WZB117 is a Glucose Transporter 1 (GLUT1) inhibitor. when IC50 of WZB117 approximate 10 μM, it inhibits lung cancer A549 cells and breast cancer MCF7 cells proliferation.

GLUT1:10μM

WZB117 treats Cancer cell resulting in decreases in levels of Glut1 protein, intracellular ATP, and glycolytic enzymes. And WZB117 inhibits glucose transport in human red blood cells. The declines in cyclin E2 as well as phosphorylated retinoblastoma and increases in ATP-sensing enzyme AMP-activated protein kinase (AMPK), lead to the cell-cycle arrest, senescence, and necrosis.

WZB117 inject 10 mg/kg daily intraperitoneal into nude mice, which were grafted human A549 lung cancer, show 70% reduction in tumor volume.

Recombinant proteins expressed with Sf21 cells and baculovirus vectors are purified with affinity chromatography. JAK kinase assay is done by a homogeneous time-resolved fluorescence assay with the peptide substrate (-EQEDEPEGDYFEWLE). Each enzyme reaction is carried out with Ruxolitinib or control, JAK enzyme, 500 nM peptide, adenosine triphosphate (ATP; 1 mM), and 2% dimethyl sulfoxide (DMSO) for 1 hour. IC50 is the INCB018424 concentration required for inhibition of 50% of the fluorescent signal.

Human non–small cell lung cancer (NSCLC) cell lines H1299 and A549 are treated with compound WZB117（10 μM） for 24 or 48 hours.

Male NU/J nude mice were given intraperitoneal injection with WZB117 (10 mg/kg) daily for 10 weeks.