17β-Hydroxywortmannin is an orally active phosphatidylinositol-3-kinase (PI-3-kinase) inhibitor, exhibiting an IC50 of 0.5 nM and notably suppresses osteoclast resorption at an IC50 of 10 nM. Additionally, it demonstrates antitumor activity.

17β-Hydroxywortmannin (0.1 μg/kg，口服 5 周) 能促进破骨细胞分化，防止去卵巢大鼠因雌激素缺乏导致骨质流失[1]。同时，17β-Hydroxywortmannin (2.5 mg/kg/week，静脉注射 2 周) 对U87MG胶质瘤展示出抗肿瘤效应，且在人肿瘤异种移植裸鼠中的治疗指数达到26[2]。