WSF1-IN-1 (compound 136), an orally active WSF1 inhibitor, can be used in the study for WSF1 (Wolfram syndrome) related tumors, with IC50 values of 0.33 μM and >27 μM in HepG2 parental and HepG2 WFS1 KO cell lines, respectively.In Vitro: WSF1-IN-1 (compound 136) exhibits IC50 values of >27 μM and 0.03 μM for Hek293 empty vector and Hek293 WFS1 over-expressor, respectively. WSF1-IN-1 (compound 136) exhibits IC50 values of 0.05 μM (Colo-205 Control shRNA), >9 μM (Colo-205 WSF1 shRNA), 0.08 μM (DU4415 Control shRNA), 6.1 μM (DU4415 WSF1 shRNA), 0.26 μM (HepG2 Control shRNA), 2.2 μM (HepG2 WSF1 shRNA) for cell valiablity, respectively.In Vivo: WSF1-IN-1 (compound 136, 100 mpk qd, orally, 14 days) exhibits 106.65% tumor growth inhibition (TGI) in NSCLC patient derived xenograft OD33996 nu/nu mice.