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Chemical Structure| 1223397-11-2 Chemical Structure| 1223397-11-2

Structure of WZB117
CAS No.: 1223397-11-2

Chemical Structure| 1223397-11-2

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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.

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Product Details of WZB117

CAS No. :1223397-11-2
Formula : C20H13FO6
M.W : 368.31
SMILES Code : FC1=C(C(OC(C2=CC=CC(O)=C2)=O)=CC=C1)OC(C3=CC=CC(O)=C3)=O
MDL No. :MFCD24387113
InChI Key :FRSWCCBXIHFKKY-UHFFFAOYSA-N
Pubchem ID :46830365

Safety of WZB117

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

Target
  • GLUT1

    GLUT1, IC50:10μM

In Vitro:

Cell Line
Concentration Treated Time Description References
Cortical neurons 10 µM 24 hours No effect on cell viability Antioxidants (Basel). 2021 Sep 3;10(9):1413.
CHO cells 3 µM Validate the inhibitory activity of WZB117 on GluN1/GluN3A receptors Front Pharmacol. 2022 Jun 9;13:888308.
MCF-7 cells 50 µM 1.5 hours Evaluate the activity of GLUT1 inhibitors, WZB117 showed significant inhibition of glucose uptake Molecules. 2022 Nov 21;27(22):8106.
Human erythrocytes 0.1 µM to 7 µM 10 min to 1 min WZB117 reversibly and competitively inhibits erythrocyte 3-O-methylglucose (3MG) uptake with Ki(app) of 6.2 μM. J Biol Chem. 2016 Dec 23;291(52):26762-26772.
HEK-293 cells 1.15 ± 0.34 µM (IC50) 20 minutes Evaluate the inhibitory activity and IC50 value of WZB117 on GluN1/GluN3A receptors Front Pharmacol. 2022 Jun 9;13:888308.
Peritoneal macrophages 50 and 100 µM 2–3 hours Evaluate the inhibitory effect of WZB117 on macrophage glycolysis Int J Mol Sci. 2021 Jun 14;22(12):6350.
Human subventricular tumor C3 cells (HSVT-C3) 5 µM 24 and 48 hours Inhibited GLUT1, reduced neurite growth Antioxidants (Basel). 2021 Sep 3;10(9):1413.
Neuroblastoma 2a cells (Neuro2a) 5 µM 24 and 48 hours Inhibited GLUT1, reduced neurite growth Antioxidants (Basel). 2021 Sep 3;10(9):1413.
Human periodontal ligament cells (PDLCs) 10 µM 24 hours Inhibited GLUT1 expression, reduced mechanical stress-induced RANKL upregulation, thereby suppressing osteoclast differentiation. Int J Oral Sci. 2018 Aug 15;10(3):27.
SW620 cells 80 µM 24 hours Evaluate the effect of WZB117 on glycolysis activity and mitochondrial respiration in SW620 cells, showing significant inhibition of glycolysis. EBioMedicine. 2018 Jul;33:105-121.
SW480 cells 80 µM 24 hours Evaluate the effect of WZB117 on glycolysis activity and mitochondrial respiration in SW480 cells, showing significant inhibition of glycolysis. EBioMedicine. 2018 Jul;33:105-121.
HTR8/SVneo cells 20 µM 24 hours To evaluate the effect of WZB117 on ferroptosis in HTR8/SVneo cells under high glucose conditions. Results showed that WZB117 significantly reduced RSL3-induced ferroptosis, indicating that GLUT1 inhibition can protect trophoblast cells from ferroptosis. Mol Med. 2024 Dec 20;30(1):257.
Cortical astrocytes 5 µM and 10 µM 24 hours Significant decrease in viability at 10 µM Antioxidants (Basel). 2021 Sep 3;10(9):1413.
U87 cells 5 µM and 10 µM 24 hours No effect on viability at 5 µM, decreased viability by 28.57% at 10 µM Antioxidants (Basel). 2021 Sep 3;10(9):1413.
Chondrocytes 40 µM 3 days Inhibited GLUT1 expression, reducing compression-induced chondrocyte hypertrophy Bone Joint Res. 2025 Mar 10;14(3):209-222.
MCF-10A 93.3 µg/mL 48 hours Evaluate the cytotoxicity of WZB117-OCMC-MET on MCF-10A cells, showing an IC50 of 93.3 µg/mL, indicating low toxicity to normal cells. Polymers (Basel). 2023 Feb 16;15(4):976.
MDA-MB-231 8.3 µg/mL 48 hours Evaluate the cytotoxicity of WZB117-OCMC-MET on MDA-MB-231 cells, showing an IC50 of 8.3 µg/mL. Polymers (Basel). 2023 Feb 16;15(4):976.
MCF-7 10.2 µg/mL 48 hours Evaluate the cytotoxicity of WZB117-OCMC-MET on MCF-7 cells, showing an IC50 of 10.2 µg/mL. Polymers (Basel). 2023 Feb 16;15(4):976.
A549 50 µM 48 hours Inhibition of glucose uptake and glycolysis, but with minimal impact on the viability of ADC cell lines Nat Commun. 2017 May 26;8:15503.
HCC2814 50 µM 48 hours Inhibition of glucose uptake and glycolysis, significantly reducing the viability of SqCC cell lines Nat Commun. 2017 May 26;8:15503.
