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(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。

WZB117 Chemical Structure

Cas No.:1223397-11-2

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Description

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]

实验参考方法

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:
[1]. 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.
[2]. 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.

化学性质

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
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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。
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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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