WZB117 Property

Boiling point:

628.4±55.0 °C(Predicted)

Density 

1.431±0.06 g/cm3(Predicted)

storage temp. 

2-8°C

solubility 

DMSO: soluble20mg/mL, clear

form 

powder

pka

8.96±0.10(Predicted)

color 

white to beige

Stability:

Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may br stored at -20° for up to 2 months.

Safety

Hazard Codes 

N

Risk Statements 

50

Safety Statements 

61

WGK Germany 

3

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

WZB117 Chemical Properties,Usage,Production

Description

WZB117 (1223397-11-2) is an inhibitor of Glucose Transporter 1 (GLUT1). It inhibited cell proliferation in lung cancer A549 cells and breast cancer MCF7 cells with an IC50 of approximately 10 μM. Daily intraperitoneal injection of WZB117 at 10mg/kg resulted in 70% reduction in tumor volume of human A549 lung cancer grafted on nude mice.

Uses

WZB 117 is a GLUT1 inhibitor.

Uses

WZB-117 has been used to study its tumor initiating ability in cancer stem cells. It has also been used to study the effect of glucose antagonists on 2-NBDG (2-(N-(7-Nitrobenz-2-oxa-1,3-diazol-4-yl)Amino)-2-Deoxyglucose) uptake.

General Description

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).

Biochem/physiol Actions

Cell permeable: yes

in vitro

previous study found that wzb117 could inhibit glucose transport in human red blood cells expressing glut1 as their sole glucose transporter. moreover, cancer cell treatment with wzb117 resulted in decreased levels of glut1 protein, intracellular atp, as well as glycolytic enzymes. all these changes were followed by increase in atp-sensing enzyme amp-activated protein kinase and declined in cyclin e2 as well as phosphorylated retinoblastoma, leading to cell-cycle arrest, senescence, and necrosis [1].

in vivo

animal study showed that the daily ip injection of wzb117 at 10 mg/kg led to a more than 70% reduction in the size of human lung cancer of a549 cell origin [1].

IC 50

~0.6 μm for blocking glucose transport in diverse cancer cells

storage

Store at +4°C

References

1) Liu?et al. (2012),?A small-molecule inhibitor of glucose transporter 1 downregulates glycolysis, induces cell-cycle arrest, and inhibits cancer cell growth in vitro and in vivo; Mol. Cancer Ther.,?11?1672