HCC1588 50 µM 48 hours Inhibition of glucose uptake and glycolysis, significantly reducing the viability of SqCC cell lines Nat Commun. 2017 May 26;8:15503.
HCC95 50 µM 48 hours Inhibition of glucose uptake and glycolysis, significantly reducing the viability of SqCC cell lines Nat Commun. 2017 May 26;8:15503.
SK-MEL-28 113.91 µM 48 hours To evaluate the inhibitory effect of WZB117 on SK-MEL-28 cell proliferation, results showed that WZB117 inhibited cell proliferation in a dose- and time-dependent manner. Front Pharmacol. 2022 Sep 16;13:976117.
A375 116.85 µM 48 hours To evaluate the inhibitory effect of WZB117 on A375 cell proliferation, results showed that WZB117 inhibited cell proliferation in a dose- and time-dependent manner. Front Pharmacol. 2022 Sep 16;13:976117.
MDA-MB-231 cells 60 µM 48 hours WZB117 inhibits glucose uptake in MDA-MB-231 cells and shows synergistic growth inhibition and apoptosis induction when combined with MK-2206. Front Pharmacol. 2019 Nov 6;10:1311.
MCF-7 cells 60 µM 48 hours WZB117 inhibits glucose uptake in MCF-7 cells and shows synergistic growth inhibition and apoptosis induction when combined with MK-2206. Front Pharmacol. 2019 Nov 6;10:1311.
GIST-T1/IM-R cells 10 µM 72 hours WZB117 significantly downregulated AKT phosphorylation and Bcl-2 expression, and combined use with imatinib showed synergistic growth inhibition effects in apoptosis assays. Oncol Rep. 2022 Jan;47(1):7.
SKOV3 cells 100 µM 90 minutes Evaluate the activity of GLUT1 inhibitors, WZB117 showed significant inhibition of glucose uptake Molecules. 2022 Nov 21;27(22):8106.
COS-7 cells 100 µM 90 minutes Evaluate the activity of GLUT1 inhibitors, WZB117 showed significant inhibition of glucose uptake Molecules. 2022 Nov 21;27(22):8106.
HEK293 cells 0.1 µM to 13.32 µM WZB117 inhibits GLUT1- and GLUT3-mediated 2-deoxy-D-glucose (2DG) uptake with Ki(app) of ~10 μM but is a more potent inhibitor of GLUT4-mediated uptake (Ki(app) of 0.2 μM). J Biol Chem. 2016 Dec 23;291(52):26762-26772.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Rat Postnatal day 5 rats Cerebral cortex injection 10 µM Single injection, lasting 72 hours Inhibited GLUT1, reduced neurite length and branching Antioxidants (Basel). 2021 Sep 3;10(9):1413.
Nude mice HCC1588 and HCC2814 xenograft models Intraperitoneal injection 10 mg/kg Once daily for 3-4 weeks GLUT1 inhibition significantly suppressed SqCC tumor growth but had no significant effect on ADC tumor growth Nat Commun. 2017 May 26;8:15503.
C57BL/6 mice Orthodontic tooth movement (OTM) model Intraperitoneal injection 10 mg/kg Every other day for 7 days Inhibited GLUT1 activity, reduced orthodontic tooth movement distance and osteoclastic activities. Int J Oral Sci. 2018 Aug 15;10(3):27.
C57BL/6J mice STZ-induced gestational diabetes model Intraperitoneal injection 10 mg/kg Every other day from E13.5 to E18.5 To evaluate the effect of WZB117 on fetal growth restriction in STZ-induced gestational diabetes mouse model. Results showed that WZB117 treatment significantly improved fetal weight and crown-rump length, reduced placental ferroptosis markers, indicating that GLUT1 inhibition can ameliorate gestational diabetes-associated fetal growth restriction. Mol Med. 2024 Dec 20;30(1):257.
Nude mice ICCA patient-derived xenograft (PDX) model Intraperitoneal injection 10 mg/kg Once daily for 6 weeks WZB117 inhibited the tumor growth of the PDX#4 models but did not inhibit tumor growth in the PDX#1 group. Oncogenesis. 2020 Feb 13;9(2):19
Sprague-Dawley (SD) rats TMJ degeneration model Intra-articular injection 10 mg/ml Daily for the duration of the experiment Inhibited GLUT1 expression, reducing chondrocyte hypertrophy and O-GlcNAcylation levels Bone Joint Res. 2025 Mar 10;14(3):209-222.
Mice Orthotopic model of pancreatic ductal adenocarcinoma Oral 250 ppm (equivalent to a 50 mg/kg daily dose) Once daily for 7 days Evaluate the effect of WZB117 on tumor burden, results showed WZB117 significantly reduced tumor burden Int J Mol Sci. 2021 Jun 14;22(12):6350.

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.72mL

0.54mL

0.27mL

13.58mL

2.72mL

1.36mL

27.15mL

5.43mL

2.72mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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