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Merck
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文件

400036

Sigma-Aldrich

葡萄糖转运蛋白抑制剂 IV,WZB117-CAS 1223397-11-2-Calbiochem

The Glucose Transporter Inhibitor IV, WZB117 controls the biological activity of Glucose Transporter.

别名:

Glucose Transporter Inhibitor IV, WZB117, 3-Fluoro-1,2-phenylene bis(3-hydroxybenzoate), GLUT Inhibitor IV, WZB117

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About This Item

经验公式(希尔记法):
C20H13FO6
分子量:
368.31
MDL號碼:
分類程式碼代碼:
12352200
NACRES:
NA.77

品質等級

化驗

≥98% (HPLC)

形狀

powder

製造商/商標名

Calbiochem®

儲存條件

OK to freeze
desiccated
protect from light

顏色

white

溶解度

ethanol: 100 mg/mL

運輸包裝

ambient

儲存溫度

−20°C

一般說明

A bis-hydroxybenzoate compound that acts as a fast-acting, irreversible blocker of glucose transport by GLUT1 in red blood cells. Shown to rapidly inhibit glucose transport in cancer cells (IC50 ~ 500 nM in A549 cells) and block proliferation. Its inhibitory effects are more pronounced in hypoxic cancer cells. It binds directly to GLUT1 involving three hydrogen bonds, one each with Asn34, Arg126, and Trp412. Also shown to reduce the levels of GLUT1 protein, intracellular ATP levels, and glycolytic enzymes and increase the level of AMPK in tumor cells. Preferentially induces cell cycle arrest and causes senescence and necrosis in red blood cells and tumor cells (IC50 = 10 µM) over non cancerous cells and synergizes the anti-tumor effects of cisplatin (>Cat. No. 232120) and paclitaxel (>Cat. No. 580555). Also, effectively suppresses tumor growth in human A549 lung cancer grafted nude mice model (10 mg/kg, i.p., daily).

生化/生理作用

Cell permeable: yes
Primary Target
Glut1
Reversible: no

包裝

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重構

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 2 weeks at -20°C. Unstable in DMSO.

其他說明

Liu. Y., et al. 2012. Mol. Cancer Ther.11, 1672.

法律資訊

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


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Victoria Sanchez-Martin et al.
Cell chemical biology, 28(11), 1590-1601 (2021-06-25)
Guanine quadruplexes (G4s) are non-canonical nucleic acid structures commonly found in regulatory genomic regions. G4 targeting has emerged as a therapeutic approach in cancer. We have screened naphthalene-diimides (NDIs), a class of G4 ligands, in a cellular model of colorectal
Giulia Salvadori et al.
Cell metabolism, 33(11), 2247-2259 (2021-11-04)
Metastatic tumors remain lethal due to primary/acquired resistance to therapy or cancer stem cell (CSC)-mediated repopulation. We show that a fasting-mimicking diet (FMD) activates starvation escape pathways in triple-negative breast cancer (TNBC) cells, which can be identified and targeted by
Fiona Grimm et al.
The EMBO journal, 43(8), 1545-1569 (2024-03-15)
Adaptation to chronic hypoxia occurs through changes in protein expression, which are controlled by hypoxia-inducible factor 1α (HIF1α) and are necessary for cancer cell survival. However, the mechanisms that enable cancer cells to adapt in early hypoxia, before the HIF1α-mediated

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