Following our published report regarding the anti-Hh signaling effects of Oxy16 (Figure 1), a naturally occurring oxysterol, we screened numerous semi-synthetic analogues of Oxy16 in cell-based assays and selected Oxy210 as a lead compound based on: (1) the significantly enhanced biological activity of Oxy210 in inhibiting Hh as well as TGFβ signaling in vitro in NIH3T3 and human NSCLC cells relative to Oxy16, (2) ease of synthesis and scale up, and (3) favorable metabolic stability derived from in vitro human and mouse liver microsomal assays. The gene discussed is TGFB1; the disease is non-small cell lung carcinoma.