400036
Glucose Transporter Inhibitor IV, WZB117
The Glucose Transporter Inhibitor IV, WZB117 controls the biological activity of Glucose Transporter.
Sinônimo(s):
Glucose Transporter Inhibitor IV, WZB117, 3-Fluoro-1,2-phenylene bis(3-hydroxybenzoate), GLUT Inhibitor IV, WZB117
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About This Item
Fórmula empírica (Notação de Hill):
C20H13FO6
Número CAS:
Peso molecular:
368.31
Número MDL:
Código UNSPSC:
12352200
NACRES:
NA.77
Preço e disponibilidade não estão disponíveis no momento.
Produtos recomendados
Nível de qualidade
Ensaio
≥98% (HPLC)
Formulário
powder
fabricante/nome comercial
Calbiochem®
condição de armazenamento
OK to freeze
desiccated
protect from light
cor
white
solubilidade
ethanol: 100 mg/mL
Condições de expedição
ambient
temperatura de armazenamento
−20°C
cadeia de caracteres SMILES
Fc1c(c(ccc1)OC(=O)c3cc(ccc3)O)OC(=O)c2cc(ccc2)O
Descrição geral
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).
Ações bioquímicas/fisiológicas
Cell permeable: yes
Primary Target
Glut1
Glut1
Reversible: no
Embalagem
Packaged under inert gas
Advertência
Toxicity: Standard Handling (A)
Reconstituição
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 2 weeks at -20°C. Unstable in DMSO.
Outras notas
Liu. Y., et al. 2012. Mol. Cancer Ther.11, 1672.
Informações legais
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Código de classe de armazenamento
11 - Combustible Solids
Classe de risco de água (WGK)
WGK 3
Ponto de fulgor (°F)
Not applicable
Ponto de fulgor (°C)
Not applicable
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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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