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

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.