei ANKA-infected RBCs were intravenously injected into female BALB/c mice. We injected 10mg/kg WZB117 in 1:1 PBS/DMSO (v/v) or vehicle alone into the mice by intraperitoneal injection. The change in parasitemia was determined by a light microscope examination of Giemsa-stained thin smears from tail blood. |
Dosage form | 10mg/kg; iv; 11d |
Applications | WZB117 effectively inhibits the growth of blood-stage parasites. |
References: | |
| Cas No. | 1223397-11-2 | SDF | |
| Synonyms | Glucose Transporter Inhibitor IV | ||
| Chemical Name | 3-hydroxy-benzoic acid, (3-fluoro-1,2-phenylene)ester | ||
| Canonical SMILES | OC1=CC=CC(C(OC2=CC=CC(F)=C2OC(C3=CC(O)=CC=C3)=O)=O)=C1 | ||
| Formula | C20H13FO6 | M.Wt | 368.3 |
| Solubility | ≥ 18.4mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.7152 mL | 13.5759 mL | 27.1518 mL |
| 5 mM | 543 μL | 2.7152 mL | 5.4304 mL |
| 10 mM | 271.5 μL | 1.3576 mL | 2.7152 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 31 reference(s) in Google Scholar.)