WZB117

Name: WZB117
Brand: MedChemExpress
SKU: HY-19331
Rating: 5.0 (21 reviews)

Cat. No.: HY-19331 Purity: 99.74%: Data Sheet
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WZB117 is a glucose transporter 1 (Glut1) inhibitor, which downregulates glycolysis, induces cell-cycle arrest, and inhibits cancer cell growth in vitro and in vivo.

For research use only. We do not sell to patients.

CAS No. : 1223397-11-2

Size	Stock	Quantity

Free Sample (0.1 - 0.2 mg)	Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 21 publication(s) in Google Scholar

21 Publications Citing Use of MCE WZB117

Cell Proliferation/Viability Assay

Flow Cytometry

Cell Imaging/Staining

RT-PCR

: WZB117 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Jun 18:e2304687. [Abstract]; CCK-8 assay was used to quantify the cell viability of SH‐SY5Y cells after treatment with conditioned media from BV2 cells. BV2 cells were treated with or without WZB117 (10 µM), and COR for 24 h.

: WZB117 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Jun 18:e2304687. [Abstract]; FACS plots showing representative mtROS expression levels and mitochondrial membrane potential in BV2 cells. BV2 cells were treated with or without WZB117 (10 µM), and COR for 24 h.

: WZB117 purchased from MedChemExpress. Usage Cited in: Cell Metab. 2022 Dec 6;34(12):1999-2017.e10. [Abstract]; WZB117 (200 μM; 24 h) significantly increased the level of NGF in Cal27 cells.

: WZB117 purchased from MedChemExpress. Usage Cited in: J Nanobiotechnology. 2022 Sep 15;20(1):414. [Abstract]; The quantitative analysis of cellular uptake of C-Lp/C6, Rg3-Lp/C6 and Rg3-Lp/C6 with Glut1 inhibitors (WZB117) in 4T1 cells via flow cytometry. The fluorescent intensity represents the mean fluorescence intensity (MFI) of C6-loaded liposome uptake by 4T1 cells. The results showed that WZB117 (10 μM; 1 h) significantly inhibited the cellular uptake of Rg3-Lp in 4T1 cells.

: WZB117 purchased from MedChemExpress. Usage Cited in: J Nanobiotechnology. 2022 Sep 15;20(1):414. [Abstract]; Confocal laser scanning microscope (CLSM) images of the cellular uptake of C-Lp/C6, Rg3-Lp/C6 and Rg3-Lp/C6 with Glut1 inhibitors (WZB117) in 4T1 cells. The results showed that WZB117 (10 μM; 1 h) significantly inhibited the cellular uptake of Rg3-Lp in 4T1 cells. Scale bars: 20 μm.

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GLUT1 GLUT2 GLUT3 GLUT4

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

WZB117 is a glucose transporter 1 (Glut1) inhibitor, which downregulates glycolysis, induces cell-cycle arrest, and inhibits cancer cell growth in vitro and in vivo.

IC₅₀ & Target^[1]

