Denosumab (anti-TNFSF11)

Denosumab (anti-TNFSF11) is a human monoclonal antibody that targets the protein RANKL. Denosumab binds to the receptor activator of nuclear factor kappa-B ligand (RANKL) and prevents its binding to the RANK receptor (K_D of 0.003 nM for human RANKL). Denosumab promotes proliferation and spermatogenesis. Denosumab prevents bone resorption through inhibition of the NF-κB pathway. Denosumab can be used in bone-related studies^{[1][2][3][4][5][6][7]}. In Vitro:Denosumab (0.25-20 μM, 7 days) enhances osteogenic differentiation at physiological concentrations in human mesenchymal stem cells of the jaw bone^[4].
Denosumab (0.1 μM–5 μM) alleviates ROS-induced chondrocytes Apoptosis, with promoting Bcl-2 and suppressing pro-apoptotic genes Bax and caspase-3^[5].
Denosumab (5 μM, 5-60 min) suppresses RANKL-induced osteoclastogenesis by inhibiting the NF-κB signaling pathway^[5].
Denosumab (0.001-0.1 μg/mL, 24-72 h) significantly increases human β-cell proliferation^[6].
In Vivo:Denosumab (10 mg/kg, s.c., twice a week for 4 weeks) ameliorates pain-related behaviors and osteoarthritis (OA) progression in the OA mouse model^[5].
Denosumab (1 mg/kg, s.c., single) enhances human β-cell proliferation in human islets transplanted under the kidney capsule of male euglycemic NOD/SCID mice^[6].
Denosumab (5 mg/kg, s.c., single) increases testis weight, inhibin B, and sperm count in humanized RANKL mice^[7].