A cell-permeable thiazolidinedione compound that is shown to reversibly block glucose uptake in androgen-sensitive human prostate adenocarcinoma (LNCaP) cells transfected with GLUT1 (IC50 = 2 µM). Blocks GLUT3, GLUT4, and GLUT9-mediated transport at higher concentration (IC50 ≥ 5 µM). Binds to GLUT1 at a site that is distinct from the glucose binding site. Selectively reduces proliferation (IC50 = 2.0 µM) and induces apoptosis (IC50 = 2.5 µM) in LNCaP cells without affecting normal human prostate epithelial cells and mammary epithelial cells (~ 10 µM). Shown to elicit energy restriction-associated cellular responses in LNCaP cells, such as β-TrCP facilitated protein degradation, activation of AMP-activated kinase, and endoplasmic reticulum stress.
Biochem/physiol Actions
Cell permeable: yes
Primary Target glucose transporter
Reversible: yes
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C. Use only fresh DMSO.
Other Notes
Wang, D-S., et al. 2012, J. Med. Chem.55, 3827.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class
11 - Combustible Solids
wgk_germany
WGK 1
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
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