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

C₂₀H₁₃FO₆

368.31

MFCD24387113

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).

Cell permeable: yes
Reversible: no
Primary Target
Glut1

Toxicity: Standard Handling (A)

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

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

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

100

≥98% (HPLC)

powder

Calbiochem^®

OK to freeze
desiccated
protect from light

white

ethanol: 100 mg/mL

ambient

−20℃

25 mg in Glass bottle
Packaged under inert gas

11 - Combustible Solids

WGK 3