GLUT1

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	2.5 μM Compound: 46830365	Inhibition of the Glucose Transporter (GLUT4, SLC2A4) as assessed by a FRET based flow cytometry assay using a genetically-encoded biosensor for measuring free glucose (FLII12Pglu-700uDelta6) in HEK293 JumpIN TRex SLC2A4 WT-OE cells (PubChem AID: 1794828) Inhibition of the Glucose Transporter (GLUT4, SLC2A4) as assessed by a FRET based flow cytometry assay using a genetically-encoded biosensor for measuring free glucose (FLII12Pglu-700uDelta6) in HEK293 JumpIN TRex SLC2A4 WT-OE cells (PubChem AID: 1794828)	10.5281/zenodo.7360638
HEK293	IC₅₀	> 10 μM Compound: 46830365	Inhibition of the Glucose Transporter (GLUT3, SLC2A3) as assessed by a FRET based flow cytometry assay using a genetically-encoded biosensor for measuring free glucose (FLII12Pglu-700uDelta6) in HEK293 JumpIN TRex SLC2A3 WT-OE cells (PubChem AID: 1794827) Inhibition of the Glucose Transporter (GLUT3, SLC2A3) as assessed by a FRET based flow cytometry assay using a genetically-encoded biosensor for measuring free glucose (FLII12Pglu-700uDelta6) in HEK293 JumpIN TRex SLC2A3 WT-OE cells (PubChem AID: 1794827)	10.5281/zenodo.7360656
HEK293	IC₅₀	> 10 μM Compound: 46830365	Inhibition of the Glucose Transporter (GLUT2, SLC2A2) as assessed by a FRET based flow cytometry assay using a genetically-encoded biosensor for measuring free glucose (FLII12Pglu-700uDelta6) in HEK293 JumpIN TRex SLC2A2 WT-OE cells (PubChem AID: 1794829) Inhibition of the Glucose Transporter (GLUT2, SLC2A2) as assessed by a FRET based flow cytometry assay using a genetically-encoded biosensor for measuring free glucose (FLII12Pglu-700uDelta6) in HEK293 JumpIN TRex SLC2A2 WT-OE cells (PubChem AID: 1794829)	10.5281/zenodo.7360664
HEK293	IC₅₀	> 10 μM Compound: 46830365	Inhibition of the Glucose Transporter (GLUT1, SLC2A1) as assessed by a FRET based flow cytometry assay using a genetically-encoded biosensor for measuring free glucose (FLII12Pglu-700uDelta6) in HEK293 JumpIN TRex SLC2A1 WT-OE cells (PubChem AID: 1794830) Inhibition of the Glucose Transporter (GLUT1, SLC2A1) as assessed by a FRET based flow cytometry assay using a genetically-encoded biosensor for measuring free glucose (FLII12Pglu-700uDelta6) in HEK293 JumpIN TRex SLC2A1 WT-OE cells (PubChem AID: 1794830)	10.5281/zenodo.7360676
NCI-H1299	IC₅₀	10 μM Compound: 1, WZB117	Cytotoxicity against human H1299 cells assessed as reduction in cell viability Cytotoxicity against human H1299 cells assessed as reduction in cell viability	[PMID: 25288186]
NCI-H1299	IC₅₀	20.4 μM Compound: WZB117	Cytotoxicity against human H1299 cells assessed as growth inhibition after 48 hrs by MTT assay Cytotoxicity against human H1299 cells assessed as growth inhibition after 48 hrs by MTT assay	[PMID: 24200808]

In Vitro

Glucose uptake assays show that WZB117 inhibits glucose transport in cancer cells in a dose-dependent manner. The inhibition of glucose transport induced by WZB117 occurres within 1 minute after the assay started, suggesting that the inhibitory activity is likely to be via a direct and fast mechanism. Cell viability assay shows that WZB117 inhibits cancer cell proliferation with an IC₅₀ of approximately 10 μM. The inhibitory activity of WZB117 on cancer cell growth is also confirmed with a clonogenic assay, which also indicates that the inhibition is irreversible in nature. WZB117 treatment results in significantly more cell growth inhibition in lung cancer A549 cells than in nontumorigenic lung NL20 cells. Similar results are also observed in breast cancer MCF7 cells and their nontumorigenic MCF12A cells. When WZB117 is added to cancer cells grown under hypoxic conditions, more cell growth inhibition is observed than under normoxic conditions^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

The animal study shows that after daily intraperitoneal injection of WZB117 at 10 mg/kg body weight, the sizes of the compound-treated tumors are on average more than 70% smaller than those of the mock (PBS/DMSO)-treated tumors. Notably, 2 of the 10 compound-treated tumors disappear during the treatment and never grow back even at the end of the study. Body weight measurement and analysis reveal that the mice treated with WZB117 lost about 1 to 2 grams of body weight compared with the mock-treated mice with most of the weight loss in the fat tissue. Blood counts and analysis of mice at the end of the study show that lymphocytes and platelets are changed in the compound-treated mice compared with the vehicle-treated mice, but the cell counts remained in the normal ranges. One of the concerns for using glucose transport inhibitors is that the inhibitor might produce hyperglycemia in the treated mice^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

368.31

Formula

C₂₀H₁₃FO₆

CAS No.

