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400036

Sigma-Aldrich

Glucose Transporter Inhibitor IV, WZB117

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

Synonyme(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

Formule empirique (notation de Hill):
C20H13FO6
Numéro CAS:
1223397-11-2
Poids moléculaire :
368.31
Numéro MDL:
MFCD24387113
Code UNSPSC :
12352200

Niveau de qualité

100

Pureté

≥98% (HPLC)

Forme

powder

Fabricant/nom de marque

Calbiochem®

Conditions de stockage

OK to freeze
desiccated
protect from light

Couleur

white

Solubilité

ethanol: 100 mg/mL

Conditions d'expédition

ambient

Température de stockage

−20°C

Description générale

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).

Actions biochimiques/physiologiques

Cell permeable: yes
Primary Target
Glut1
Reversible: no

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

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

Autres remarques

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

Informations légales

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

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 3

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

Certificats d'analyse (COA)

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Consulter la Bibliothèque de documents

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

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