RANKL-IN-1 is a selective and orally active Receptor Activator of Nuclear Factor-κ B Ligand (RANKL) inhibitor with a KD value of 7.6 μM. RANKL-IN-1 exhibits inhibitory activity and selectivity against osteoclastogenesis with an IC50 value of 0.07 μM and SI of 82.57. RANKL-IN-1binds directly to RANKL and blocks the RANKL-induced activation of the NF-κB and MAPK pathways. RANKL-IN-1 can be used for the research of metabolic disease, such as osteoporosis[1].
