GNF-2 is an inhibitor of Abl kinase that exhibits anticancer chemotherapeutic, anti-resorptive, and anti-osteoporotic activities. GNF-2 causes a dose-dependent growth inhibition of the Bcr-abl–positive cell lines with IC50 values of 273 nM (K562) and 268 nM (SUP-B15). GNF-2 shows potential benefit in the treatment of Philadelphia chromosome-positive acute myelogenous leukemia (ALL). In vitro, GNF-2 inhibits differentiation of osteoclasts, activity of NF-κB, and induction of c-Fos and NFATc1, resulting in caspase-mediated apoptosis. GNF-2 also inhibits resorption of mature osteoclasts and prevents phagocytosis in bone marrow-derived macrophages. In vivo, this compound decreases osteoclast numbers and prevents bone loss.