WZB117
(Synonyms: Glucose Transporter Inhibitor IV) 目录号 : GC13381
WZB117是一种靶向葡萄糖转运蛋白1（GLUT1）的小分子抑制剂。
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.
WZB117是一种靶向葡萄糖转运蛋白1（GLUT1）的小分子抑制剂 [1]。WZB117可降低癌细胞对葡萄糖的摄取，降低细胞内ATP水平，并激活AMPK，进而引发细胞周期停滞、衰老和坏死 [2-3]。WZB117主要用于肿瘤研究领域，抑制癌细胞的葡萄糖代谢和生长 [4]。
在A375和SK-MEL-28细胞中，阿帕替尼与WZB117（0-160μM；24h、48h、72h）联合用药对细胞生长有协同抑制作用 [5]。在PANC-1细胞中，WZB117（10μM、25μM；24h）以剂量依赖性方式显著降低细胞糖原分解 [6]。在SH-SY5Y细胞中，WZB117（1-30μM；72h）治疗可降低肿瘤细胞活力并下调GLUT1蛋白水平 [7]。
在感染伯氏疟原虫ANKA的小鼠模型中，WZB117（10mg/kg；ip；11d）可有效抑制血液阶段寄生虫的生长 [8]。在PANC-1 CSLC皮下肿瘤小鼠模型中，WZB117（20mg/kg；ip；20d）可抑制PANC-1 CSLC在体内的肿瘤起始能力 [9]。
| 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 | |
| 别名 | Glucose Transporter Inhibitor IV | ||
| 化学名 | 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 | ||
| 分子式 | C20H13FO6 | 分子量 | 368.3 |
| 溶解度 | ≥ 18.4mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.7152 mL | 13.5759 mL | 27.1518 mL |
| 5 mM | 0.543 mL | 2.7152 mL | 5.4304 mL |
| 10 mM | 0.2715 mL | 1.3576 mL | 2.7152 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
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计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
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2.
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Quality Control & SDS
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- Purity: >99.50%
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