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对癌细胞进行治疗，导致Glut1蛋白、细胞内ATP和糖酵解酶水平下降。同时，WZB117抑制人类红细胞中的葡萄糖转运。cyclin E2以及磷酸化视网膜母细胞瘤蛋白的下降和ATP感应酶AMP-activated protein kinase (AMPK)的增加，导致细胞周期停滞、衰老和坏死。

WZB117每日通过腹腔注射给予裸鼠10 mg/kg，这些裸鼠被移植了人类A549肺癌细胞，结果显示肿瘤体积减少了70%。

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.