WZB117 (Synonyms: Glucose Transporter Inhibitor IV) |
Catalog No.GC13381
One-Click Copy Product Info
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WZB117 es un inhibidor de molécula pequeña dirigido al transportador de glucosa 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 es un inhibidor de molécula pequeña dirigido al transportador de glucosa 1 (GLUT1) [1]. WZB117 reduce la absorción de glucosa en las células cancerosas, reduce los niveles de ATP intracelular y activa la AMPK, lo que a su vez desencadena la detención del ciclo celular, la senescencia y la necrosis[2-3]. WZB117 se utiliza principalmente en el campo de la investigación tumoral para inhibir el metabolismo de la glucosa y el crecimiento de las células cancerosas [4].
En las células A375 y SK-MEL-28, Apatinib combinado con WZB117 (0-160μM; 24h, 48h, 72h) mostró efectos inhibidores sinérgicos del crecimiento celular en la célula [5]. En las células PANC-1, WZB117 (10μM, 25μM; 24h) redujo significativamente la glucogenólisis en las células de una manera dependiente de la dosis[6]. En las células SH-SY5Y, el tratamiento WZB117 (1-30μM; 72h) reduce la viabilidad de las células tumorales y regula a la baja los niveles de proteína GLUT1[7].
En el modelo de ratones infectados por P. berghei ANKA, WZB117 (10mg/kg; iv; 11d) inhibe eficazmente el crecimiento de parásitos en etapas sanguíneas [8]. En el modelo de ratones de tumor subcutáneos PANC-1 CSLC WZB117 (20mg/kg; ip; 20d) inhibe la capacidad de iniciación del tumor de los 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.
| Experimentos celulares [1]: | |
Líneas celulares | Células de melanoma A375 y SK-MEL-28 |
Método de preparación | Las células estuvieron expuestas a varias concentraciones de medicamentos (apatinib: rango de 0 a 100 μM; WZB117: rango de 0 a 160 μM) durante 24h/48h/72h. Después del tratamiento con apatinib o WZB117, se añadieron 20 μL de 0,5 mg/ml de MTT a cada pozo y se incubaron durante otras 4 horas a 37℃. Luego, los sobrenadantes se eliminaron cuidadosamente y se agregaron 150 μL de DMSO por pozo. Por fin, la absorción de luz a 570 nm se determinó en un lector de placas de luminiscencia de acuerdo con las instrucciones del fabricante. |
Condiciones de reacción | 0-160 μM; 24h, 48h, 72h |
Áreas de aplicación | Apatinib combinado con WZB117 mostró efectos inhibidores sinérgicos del crecimiento celular en las células A375 y SK-MEL-28. |
| Experimentos con animales [2]: | |
Modelos animales | Modelo de ratones infectados con P. berghei ANKA |
Método de preparación | Para el tratamiento in vivo con WZB117, se inyectaron 1,5 × 106 glóbulos rojos infectados con ANKA de 1,5 × berghei en ratones BALB/c hembra. Inyectamos 10 mg/kg de WZB117 en 1:1 PBS/DMSO (v/v) o vehículo solo en los ratones mediante inyección intraperitoneal. El cambio en la parasitemia se determinó mediante un examen de microscopio óptico de frotis finos de sangre de cola teñidos con Giemsa. |
Forma de dosificación | 10 mg/kg; iv; 11d |
Áreas de aplicación | WZB117 inhibe eficazmente el crecimiento de parásitos en la etapa sanguínea. |
References: | |
| Cas No. | 1223397-11-2 | SDF | |
| Sinónimos | 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
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Quality Control & SDS
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- Purity: >99.50% Appearance: A solid
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Average Rating: 5 (Based on Reviews and 31 reference(s) in Google Scholar.)