1223397-11-2

Appearance

Solid

Color

White to off-white

SMILES

OC1=CC=CC(C(OC2=CC=CC(F)=C2OC(C3=CC(O)=CC=C3)=O)=O)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 250 mg/mL (678.78 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.7151 mL	13.5755 mL	27.1510 mL
5 mM	0.5430 mL	2.7151 mL	5.4302 mL
10 mM	0.2715 mL	1.3576 mL	2.7151 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.79 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.79 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.79 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.93%

Select Batch:

Data Sheet (277 KB) SDS (393 KB)

COA (246 KB) HNMR (201 KB) LCMS (138 KB)

Handling Instructions (2659 KB)

References

[1]. Liu Y, 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. 2012 Aug;11(8):1672-82. [Content Brief]

Cell Assay ^[1]	Human non-small cell lung cancer (NSCLC) cell lines H1299 and A549, human breast ductal carcinoma MCF7, as well as human nontumorigenic NL20 lung and MCF12A breast cells are maintained in cell culture media. Cells are treated with WZB117 for 24 or 48 hours. WZB117 (10 μM) is used in the experiments unless otherwise noted. Mock-treated and glucose deprivation samples served as negative and positive controls, respectively. In glucose deprivation, Dulbecco's Modified Eagle's Media (DMEM) with reduced glucose concentration (2 mM or 8% of glucose concentration in the regular cell culture medium) is prepared by mixing glucose-free DMEM with regular DMEM^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Mice^[1] Male NU/J nude mice of 6 to 8 weeks of age are used. To determine the in vivo anticancer efficacy of WZB117 on human tumor xenograft growth, NSCLC A549 cells in exponential growth phase are harvested, washed, precipitated, and resuspended in PBS. Each mouse is injected subcutaneously with 5×10⁶ cancer cells in the flank. Compound treatment started 3 days after the cancer cells injection and when all tumors become palpable. Tumor cell–injected mice are randomly divided into 2 groups: control group (n=10) treated with PBS/DMSO (1:1, v/v) and WZB117 treatment group (n=10) treated with WZB117 (10 mg/kg body weight) dissolved in PBS/DMSO solution (1:1, v/v). Mice are given intraperitoneal injection with either PBS/DMSO vehicle or WZB117 (10 mg/kg) daily for 10 weeks. Tumor sizes are measured every 7 days with calipers, and tumor volume is calculated^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Liu Y, 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. 2012 Aug;11(8):1672-82. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.7151 mL	13.5755 mL	27.1510 mL	67.8776 mL
	5 mM	0.5430 mL	2.7151 mL	5.4302 mL	13.5755 mL
	10 mM	0.2715 mL	1.3576 mL	2.7151 mL	6.7878 mL
	15 mM	0.1810 mL	0.9050 mL	1.8101 mL	4.5252 mL
	20 mM	0.1358 mL	0.6788 mL	1.3576 mL	3.3939 mL
	25 mM	0.1086 mL	0.5430 mL	1.0860 mL	2.7151 mL
	30 mM	0.0905 mL	0.4525 mL	0.9050 mL	2.2626 mL
	40 mM	0.0679 mL	0.3394 mL	0.6788 mL	1.6969 mL
	50 mM	0.0543 mL	0.2715 mL	0.5430 mL	1.3576 mL
	60 mM	0.0453 mL	0.2263 mL	0.4525 mL	1.1313 mL
	80 mM	0.0339 mL	0.1697 mL	0.3394 mL	0.8485 mL
	100 mM	0.0272 mL	0.1358 mL	0.2715 mL	0.6788 mL

WZB117 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

WZB1171223397-11-2WZB 117WZB-117GLUTGlucose transporterInhibitorinhibitorinhibit

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WZB117

Customer Review

WZB117 Related Antibodies

21 Publications Citing Use of MCE WZB117

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•Related Screening Libraries:

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View All GLUT Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

WZB117 Related Antibodies

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Complete Stock Solution Preparation Table

WZB117 Related Classifications

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